US2008108598A1PendingUtilityA1
Pharmaceutical use of substituted amides
Est. expiryFeb 7, 2023(expired)· nominal 20-yr term from priority
Inventors:Henrik Sune AndersenGita Camilla Tejlgaard KampenInge Thoger ChristensenJohn Patrick MogensenAnnette Rosendal LarsenJohn Paul Kilburn
A61P 3/10A61K 45/06C07D 401/06C07D 401/12A61P 3/04C07D 209/02A61P 3/00A61K 31/16C07D 487/08A61K 31/415C07D 403/12
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Claims
Abstract
The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Claims
exact text as granted — not AI-modified1 . A method of modulating of the activity of 11βHSD1, or inhibiting 11βHSD1, comprising administering to a patient in need of such method a therapeutically effective amount of a substituted amide, a prodrug thereof, or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture or tautomeric forms thereof.
2 . A method for the treatment, prevention and/or prophylaxis of any disorder and disease where it is desirable to modulate the activity of 11βHSD1, or inhibit 11βHSD1, comprising administering to a patient in need of such method a therapeutically effective amount of a substituted amide, a prodrug thereof, or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture or any tautomeric forms thereof.
3 . The method according to claim 2 , wherein the substituted amide or a prodrug thereof is of formula (I)
wherein
R 1 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl, wherein the cycloalkyl, hetcycloalkyl, alkyl, arylalkyl and hetarylalkyl groups independently are optionally substituted with one or more of R 4 .
R 2 is hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl wherein the alkyl, aryl and cycloalkyl groups independently are optionally substituted with one or more of R 5 ; or
R 1 and R 2 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 14 ;
R 3 is C 1 -C 8 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, aryl-R 6 —C 1 -C 6 alkyl, hetaryl-R 6 —C 1 -C 6 alkyl or arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl wherein the alkyl, cycloalkyl, hetcycloalkyl, alkenyl, alkynyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 ;
R 4 and R 5 independently are hydrogen, hydroxy, oxo, cyano, halo, methylendioxo, NR 8 R 9 , C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethyloxy, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkenyl, aryl, hetaryl, hetarylSO n , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylcarbonyl, hetarylC 1 -C 6 alkyl-carbonyl, C 1 -C 6 alkylSO n , C 1 -C 6 alkyl-carboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 15 ;
R 6 is oxygen, sulphur, SO n or NR 16 ;
R 7 is hydrogen, halo, hydroxy, cyano, nitro, COOR 17 , C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, methylendioxo, trihalomethyl, trihalomethyloxy, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, NR 8 R 9 , SO 2 NR 8 R 9 , NR 4 R 5 carbonylC 1 -C 6 alkyl, arylthio, hetarylthio, R 18 carbonylNR 8 , arylSO n , hetarylSO n , R 19 SO m NR 8 , arylthioC 1 -C 6 alkyl, hetarylthioC 1 -C 6 alkyl or arylC 1 -C 6 alkylR 6 C 1 -C 6 alkyl; wherein the aryl and hetaryl groups independently are optionally substituted with one or more R 10 ;
R 8 and R 9 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 11 ; or
R 8 and R 9 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system optionally being substituted with at least one halo, cyano, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkyl-carbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, hydroxy, oxo, halo, cyano, nitro, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, NR 12 R 13 , methylendioxo, trihalomethyl or trihalomethyloxy;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl or arylC 1 -C 6 alkyl;
R 14 is hydrogen, halo, hydroxy, oxo, nitro, cyano, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy or aryloxy;
R 15 is hydrogen, halo, hydroxy, oxo, nitro, cyano, CONR 8 R 9 or COOR 17 ;
R 16 is hydrogen, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, aryloxyC 1 -C 6 alkyl, hetaryloxyC 1 -C 6 alkyl, arylthioC 1 -C 6 alkyl or hetarylthioC 1 -C 6 alkyl; wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 10 ;
R 17 is hydrogen, C 1 -C 8 alkyl, aryl or arylC 1 -C 6 alkyl;
R 18 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxyC 1 -C 6 alkyl or R 8 R 9 NC 1 -C 6 alkyl wherein the alkyl, alkenyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups are optionally substituted with R 15 ;
R 19 is C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl;
m is 1 or 2;
n is 0, 1 or 2; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
4 . The method according to claim 3 , wherein the substituted amide or a prodrug thereof is of formula (I)
wherein
R 1 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl, wherein the cycloalkyl, hetcycloalkyl, alkyl, arylalkyl and hetarylalkyl groups independently are optionally substituted with one or more of R 4 ;
R 2 is hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl wherein the alkyl, aryl and cycloalkyl groups independently are optionally substituted with one or more of R 5 ; or
R 1 and R 2 are together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1-6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 14 ;
R 3 is C 1 -C 8 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, aryl-R 6 —C 1 -C 6 alkyl, hetaryl-R 6 —C 1 -C 6 alkyl or arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl wherein the alkyl, cycloalkyl, hetcycloalkyl, alkenyl, alkynyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 ;
R 4 and R 5 independently are hydrogen, hydroxy, oxo, cyano, halo, methylendioxo, NR 8 R 9 , C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethyloxy, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkenyl, aryl, hetaryl, hetarylSO n , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylcarbonyl, hetarylC 1 -C 6 alkyl-carbonyl, C 1 -C 6 alkylSO n , C 1 -C 6 alkyl-carboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 15 ;
R 6 is oxygen, sulphur, SO n , NR 16 ;
R 7 is hydrogen, halo, hydroxyl, cyano, nitro, COOR 7 , C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, methylendioxo, trihalomethyl, trihalomethyloxy, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, NR 8 R 9 , SO 2 NR 8 R 9 , NR 4 R 5 carbonylalkyl, arylcarbonylNR 8 , arylthio, hetarylthio, arylSO n , hetarylSO n , arylSO m NR 8 , arylthioC 1 -C 6 alkyl, hetarylthioC 1 -C 6 alkyl or arylC 1 -C 6 alkylR 6 C 1 -C 6 alkyl; wherein the aryl and hetaryl groups independently are optionally substituted with one or more R 10 ;
R 8 and R 9 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 11 ; or
R 8 and R 9 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system optionally being substituted with at least one C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkyl-carboxy or hetarylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, hydroxy, oxo, halo, cyano, nitro, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, NR 12 R 13 , methylendioxo, trihalomethyl or trihalomethyloxy;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl or arylC 1 -C 6 alkyl;
R 14 is hydrogen, halo, hydroxy, oxo, nitro, cyano, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy or aryloxy;
R 15 is hydrogen, halo, hydroxy, oxo, nitro, cyano or COOR 17 ;
R 16 is hydrogen, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, aryloxyC 1 -C 6 alkyl, hetaryloxyC 1 -C 6 alkyl, arylthioC 1 -C 6 alkyl or hetarylthioC 1 -C 6 alkyl; wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 10 ;
R 17 is hydrogen, C 1 -C 8 alkyl, aryl or arylC 1 -C 6 alkyl;
m is 1 or 2;
n is 0, 1 or 2; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
5 . The method according to claim 3 , wherein R 1 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 4 .
6 . The method according to claim 3 , wherein R 2 is hydrogen or C 1 -C 8 alkyl, wherein the alkyl group is optionally substituted with one or more of R 5 .
7 . The method according to claim 3 , wherein R 1 and R 2 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 14 .
8 . The method according to claim 3 , wherein R 3 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, aryl-R 6 —C 1 -C 6 alkyl, hetaryl-R 6 —C 1 -C 6 alkyl or arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 .
9 . The method according to claim 3 , wherein R 4 and R 5 independently are hydrogen, hydroxy, oxo, halo, C 1 -C 8 alkyl, wherein the alkyl group is optionally substituted with one or more of R 15 .
10 . The method according to claim 3 , wherein R 5 is oxygen.
11 . The method according to claim 3 , wherein R 7 is hydrogen, halo, hydroxy, cyano, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, trihalomethyl, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, NR 8 R 9 , NR 4 R 5 carbonylC 1 -C 6 alkyl, R 18 carbonylNR 8 , R 19 SO m NR 8 , wherein the aryl and hetaryl groups independently are optionally substituted with one or more R 10 .
12 . The method according to claim 3 , wherein R 8 and R 9 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system optionally being substituted with at least one halo, cyano, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy.
13 . The method according to claim 3 , wherein R 15 is CONR 8 R 9 .
14 . The method according to claim 3 , wherein R 18 is C 1 -C 6 alkyl.
15 . The method according to claim 3 , wherein the substituted amide or a prodrug thereof of formula (I) is selected from the group consisting of:
3-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-1-[4-(1H-imidazol-4-yl)-piperidin-1-yl]-propan-1-one; 4-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-1-[4-(3H-imidazol-4-yl)-piperidin-1-yl]-butan-1-one; 2,4-Bis-benzyloxy-benzamide; (1H-Indol-4-yl)-piperidin-1-yl-methanone; N-(1,4-Dioxo-1,4-dihydro-naphthalen-2-yl)-benzamide; N-(2,3-Dihydroxy-propyl)-2-(2-phenyl-adamantan-2-yl)-acetamide; (6-Fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-phenyl-methanone; (2-Chloro-phenyl)-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; 3-Cyclopentyl-1-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-propan-1-one; (3-Chloro-thieno[2,3-b]thiophen-2-yl)-thiomorpholin-4-yl-methanone; 2-[2-(4-Chloro-phenyl)-adamantan-2-yl]-1-[4-(4-methoxy-phenyl)-piperazin-1-yl]-ethanone; 1-(4-Benzyl-piperazin-1-yl)-2-[2-(4-chloro-phenyl)-adamantan-2-yl]-ethanone; 2-[2-(4-Chloro-phenyl)-adamantan-2-yl]-1-(4-methyl-piperazin-1-yl)-ethanone; 1-[4-(6-Chloro-pyridin-2-yl)-piperazin-1-yl]-2-(2-phenyl-adamantan-2-yl)-ethanone; 4-Chloro-N-(1,7,7-trimethyl-bicyclo[2.2.1]hept-2-yl)-benzamide; 3-Chloro-benzo[b]thiophene-2-carboxylic acid (2-cyano-ethyl)-cyclohexyl-amide; 2-[2-(Bicyclo[2.2.1]hept-5-en-2-ylamino)-4-oxo-4,5-dihydro-thiazol-5-yl]-N-(2-chloro-phenyl)acetamide; [3-(4-sec-Butyl-phenoxy)-phenyl]-piperidin-1-yl-methanone; 3-(6-Chloro-pyridin-2-yloxy)-N-ethyl-benzamide; N-Benzyl-2,4-dichloro-N-pyridin-2-yl-benzamide; 2-[Benzoyl-(3-chloro-4-fluoro-phenyl)-amino]-propionic acid butyl ester; 2-[Benzoyl-(3-chloro-4-fluoro-phenyl)-amino]-propionic acid pentyl ester; 3-(4-Fluoro-phenyl)-1-(4-phenyl-piperidin-1-yl)-but-2-en-1-one; N-(1,7,7-Trimethyl-bicyclo[2.2.1]hept-2-yl)-benzamide; 1-(3-Cyclopentyl-propionyl)-piperidine-3-carboxylic acid ethyl ester; 4-Phenyl-1-phenylacetyl-piperidine-4-carbonitrile; 1-Octanoyl-4-phenyl-piperidine-4-carbonitrile; 2,2-Dimethyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-propan-1-one; (4-Chloro-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-[1-(4-Methanesulfonyl-phenyl)-ethyl]-N-(tetrahydro-furan-2-ylmethyl)-benzamide; 2-(2-Amino-phenylsulfanyl)-1-(5-fluoro-2,3-dihydro-indol-1-yl)-ethanone; N-(1-Methyl-2,3-dihydro-1H-indol-5-ylmethyl)-N-(tetrahydro-furan-2-ylmethyl)-benzamide; 1-Benzoyl-piperidine-2-carboxylic acid ethyl ester; N-(2-Chloro-phenyl)-2-(1,2,3,4-tetrahydro-isoquinolin-1-yl)-acetamide; (Decahydro-naphthalen-1-yl)-(4-methyl-piperazin-1-yl)-methanone; (4-Methyl-piperazin-1-yl)-(2-p-tolylsulfanyl-phenyl)-methanone; Adamantane-1-carboxylic acid (3-benzyloxy-2-ethyl-6-methyl-pyridin-4-yl)-amide; (6-Fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-(3,4,5-trimethoxy-phenyl)-methanone; N-Bicyclo[2.2.1]hept-2-yl-3-cyclopentyl-propionamide; (2-Benzo[1,2,5]oxadiazol-5-yl-thiazol-4-yl)-piperidin-1-yl-methanone; Thiophene-2-carboxylic acid [4-(4-fluoro-phenyl)-4-hydroxy-butyl]-isopropyl-amide; N-Cyclohexyl-3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionamide; 2-[(Adamantane-1-carbonyl)-amino]-3-(1H-indol-3-yl)-propionic acid methyl ester; Adamantane-1-carboxylic acid [3-(1H-benzoimidazol-2-ylsulfanyl)-5-nitro-phenyl]-amide; N-Benzyl-N-(1-cyclopropyl-ethyl)-4-fluoro-benzamide; Thiophene-2-carboxylic acid 2-[2-(2-phenyl-adamantan-2-yl)-acetylamino]-ethyl ester; N-(4-Acetyl-phenyl)-2-(2-phenyl-adamantan-2-yl)-acetamide; 2-[2-(4-Chloro-phenyl)-adamantan-2-yl]-N-(2-hydroxy-ethyl)-acetamide; (4-Benzoyl-piperidin-1-yl)-thiophen-2-yl-methanone; N-(2-Benzoyl-4-methyl-phenyl)-3-phenyl-acrylamide; N-(2-Benzoyl-4-methyl-phenyl)-2-fluoro-benzamide; Adamantane-1-carboxylic acid (4-ethoxy-benzothiazol-2-yl)-amide; Adamantane-1-carboxylic acid (5-benzoyl-4-phenyl-thiazol-2-yl)-amide; 3-(2-Hydroxy-phenyl)-1,3-di-piperidin-1-yl-propan-1-one; N-(1-Methyl-2-phenyl-ethyl)-3-phenyl-propionamide; 4-Oxo-4-piperidin-1-yl-butyric acid 4-tert-butyl-cyclohexyl ester; N-tert-Butyl-N-(4-methoxy-benzyl)-4-nitro-benzamide; {4-[(Adamantane-1-carbonyl)-amino]-phenoxy}-acetic acid; 2-(4-Isobutyl-phenyl)-N-(1-phenyl-ethyl)-propionamide; Adamantane-1-carboxylic acid 4-[(adamantane-1-carbonyl)-amino]-2,6-dimethyl-pyridin-3-yl ester; 2-Phenyl-1-(3-phenyl-pyrrolidin-1-yl)-ethanone; Adamantane-1-carboxylic acid 4-[(adamantane-1-carbonyl)-amino]-2-ethyl-6-methyl-pyridin-3-yl ester; N-(1,3-Dioxo-1,3-dihydro-isoindol-2-ylmethyl)-N-(4-hydroxy-phenyl)-benzamide; Biphenyl-4-yl-piperidin-1-yl-methanone; Azepan-1-yl-(3,5-dichloro-phenyl)-methanone; Azepan-1-yl-biphenyl-4-yl-methanone; Azepan-1-yl-(4-chloro-phenyl)-methanone; 3-Heptylcarbamoyl-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid; Adamantan-1-yl-azepan-1-yl-methanone; N,N-Dibenzyl-3,4-dimethoxy-benzamide; N-Benzyl-N-isopropyl-4-nitro-benzamide; N-[2-(1H-Indol-3-yl)-1-methyl-ethyl]-2-(4-isobutyl-phenyl)-propionamide; N-tert-Butyl-2-(4-isobutyl-phenyl)-propionamide; Adamantane-1-carboxylic acid (2-acetyl-phenyl)-amide; N-(1,3-Dioxo-1,3-dihydro-isoindol-2-ylmethyl)-N-(4-fluoro-phenyl)-benzamide; (Octahydro-quinolin-1-yl)-phenyl-methanone; (7-Hydroxy-octahydro-quinolin-1-yl)-phenyl-methanone; N-(1,3-Dioxo-1,3-dihydro-isoindol-2-ylmethyl)-N-p-tolyl-benzamide; N,N-Dibenzyl-4-methyl-benzamide; (2-Chloro-phenyl)-(2-methyl-piperidin-1-yl)-methanone; [4-Bromo-3-(piperidine-1-sulfonyl)-phenyl]-piperidin-1-yl-methanone; 2-Chloro-N-(3,4-dimethyl-phenyl)-benzamide; 1-Azepan-1-yl-2-(3,3-dimethyl-3,4-dihydro-2H-isoquinolin-1-ylidene)-ethanone; N-Cyclohexyl-4-(2,4-dichloro-phenoxy)-butyramide; N-Benzo[1,3]dioxol-5-yl-2-chloro-benzamide; (4-Benzyl-piperidin-1-yl)-(2-chloro-phenyl)-methanone; 2-(Benzothiazol-2-ylsulfanyl)-N-cyclohexyl-acetamide; Cyclohexanecarboxylic acid (7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-quinazolin-2-yl)-amide; 2,4-Dichloro-N-ethyl-N-o-tolyl-benzamide; (4-Benzyl-piperidin-1-yl)-(4-fluoro-phenyl)-methanone; N-Cyclohexyl-4-(2,4-dichloro-phenoxy)-N-methyl-butyramide; 3-[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-ethyl]-adamantane-1-carboxylic acid; Morpholin-4-yl-(3-p-tolyl-adamantan-1-yl)-methanone; N-Benzyl-2,4-dichloro-N-methyl-benzamide; Thiophene-2-carboxylic acid dibenzylamide; Azepan-1-yl-(2-bromo-phenyl)-methanone; (3,4-Dichloro-phenyl)-(4-methyl-piperidin-1-yl)-methanone; N,N-Dibenzyl-3,4-dichloro-benzamide; 4-(2,4-Dichloro-phenoxy)-1-piperidin-1-yl-butan-1-one; N,N-Dibenzyl-2-fluoro-benzamide; (2-Chloro-phenyl)-piperidin-1-yl-methanone; 2-Chloro-N-(3-trifluoromethyl-phenyl)-benzamide; N-Benzyl-N-ethyl-2-phenyl-acetamide; (3,4-Dihydro-2H-quinolin-1-yl)-p-tolyl-methanone; Thiophene-2-carboxylic acid benzyl-ethyl-amide; N-Adamantan-1-yl-2-dibenzylamino-acetamide; N-Cyclohexyl-2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionamide; Thiophene-2-carboxylic acid cycloheptylamide; N-Cyclohexyl-3-diethylsulfamoyl-4-methyl-benzamide; 4-Benzoyl-N-methyl-N-phenyl-benzamide; N-Benzyl-2-bromo-N-methyl-benzamide; 2-Chloro-N-methyl-N-phenyl-benzamide; 4-Chloro-N-ethyl-N-o-tolyl-benzamide; N-Benzyl-4,N-dimethyl-benzamide; 2-(4-Chloro-3,5-dimethyl-phenoxy)-N-cyclohexyl-N-methyl-acetamide; N-Benzyl-2-bromo-N-isopropyl-benzamide; 3-(2-Chloro-phenyl)-N-cyclohexyl-N-methyl-acrylamide; N-Phenyl-N-(2,2,5-trimethyl-hex-4-enyl)-acetamide; N-m-Tolyl-N-(2,2,5-trimethyl-hex-4-enyl)-acetamide; (3-Chloro-benzo[b]thiophen-2-yl)-(4-methyl-piperazin-1-yl)-methanone; Adamantane-1-carboxylic acid (5-methyl-pyridin-2-yl)-amide; 3-Bromo-N-[2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-butyl]-benzamide; 4-Chloro-N-[2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-butyl]-benzamide; 4-Methyl-N-[2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-butyl]-benzamide;
Cyclohexanecarboxylic acid [2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)butyl]-amide;
3-Cyclopentyl-N-[2-methyl-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-butyl]-propionamide; 2-Chloro-N-[2-(4-ethyl-benzoylamino)-ethyl]-N-(4-fluoro-phenyl)-benzamide; N-{1-Benzyl-2-[4-(3-cyclopentyl-propionyl)-piperazin-1-yl]-2-oxo-ethyl}-3-cyclopentyl-propionamide; N-Bicyclo[2.2.1]hept-5-en-2-ylmethyl-3-cyclopentyl-N-[2-(1H-indol-3-yl)-ethyl]-propionamide; N-Bicyclo[2.2.1]hept-5-en-2-ylmethyl-2,4-dichloro-N-[2-(1H-indol-3-yl)-ethyl]-benzamide; Naphthalene-2-carboxylic acid (2-oxo-azepan-3-yl)-thiophen-3-ylmethyl-amide; 3,4,5-Trimethoxy-N-(4-methyl-benzyl)-N-[6-(pyridin-2-ylamino)-hexyl]-benzamide; 3-Cyclopentyl-N-(4-methyl-benzyl)-N-[6-(pyridin-2-ylamino)-hexyl]-propionamide; N-(3,4-Dimethoxy-benzyl)-3-methoxy-N-[6-(pyridin-2-ylamino)-hexyl]-benzamide; N,N-Dimethyl-2-[3-(4-nitro-phenyl)-adamantan-1-yl]-acetamide; Adamantane-1-carboxylic acid [4-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-butyl]-p-tolyl-amide; 2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-methyl-N-(2-trifluoromethyl-phenyl)-butyramide; 2-(4-Chloro-2-methyl-phenoxy)-N-(2-trifluoromethyl-phenyl)-propionamide; 4-(2,4-Dichloro-phenoxy)-1-[4-(4-fluoro-phenyl)-piperazin-1-yl]-butan-1-one; (3,4-Dihydro-2H-quinolin-1-yl)-[3-(piperidine-1-sulfonyl)-phenyl]-methanone; Acetic acid 4-(azepane-1-carbonyl)-phenyl ester; N-Adamantan-1-ylmethyl-benzamide; [3-(4-Nitro-phenyl)-adamantan-1-yl]-piperidin-1-yl-methanone; N-(1,1-Dimethyl-hexyl)-2-morpholin-4-yl-acetamide; Adamantyl-1-carboxylic acid (2-methoxy-ethyl)-amide; N-(4-Adamantan-1-yl-2-methyl-phenyl)-acetamide; 3-p-Tolyl-adamantane-1-carboxylic acid (2,5-dichloro-phenyl)-amide; (3-Chloro-adamantan-1-yl)-pyrrolidin-1-yl-methanone; 2-Amino-5-cyclohexylcarbamoyl-4-methyl-thiophene-3-carboxylic acid ethyl ester; N-(2-Chloro-phenyl)-2-{3-[(2-chloro-phenylcarbamoyl)-methyl]-adamantan-1-yl}-acetamide; 3-p-Tolyl-adamantane-1-carboxylic acid (2,4-difluoro-phenyl)-amide; Adamantyl-1-carboxylic acid tert-butylamide; 2-Adamantan-1-yl-N-tert-butyl-acetamide; N-Methyl-N-phenyl-4-(pyrrolidine-1-sulfonyl)-benzamide; N-(1-Adamantan-1-yl-ethyl)-2-fluoro-benzamide; Adamantane-1-carboxylic acid [2-(3,4-dimethoxy-phenyl)-ethyl]-amide; Adamantane-1-carboxylic acid dimethylamide; N-Benzyl-4-chloro-N-(1-cyclopropyl-vinyl)-benzamide; 3,5-Dimethyl-adamantane-1-carboxylic acid benzylamide; 2,4-Dichloro-N-cyclohexyl-N-(2-hydroxy-ethyl)-benzamide; N-Adamantan-1-yl-2,4-dichloro-N-ethyl-benzamide; 2-[(3-p-Tolyl-adamantane-1-carbonyl)-amino]-propionic acid methyl ester; N-Adamantan-1-yl-3-morpholin-4-yl-propionamide; 3-p-Tolyl-adamantane-1-carboxylic acid isopropylamide; N-Adamantan-1-yl-2-benzylamino-acetamide; N-Benzyl-2,4-dichloro-N-(1-cyclopropyl-ethyl)-5-methyl-benzamide; 2-[(Adamantane-1-carbonyl)-amino]-benzoic acid ethyl ester; N-Benzyl-N-isopropyl-4-methyl-3-nitro-benzamide; (3,4-Dihydro-2H-quinolin-1-yl)-(2-fluoro-phenyl)-methanone; N-Ethyl-2-fluoro-N-phenyl-benzamide; 2-Phenethyl-N-(2-trifluoromethyl-phenyl)-benzamide; 1-(3,4-Dihydro-2H-quinolin-1-yl)-2-o-tolyloxy-ethanone; 2-(1-Benzyl-1H-imidazol-2-ylsulfanyl)-N-cyclohexyl-acetamide; Cyclohexanecarboxylic acid (2-propoxy-phenyl)-amide; 2-{3-[4-(2-Chloro-phenyl)-piperazin-1-yl]-3-oxo-propyl}-isoindole-1,3-dione; N-Cyclopentyl-2-(2,4-dichloro-phenoxy)-propionamide; Adamantane-1-carboxylic acid (2-trifluoromethyl-phenyl)-amide; (4-Chloro-3-nitro-phenyl)-(2,6-dimethyl-piperidin-1-yl)-methanone; 4-(2-Ethyl-phenyl)-4-aza-tricyclo[5.2.2.0 2,6 ]undec-8-ene-3,5-dione; 2-Phenyl-N-(2-trifluoromethyl-phenyl)-butyramide; N-Adamantan-1-yl-4-chloro-2-nitro-benzamide; 3-p-Tolyl-adamantane-1-carboxylic acid (2,3-dimethyl-phenyl)-amide; N-Benzyl-3-methyl-4-p-tolyl-butyramide; N-(2-Cyclohex-1-enyl-ethyl)-2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionamide; (4-tert-Butyl-phenyl)-(3,4-dihydro-1H-isoquinolin-2-yl)-methanone; 2-[1-(4-Chloro-benzenesulfonyl)-1H-benzoimidazol-2-ylsulfanyl]-N-thiophen-2-ylmethyl-acetamide; 2-Phenoxy-1-[4-(2-trifluoromethyl-benzyl)-piperazin-1-yl]-ethanone; Cyclohexanecarboxylic acid [5-(2-fluoro-benzylsulfanylmethyl)-[1,3,4]thiadiazol-2-yl]-amide; 4-Methyl-2-phenyl-thiazole-5-carboxylic acid naphthalen-1-ylamide; 4-Fluoro-N-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-benzenesulfonamide; (3-Methoxy-phenyl)-(4-o-tolyl-piperazin-1-yl)-methanone; N-Adamantan-1-yl-3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propionamide; N-Cyclooctyl-2-methoxy-3-methyl-benzamide; 2-[4-(2,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-isoindole-1,3-dione; (2,3-Diphenyl-quinoxalin-6-yl)-(2,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Adamantan-1-yl-(1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl)-methanone; N-{4-[1-(Naphthalene-2-sulfonyl)-piperidin-3-yl]-butyl}-N′-p-tolyl-oxalamide; N-Benzyl-N-(2-oxo-2-pyrrolidin-1-yl-ethyl)-benzenesulfonamide; (4-Amino-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 1-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-2-(2-isopropyl-5-methyl-phenoxy)-ethanone; Adamantane-1-carboxylic acid benzyl-pyridin-2-yl-amide; Adamantan-1-yl-piperidin-1-yl-methanone; Adamantan-1-yl-pyrrolidin-1-yl-methanone; (3,4-Dihydro-2H-quinolin-1-yl)-o-tolyl-methanone; Adamantyl-1-carboxylic acid benzylamide; Pyridine-2-carboxylic acid adamantan-2-ylamide; (3-Chloro-adamantan-1-yl)-piperidin-1-yl-methanone; Adamantan-1-yl-(4-methyl-piperidin-1-yl)-methanone; 2-[3-(Azepane-1-carbonyl)-phenyl]-isoindole-1,3-dione; 2-[3-(Piperidine-1-carbonyl)-phenyl]-isoindole-1,3-dione; 4-(Benzyl-methanesulfonyl-amino)-N-furan-2-ylmethyl-benzamide; (4-Nitro-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 1-Cyclohexyl-5-oxo-pyrrolidine-3-carboxylic acid (4-chloro-3-nitro-phenyl)-amide; N-(2-Chloro-phenyl)-2-(2-oxo-2-phenyl-ethylsulfanyl)-acetamide; 3-(4-Hydroxy-phenyl)-N-isochroman-1-ylmethyl-3-phenyl-propionamide; (4-Ethoxy-phenyl)-(2-methyl-piperidin-1-yl)-methanone; 1-Cyclohexyl-5-oxo-pyrrolidine-3-carboxylic acid (3-chloro-phenyl)-amide; N-[4-(Benzyl-isopropyl-sulfamoyl)-phenyl]-acetamide; N-(3,4-Dimethyl-phenyl)-N-[4-(piperidine-1-carbonyl)-benzyl]-methanesulfonamide; 2-(5-Phenyl-1H-imidazol-2-ylsulfanyl)-N-(1,1,3,3-tetramethyl-butyl)-acetamide; 2-(Benzothiazol-2-ylsulfanyl)-N-(1,1,3,3-tetramethyl-butyl)-acetamide; 2-(Benzooxazol-2-ylsulfanyl)-N-(1,1,3,3-tetramethyl-butyl)-acetamide; 2-(Naphthalen-2-ylcarbamoylmethylsulfanyl)-N-(1,1,3,3-tetramethyl-butyl)-acetamide; Acetic acid 4-(3,5-dimethyl-piperidine-1-carbonyl)-phenyl ester; [1-(4-Chloro-benzenesulfonyl)-piperidin-3-yl]-(octahydro-quinolin-1-yl)-methanone; (4-Fluoro-phenyl)-(3,4,4a,8a-tetrahydro-2H-quinolin-1-yl)-methanone; N-Adamantan-1-yl-2-ethoxy-acetamide; 2-(2-Oxo-2-phenothiazin-10-yl-ethyl)-hexahydro-isoindole-1,3-dione; Adamantane-1-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide; 2-Bromo-N-cycloheptyl-benzamide; Bicyclo[2.2.1]hept-2-yl-[4-(2-ethoxy-phenyl)-piperazin-1-yl]-methanone; N-Furan-2-ylmethyl-2-phenyl-2-phenylsulfanyl-acetamide; Adamantane-1-carboxylic acid benzyl-methyl-amide; 1-(3,4-Dihydro-2H-quinolin-1-yl)-3-(4-fluoro-phenyl)-propenone; Adamantan-1-yl-(2,6-dimethyl-piperidin-1-yl)-methanone; 4-Methyl-N-homoadamantyl-3-yl-benzamide; (3,5-Dimethyl-piperidin-1-yl)-(3-methyl-4-nitro-phenyl)-methanone; Quinoline-2-carboxylic acid cyclooctylamide; Adamantane-1-carboxylic acid [2-(2,4-dimethoxy-phenyl)-ethyl]-amide; (3,4-Dihydro-1H-isoquinolin-2-yl)-o-tolyl-methanone; (3,6-Dichloro-benzo[b]thiophen-2-yl)-(4-methyl-piperazin-1-yl)-methanone; 3-(1-Benzyl-1H-imidazol-2-ylsulfanyl)-N-cyclohexyl-propionamide; Propionic acid 2-amino-4-methyl-5-p-tolylcarbamoyl-thiophen-3-yl ester; 2-Cyclohexyl-N-(2,6-dimethyl-phenyl)-N-furan-2-ylmethyl-acetamide; (3-Methoxy-phenyl)-(2,2,4-trimethyl-4-phenyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; 1-[4-(2,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-2,5-dione; 1-(3,4-Dihydro-2H-quinolin-1-yl)-2-(1-naphthalen-1-yl-1H-tetrazol-5-ylsulfanyl)-ethanone; [4-(2,3-Dimethyl-phenyl)-piperazin-1-yl]-o-tolyl-methanone; (4-Benzyl-piperidin-1-yl)-(4-methyl-3-nitro-phenyl)-methanone; N-(2-Cyano-phenyl)-2-(9-ethyl-9H-1,3,4,9-tetraaza-fluoren-2-ylsulfanyl)-acetamide; N-(2-Cyano-phenyl)-2-(9-methyl-9H-1,3,4,9-tetraaza-fluoren-2-ylsulfanyl)-acetamide; 1-(Thiophene-2-carbonyl)-2,3-dihydro-1H-quinolin-4-one; (3-Chloro-6-nitro-benzo[b]thiophen-2-yl)-piperidin-1-yl-methanone; (4-Bromo-phenyl)-(3,5-dimethyl-piperidin-1-yl)-methanone; 2-Morpholin-4-yl-N-(1-phenyl-cyclopentylmethyl)-acetamide; 9-Oxo-9H-fluorene-1-carboxylic acid (3-methyl-butyl)-amide; [4-(2,5-Dimethyl-pyrrol-1-yl)-phenyl]-(4-methyl-piperidin-1-yl)-methanone; N-Cycloheptyl-3-diethylsulfamoyl-benzamide; (4-Methoxy-phenyl)-(3-phenyl-piperidin-1-yl)-methanone; 3-Amino-N-cyclohexyl-N-methyl-benzamide; N-Ethyl-3,4-dimethyl-N-phenyl-benzamide; N-Benzyl-3,4,N-trimethyl-benzamide; (4-Fluoro-phenyl)-(3-phenyl-piperidin-1-yl)-methanone; [4-(2,3-Dimethyl-phenyl)-piperazin-1-yl]-(3-methoxy-phenyl)-methanone; Furan-2-carboxylic acid [4-(4-methyl-piperidine-1-sulfonyl)-phenyl]-amide; N-(2-Cyclohex-1-enyl-ethyl)-2-o-tolyloxy-acetamide; 5-(2-Chloro-phenoxymethyl)-furan-2-carboxylic acid (1-bicyclo[2.2.1]hept-2-yl-ethyl)-amide; 3-(2-Chloro-phenyl)-1-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]-propenone; N-[3-(Azepane-1-carbonyl)-phenyl]-benzamide; [3-(Piperidine-1-carbonyl)-pyrazol-1-yl]-o-tolyl-methanone; N-(1-Phenyl-cyclopentylmethyl)-2-piperidin-1-yl-propionamide; 2-Morpholin-4-yl-N-(1-phenyl-cyclopentylmethyl)-propionamide; N-[4-(Azepane-1-sulfonyl)-phenyl]-2,2,2-trifluoro-acetamide; 2,3-Dihydro-benzo[1,4]dioxine-6-carboxylic acid (1-adamantan-1-yl-ethyl)-amide; N-Adamantan-1-yl-2-(3-methoxy-phenoxy)-acetamide; 3-Chloro-benzo[b]thiophene-2-carboxylic acid (2-cyano-ethyl)-phenyl-amide; [4-(4-Nitro-benzyl)-piperidin-1-yl]-phenyl-methanone; [4-(2-Nitro-benzyl)-piperidin-1-yl]-phenyl-methanone; 3-[5-(4-Fluoro-phenyl)-furan-2-yl]-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-propenone; 2-(3-Fluoro-benzoylamino)-4-methyl-5-(piperidine-1-carbonyl)-thiophene-3-carboxylic acid methyl ester; N-(2-Ethyl-phenyl)-2-(3-methyl-piperidin-1-yl)-acetamide; 2-(2-Methoxy-benzoylamino)-4-methyl-5-(piperidine-1-carbonyl)-thiophene-3-carboxylic acid methyl ester; 1-Phenyl-cyclopentanecarboxylic acid (4-phenyl-tetrahydro-pyran-4-ylmethyl)-amide; 4-(2,4-Dichloro-phenoxy)-1-(4-phenyl-piperazin-1-yl)-butan-1-one; Naphthalene-1-carboxylic acid cycloheptylamide; N-Indan-5-yl-2-methyl-3-nitro-benzamide; N-Cyclohexyl-3-(2,2,2-trifluoro-ethoxymethyl)-benzamide; 2-Methoxy-N-(1-phenyl-cyclopentylmethyl)-benzamide; [5-(2,5-Dichloro-phenoxymethyl)-furan-2-yl]-(2,6-dimethyl-morpholin-4-yl)-methanone; [5-(2-Bromo-phenoxymethyl)-furan-2-yl]-(2-methyl-piperidin-1-yl)-methanone; 5-(2-Methoxy-phenoxymethyl)-furan-2-carboxylic acid cycloheptylamide; (3,4-Dihydro-1H-isoquinolin-2-yl)-[1-(2-nitro-benzenesulfonyl)-piperidin-3-yl]-methanone; N-Cyclooctyl-2-(4-methoxy-phenoxy)-acetamide; N-(2,3-Dimethyl-phenyl)-4-[methyl-(toluene-4-sulfonyl)-amino]-butyramide; N-Phenyl-N-[4-(piperidine-1-carbonyl)-benzyl]-benzenesulfonamide; N-[4-(3,4-Dihydro-1H-isoquinoline-2-carbonyl)-benzyl]-N-(3,4-dimethyl-phenyl)-methanesulfonamide; 2,3-Dihydro-benzo[1,4]dioxine-2-carboxylic acid bicyclo[2.2.1]hept-2-ylamide; 4,5,6,7-Tetrahydro-benzo[b]thiophene-3-carboxylic acid cycloheptylamide; N-(2-Azepan-1-yl-2-oxo-ethyl)-N-benzyl-4-fluoro-benzenesulfonamide; 1-(2,6-Dimethyl-morpholin-4-yl)-3,3-diphenyl-propan-1-one; N-Bicyclo[2.2.1]hept-2-yl-4-morpholin-4-ylmethyl-benzamide; [3-(2-Chloro-6-nitro-phenoxy)-phenyl]-piperidin-1-yl-methanone; N-Adamantan-1-yl-2-(4-methyl-quinolin-2-ylsulfanyl)-acetamide; Cyclohexanecarboxylic acid (2-phenylsulfanyl-phenyl)-amide; (4-Hydroxy-4-phenyl-octahydro-quinolin-1-yl)-phenyl-methanone; 3-Cyclohexyl-N-(3-phenyl-propyl)-propionamide; 2-[1-(2,5-Dimethyl-phenyl)-1H-tetrazol-5-ylsulfanyl]-N-isopropyl-N-phenyl-acetamide; N-{2-[4-(3,4-Dihydro-1H-isoquinoline-2-sulfonyl)-phenyl]-ethyl}-acetamide; N-Benzyl-N-[2-oxo-2-(4-phenyl-piperazin-1-yl)-ethyl]-benzenesulfonamide; [4-(2-Chloro-6-nitro-phenoxy)-phenyl]-piperidin-1-yl-methanone; N-Cycloheptyl-3-phenyl-propionamide; (3-Chloro-6-methyl-benzo[b]thiophen-2-yl)-piperidin-1-yl-methanone; N-Cycloheptyl-2,4-dimethoxy-benzamide; N-(3-Chloro-phenyl)-2-(8,11,11-trimethyl-3,4,6-triaza-tricyclo[6.2.1.0 2,7 ]undeca-2(7),3,5-trien-5-ylsulfanyl)-acetamide; N-(2-Nitro-phenyl)-2-(8,11,11-trimethyl-3,4,6-triaza-tricyclo[6.2.1.0 2,7 ]undeca-2(7),3,5-trien-5-ylsulfanyl)-acetamide; N-Phenyl-2-(8,11,11-trimethyl-3,4,6-triaza-tricyclo[6.2.1.0 2,7 ]undeca-2(7),3,5-trien-5-ylsulfanyl)acetamide; N-Ethyl-3-methyl-N-o-tolyl-benzamide; N-[5-(2,4-Dichloro-benzylsulfanyl)-[1,3,4]thiadiazol-2-yl]-2,2-dimethyl-propionamide; 4-Bromo-1-ethyl-1H-pyrazole-3-carboxylic acid (2-methylsulfanyl-phenyl)-amide; 5-Benzoyl-furan-2-carboxylic acid diisopropylamide; N-{2-[2-(4-Bromo-phenyl)-2-oxo-ethylsulfanyl]-benzothiazol-6-yl}-acetamide; 2-(6-Amino-benzothiazol-2-ylsulfanyl)-N-cyclohexyl-acetamide; N-(2-Cyclohexylcarbamoylmethylsulfanyl-benzothiazol-6-yl)-2-methoxy-benzamide; Benzofuran-2-yl-(4-phenyl-piperidin-1-yl)-methanone; 1-(2-Nitro-phenyl)-piperidine-3-carboxylic acid diethylamide; 1-(4-Nitro-phenyl)-piperidine-3-carboxylic acid diethylamide; 5-Bromo-furan-2-carboxylic acid adamantan-2-ylamide; 3,3-Dimethyl-pentanedioic acid bis-[(2,4-difluoro-phenyl)-amide]; 2-(3-Bromo-benzylsulfanyl)-1-(4-phenyl-piperazin-1-yl)-ethanone; N-(2-Azepan-1-yl-2-oxo-ethyl)-N-benzyl-4-bromo-benzenesulfonamide; 1-(2,3-Dihydro-indol-1-yl)-2-p-tolylsulfanyl-ethanone; [4-(4-Bromo-benzenesulfonyl)-piperazin-1-yl]-furan-2-yl-methanone; [5-(2-Bromo-phenoxymethyl)-furan-2-yl]-(2,6-dimethyl-morpholin-4-yl)-methanone; 5-(2-Chloro-phenoxymethyl)-furan-2-carboxylic acid diethylamide; 5-(2-Bromo-phenoxymethyl)-furan-2-carboxylic acid diethylamide; 5-(2-Chloro-phenoxymethyl)-furan-2-carboxylic acid methyl-phenyl-amide; [5-(2-Chloro-phenoxymethyl)-furan-2-yl]-(4-methyl-piperidin-1-yl)-methanone; [3-(2,5-Dichloro-phenoxymethyl)-phenyl]-pyrrolidin-1-yl-methanone; [5-(4-Ethoxy-phenoxymethyl)-furan-2-yl]-(4-methyl-piperidin-1-yl)-methanone; 3-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-N-(2-methyl-cyclohexyl)-propionamide; 3-(3,4-Dihydro-2H-quinoline-1-carbonyl)-N-phenyl-benzenesulfonamide; [3-(2,3-Dihydro-indole-1-sulfonyl)-phenyl]-(3,4-dihydro-2H-quinolin-1-yl)-methanone; [3-(2,5-Dimethyl-pyrrol-1-yl)-phenyl]-(4-methyl-piperidin-1-yl)-methanone; N-Cyclohexyl-3-(2-hydroxy-4-methyl-phenyl)-3-phenyl-propionamide; 2-Diethylamino-N-(1-phenyl-cyclopentylmethyl)-propionamide; (6-Fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-(3-trifluoromethyl-phenyl)-methanone; (2,6-Dimethyl-morpholin-4-yl)-[4-(naphthalen-1-yloxymethyl)-phenyl]-methanone; N-Benzyl-4-bromo-N-ethyl-benzamide; (3-Methyl-piperidin-1-yl)-[4-(naphthalen-1-yloxymethyl)-phenyl]-methanone; Azepan-1-yl-[5-(2-chloro-phenoxymethyl)-furan-2-yl]-methanone; (4-Methyl-piperidin-1-yl)-[4-(naphthalen-1-yloxymethyl)-phenyl]-methanone; Azepan-1-yl-[5-(2,4-dichloro-phenoxymethyl)-furan-2-yl]-methanone; N-Cycloheptyl-4-(4-methoxy-2-methyl-phenyl)-butyramide; 2-(4-Benzothiazol-2-yl-piperazin-1-yl)-N-cyclohexyl-acetamide; N-Cycloheptyl-2-(2,6-dimethyl-phenoxy)-acetamide; (3,4-Dihydro-2H-quinolin-1-yl)-(3-iodo-phenyl)-methanone; N-Cycloheptyl-3-(2,2,2-trifluoro-ethoxymethyl)-benzamide; Azepan-1-yl-[4-(2-chloro-phenoxymethyl)-phenyl]-methanone; (2,6-Dimethyl-morpholin-4-yl)-[4-(naphthalen-2-yloxymethyl)-phenyl]-methanone; Azepan-1-yl-[3-(4-ethoxy-phenoxymethyl)-phenyl]-methanone; Benzo[b]thiophene-3-carboxylic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide; 2-(4-Chloro-2-methyl-phenoxy)-N-cycloheptyl-acetamide; 2,4-Dichloro-N-cyclohexyl-N-methyl-benzamide; N-Cyclooctyl-2-p-tolyloxy-acetamide; (3,5-Dimethyl-piperidin-1-yl)-(4-methyl-3-nitro-phenyl)-methanone; Biphenyl-4-yl-(2,6-dimethyl-piperidin-1-yl)-methanone; N-Cyclohexyl-4-fluoro-N-methyl-benzamide; N-[4-(Azepane-1-carbonyl)-phenyl]-N-methyl-benzenesulfonamide; N-Cycloheptyl-2-fluoro-benzamide; N-Cycloheptyl-4-methyl-benzamide; (3-Methyl-piperidin-1-yl)-p-tolyl-methanone; [2-(3,4-Dimethoxy-phenylcarbamoyl)-piperidin-1-yl]-acetic acid benzyl ester; N-[4-(2-Methyl-piperidine-1-sulfonyl)-phenyl]-acetamide; 2-(2,4-Dichloro-phenoxy)-N-(2-methyl-butyl)-propionamide; [4-(2-Chloro-6-nitro-phenyl)-piperazin-1-yl]-(4-methoxy-phenyl)-methanone; N-Cyclohexyl-4-(4-methoxy-3-methyl-phenyl)-butyramide; (3-Chloro-6-methoxy-benzo[b]thiophen-2-yl)-(3,4-dihydro-1H-isoquinolin-2-yl)-methanone; 2-(4-Methyl-benzylsulfanyl)-1-piperidin-1-yl-ethanone; N-Cyclohexyl-N-[(4-phenyl-thiazol-2-ylcarbamoyl)-methyl]-benzamide; N-(2-Azepan-1-yl-2-oxo-ethyl)-N-(4-isopropyl-phenyl)-methanesulfonamide; N-Adamantan-1-yl-3-p-tolylsulfanyl-propionamide; 6-(2,4-Dichloro-phenylcarbamoyl)-3,4-dimethyl-cyclohex-3-enecarboxylic acid; (4-Butyl-cyclohexyl)-morpholin-4-yl-methanone; (3,4-Dichloro-phenyl)-(3,4-dihydro-2H-quinolin-1-yl)-methanone; N-(2-Cyclohex-1-enyl-ethyl)-3-methoxy-benzamide; N-Adamantan-2-yl-3-(1,5-dimethyl-1H-pyrazol-4-yl)-acrylamide; N-Adamantan-1-yl-N-methyl-4-(4-nitro-pyrazol-1-ylmethyl)-benzamide; 5-(4-Chloro-3,5-dimethyl-pyrazol-1-ylmethyl)-furan-2-carboxylic acid adamantan-2-ylamide; 2-(4-Chloro-phenoxy)-N-(2-fluoro-5-methyl-phenyl)-2-methyl-propionamide; N-Adamantan-1-yl-2-(4-chloro-3,5-dimethyl-phenoxy)-acetamide; 2-[(3-Carboxy-bicyclo[2.2.1]heptane-2-carbonyl)-amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxylic acid propyl ester; 2-Adamantan-1-yl-N-[1-(2,5-dimethyl-phenyl)-ethyl]-acetamide; 3-Methyl-thiophene-2-carboxylic acid cyclooctylamide; N-p-Tolyl-2-(8,11,11-trimethyl-3,4,6-triaza-tricyclo[6.2.1.0 2,7 ]undeca-2,4,6-trien-5-ylsulfanyl)propionamide; Azepan-1-yl-[5-(4-chloro-5-methyl-3-nitro-pyrazol-1-ylmethyl)-furan-2-yl]-methanone; N-Adamantan-2-yl-3-(4-bromo-3-nitro-pyrazol-1-ylmethyl)-benzamide; N-Bicyclo[2.2.1]hept-2-yl-2-chloro-benzamide; [5-(3-Chloro-phenoxymethyl)-furan-2-yl]-piperidin-1-yl-methanone; 1-(4-Ethyl-benzoyl)-6-methoxy-2-methyl-2,3-dihydro-1H-quinolin-4-one; 6-Fluoro-2-methyl-1-{3-[4-(propane-1-sulfonyl)-phenoxymethyl]-benzoyl}-2,3-dihydro-1H-quinolin-4-one; N-Cycloheptyl-2-(naphthalen-1-yloxy)-acetamide; N-Cyclohexyl-4-o-tolyloxy-butyramide; (2-Benzylsulfanyl-phenyl)-morpholin-4-yl-methanone; (2-Chloro-5,6-difluoro-3-methyl-phenyl)-(4-methyl-piperidin-1-yl)-methanone; (3-Bromo-phenyl)-[4-(4-chloro-2-nitro-phenyl)-piperazin-1-yl]-methanone; 2-Bromo-N-(1,1,3,3-tetramethyl-butyl)-benzamide; N-Adamantan-1-yl-2-(2-benzoyl-5-methoxy-phenoxy)-acetamide; N-Cyclohexyl-3-methyl-4-p-tolyl-butyramide; [5-(4-Methyl-2-nitro-phenoxymethyl)-furan-2-yl]-thiomorpholin-4-yl-methanone; [5-(2,5-Dichloro-phenoxymethyl)-furan-2-yl]-thiomorpholin-4-yl-methanone; 5-(4-Chloro-2-nitro-phenoxymethyl)-furan-2-carboxylic acid adamantan-1-ylamide; 4,5,6,7-Tetrahydro-benzo[b]thiophene-3-carboxylic acid cyclohexylamide; 4-Chloro-1,5-dimethyl-1H-pyrazole-3-carboxylic acid adamantan-1-yl-methyl-amide; 4-(4-Methoxy-3-methyl-phenyl)-N-(2-methyl-cyclohexyl)-butyramide; 3-Benzo[1,3]dioxol-5-yl-1-(3,4-dihydro-1H-isoquinolin-2-yl)-propenone; N-Bicyclo[2.2.1]hept-2-yl-3-phenylsulfanyl-propionamide; Azepan-1-yl-[5-(2-nitro-phenoxymethyl)-furan-2-yl]-methanone; N-Benzyl-2-(4-chloro-phenylsulfanyl)-N-methyl-acetamide; 1-(4-Benzyl-piperidin-1-yl)-2-benzylsulfanyl-ethanone; 2-(4-tert-Butyl-phenoxy)-1-(4-ethyl-piperazin-1-yl)-ethanone; [4-(4-Ethoxy-phenoxymethyl)-phenyl]-(4-methyl-piperidin-1-yl)-methanone; 5-(4-Bromo-3,5-dimethyl-pyrazol-1-ylmethyl)-furan-2-carboxylic acid adamantan-2-ylamide; 1-Azepan-1-yl-3-(4-chloro-phenylsulfanyl)-propan-1-one; N-Bicyclo[2.2.1]hept-2-yl-2-(2-chloro-benzylsulfanyl)-acetamide; 2-(2-Methyl-benzylsulfanyl)-1-(4-phenyl-piperazin-1-yl)-ethanone; N-[2-(1-Benzo[1,3]dioxol-5-yl-3-furan-2-yl-3-oxo-propylsulfanyl)-phenyl]-acetamide; (3,5-Dimethyl-piperidin-1-yl)-(3-iodo-phenyl)-methanone; [5-(2-Bromo-phenoxymethyl)-furan-2-yl]-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; N-Benzyl-N-cyclohex-1-enyl-isonicotinamide; 1-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-2-(2-methyl-benzylsulfanyl)-ethanone; 2-(2-Bromo-4-methyl-phenoxy)-N-(2-cyclohex-1-enyl-ethyl)-acetamide; 2-[5-(2-Hydroxy-phenyl)-[1,3,4]oxadiazol-2-ylsulfanyl]-1-piperidin-1-yl-ethanone; 5-(4-Nitro-pyrazol-1-ylmethyl)-furan-2-carboxylic acid adamantan-2-ylamide; 3-Benzo[1,3]dioxol-5-yl-3-(2-methoxy-phenyl)-1-pyrrolidin-1-yl-propan-1-one; N-Adamantan-2-yl-3,4-dichloro-benzamide; Benzo[b]thiophen-3-yl-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; 2-Adamantan-1-yl-1-(3,4-dihydro-1H-isoquinolin-2-yl)-ethanone; 4,5,6,7-Tetrahydro-benzo[b]thiophene-3-carboxylic acid (2-cyclohex-1-enyl-ethyl)-amide; Benzo[b]thiophene-3-carboxylic acid (3,3,5-trimethyl-cyclohexyl)-amide; 2-(2,6-Dimethyl-phenoxy)-N-(2-isopropyl-phenyl)-acetamide; 4-Bromo-N-[3-(piperidine-1-carbonyl)-phenyl]-benzamide; N-Benzo[1,3]dioxol-5-ylmethyl-2-(2-cyano-phenylsulfanyl)-benzamide; N-Adamantan-1-yl-2-(naphthalen-2-yloxy)-acetamide; [4-(4-Chloro-phenylsulfanylmethyl)-phenyl]-morpholin-4-yl-methanone; Thiophene-2-carboxylic acid (3,3,5-trimethyl-cyclohexyl)-amide; Benzo[1,3]dioxol-5-yl-(3,4-dihydro-2H-quinolin-1-yl)-methanone; 3-Chloro-benzo[b]thiophene-2-carboxylic acid cyclooctylamide; 2-[2-Morpholin-4-yl-1-(4-nitro-benzyl)-2-oxo-ethyl]-isoindole-1,3-dione; 2-Hydroxy-4,4-dimethyl-6-oxo-cyclohex-1-enecarboxylic acid phenylamide; (2,4-Dichloro-phenyl)-(2,6-dimethyl-piperidin-1-yl)-methanone; Adamantane-1-carboxylic acid furan-2-ylmethyl-p-tolyl-amide; Azocan-1-yl-(4-tert-butyl-phenyl)-methanone; 3-Chloro-benzo[b]thiophene-2-carboxylic acid benzyl-methyl-amide; Adamantane-1-carboxylic acid (2-fluoro-phenyl)-amide; 2-(Piperidine-1-carbonyl)-5-piperidin-1-yl-oxazole-4-carbonitrile; N-(4,6-Dimethyl-5-nitro-pyridin-3-yl)-benzamide; Adamantan-1-yl-[4-(2-methoxy-phenyl)-piperazin-1-yl]-methanone; (2-Methyl-piperidin-1-yl)-o-tolyl-methanone; N-Benzyl-4-chloro-N-isopropyl-3-nitro-benzamide; N-(3-Hexylsulfanyl-[1,2,4]thiadiazol-5-yl)-3-methyl-butyramide; 4, N-Dimethyl-N-[4-(piperidine-1-carbonyl)-phenyl]-benzenesulfonamide; Azepan-1-yl-(5-tert-butyl-2H-pyrazol-3-yl)-methanone; 2-Amino-4-methyl-5-(piperidine-1-carbonyl)-thiophene-3-carboxylic acid ethyl ester; 5-Methyl-furan-2-carboxylic acid (1-adamantan-1-yl-ethyl)-amide; (3-Chloro-6-methyl-benzo[b]thiophen-2-yl)-(3,4-dihydro-1H-isoquinolin-2-yl)-methanone; N-Adamantan-1-yl-2-trifluoromethyl-benzamide; (3-Bromo-phenyl)-(2,2,4-trimethyl-4-phenyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; Benzo[1,3]dioxole-5-carboxylic acid dipropylamide; N-(3,3-Diphenyl-propyl)-4-methoxy-benzamide; [4-(2-Chloro-6-nitro-phenyl)-piperazin-1-yl]-p-tolyl-methanone; Furan-2-yl-[4-(toluene-4-sulfonyl)-piperazin-1-yl]-methanone; 3-(2-Chloro-6-fluoro-phenyl)-1-(3,4-dihydro-2H-quinolin-1-yl)-propenone; 2-Chloro-N-cycloheptyl-benzamide; 1-[4-(4-Nitro-phenyl)-piperazin-1-yl]-3-phenyl-propan-1-one; (3,4-Dihydro-1H-isoquinolin-2-yl)-(3,4-dimethyl-phenyl)-methanone; (1-Adamantan-1-yl-4-bromo-1H-pyrazol-3-yl)-morpholin-4-yl-methanone; 2-Phenyl-cyclopropanecarboxylic acid cyclooctylamide; 3-[4-(2-Ethoxy-phenyl)-piperazine-1-carbonyl]-isochromen-1-one; [3-(4-Bromo-pyrazol-1-ylmethyl)-phenyl]-(4-methyl-piperidin-1-yl)-methanone; 2-Azepan-1-yl-N-biphenyl-2-yl-acetamide; N-[5-(3,4-Dimethoxy-benzyl)-[1,3,4]thiadiazol-2-yl]-3-methyl-butyramide; Adamantan-1-yl-(4-phenyl-piperidin-1-yl)-methanone; N-(2-Azepan-1-yl-2-oxo-ethyl)-N-(4-ethoxy-phenyl)-4-methylsulfanyl-benzenesulfonamide; 1-Adamantan-1-yl-4-bromo-1H-pyrazole-3-carboxylic acid diethylamide; (6-Fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-(2-fluoro-phenyl)-methanone; 3-[4-(2,3-Dimethyl-phenyl)-piperazine-1-carbonyl]-isochromen-1-one; N-Cyclooctyl-2-(2-methoxy-phenoxy)-acetamide; N-Cyclohexyl-N-methyl-2-nitro-benzamide; Adamantane-1-carboxylic acid (1,1-dioxo-tetrahydro-thiophen-3-yl)-amide; N-Adamantan-2-yl-2-(4-chloro-phenyl)-acetamide; (2,4-Dichloro-phenyl)-(3-methyl-piperidin-1-yl)-methanone; 2-(4-tert-Butyl-phenoxy)-N-cyclooctyl-acetamide; (10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-(2-methoxy-phenyl)-methanone; (3-Chloro-phenyl)-(2-methyl-piperidin-1-yl)-methanone; (3-Chloro-6-nitro-benzo[b]thiophen-2-yl)-(3-methyl-piperidin-1-yl)-methanone; (2,5-Dichloro-phenyl)-(4-methyl-piperidin-1-yl)-methanone; N-[5-(3,4-Dichloro-benzyl)-[1,3,4]thiadiazol-2-yl]-2,2-dimethyl-propionamide; 4-(4-Chloro-2-methyl-phenoxy)-1-(3,4-dihydro-2H-quinolin-1-yl)-butan-1-one; (3,4-Dichloro-phenyl)-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]-methanone; Cyclooctanecarboxylic acid [1-(naphthalene-2-sulfonyl)-pyrrolidin-2-yl]-amide; 1-Butyl-pyrrolidine-2-carboxylic acid benzo[1,3]dioxol-4-ylamide; 5-Methyl-furan-2-carboxylic acid dibenzylamide; (3,4-Dihydro-2H-quinolin-1-yl)-[3-(4-phenyl-piperazine-1-sulfonyl)-phenyl]-methanone; Bicyclo[2.2.1]hept-2-yl-[4-(2,3-dimethyl-phenyl)-piperazin-1-yl]-methanone; N-Adamantan-1-yl-2-benzoyl-benzamide; [5-(2-Chloro-phenoxymethyl)-furan-2-yl]-(3-methyl-piperidin-1-yl)-methanone; (3,5-Dimethyl-piperidin-1-yl)-(2-iodo-phenyl)-methanone; 1-Benzenesulfonyl-pyrrolidine-2-carboxylic acid cyclooctylamide; (3,4-Dimethoxy-phenyl)-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-methanone; 3-(2,6-Dichloro-phenyl)-1-(2-ethyl-piperidin-1-yl)-propenone; N-(3,4-Difluoro-phenyl)-2,6-difluoro-benzamide; 2,6-Difluoro-N-naphthalen-1-yl-benzamide; (4-Chloro-phenyl)-(3,5-dimethyl-piperidin-1-yl)-methanone; N-[4-(2,6-Dimethyl-piperidine-1-carbonyl)-phenyl]-2-(naphthalen-2-yloxy)-acetamide; (2-Chloro-phenyl)-(3-methyl-piperidin-1-yl)-methanone; N-{2-[4-(Piperidine-1-sulfonyl)-phenyl]-ethyl}-acetamide; N-Biphenyl-2-yl-2-(pyridin-2-ylsulfanyl)-acetamide; Azepan-1-yl-[5-(4-chloro-3,5-dimethyl-pyrazol-1-ylmethyl)-furan-2-yl]-methanone; Acetic acid 4-(4-methyl-piperidine-1-carbonyl)-phenyl ester; Acetic acid 4-(4-benzyl-piperidine-1-carbonyl)-phenyl ester; Benzo[1,3]dioxole-5-carboxylic acid cycloheptylamide; 2-(2,4-Dimethyl-phenoxy)-1-(6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-ethanone; Acetic acid 4-(3,4-dihydro-2H-quinoline-1-carbonyl)-phenyl ester; Azepan-1-yl-(3,5-dibromo-phenyl)-methanone; (3,5-Dibromo-phenyl)-[4-(2-methoxy-phenyl)-piperazin-1-yl]-methanone; N-Cyclooctyl-4-isopropyl-benzamide; N-Cyclooctyl-2-(4-methoxy-phenyl)-acetamide; (4-tert-Butyl-piperidin-1-yl)-phenyl-methanone; N-(4-tert-Butyl-3-nitro-phenyl)-acetamide; (2,6-Dimethyl-piperidin-1-yl)-[5-(2,3,5,6-tetrafluoro-phenoxymethyl)-furan-2-yl]-methanone; N-Cyclohexyl-3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-N-methyl-propionamide; 2-(4-Chloro-3-methyl-phenoxy)-N-cyclohexyl-N-methyl-acetamide; N-Cyclopentyl-3-(3,4-dihydro-2H-quinoline-1-carbonyl)-benzenesulfonamide; (3,4-Dihydro-1H-isoquinolin-2-yl)-(3-dimethylamino-phenyl)-methanone; 3-Cyclohexylcarbamoyl-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid isopropyl ester; 1-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-(2-methoxy-phenyl)-ethanone; N-Benzyl-N-cyclohex-1-enyl-benzamide; [1-(Thiophene-2-sulfonyl)-piperidin-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-Adamantan-1-yl-2-(1-phenyl-1H-tetrazol-5-ylsulfanyl)-acetamide; (3,4-Dihydro-2H-quinolin-1-yl)-[4-(morpholine-4-sulfonyl)-phenyl]-methanone; (3,4-Dihydro-2H-quinolin-1-yl)-[4-(pyrrolidine-1-sulfonyl)-phenyl]-methanone; (3,4-Dihydro-2H-quinolin-1-yl)-[1-(thiophene-2-sulfonyl)-piperidin-4-yl]-methanone; (1-Benzenesulfonyl-piperidin-3-yl)-(3,4-dihydro-1H-isoquinolin-2-yl)-methanone; 6,7-Dimethyl-4-oxa-tricyclo[4.3.0.0 3,7 ]nonane-3-carboxylic acid cyclohexylamide; 6,7-Dimethyl-4-oxa-tricyclo[4.3.0.0 3,7 ]nonane-3-carboxylic acid (2-chloro-phenyl)-amide; (6,7-Dimethyl-4-oxa-tricyclo[4.3.0.0 3,7 ]non-3-yl)-piperidin-1-yl-methanone; 2-(5,6-Dimethyl-4-oxo-3,4-dihydro-thieno[2,3-d]pyrimidin-2-ylsulfanyl)-N-furan-2-ylmethyl-acetamide; N-Allyl-2-(5,6-dimethyl-4-oxo-3,4-dihydro-thieno[2,3-d]pyrimidin-2-ylsulfanyl)-acetamide; N-Adamantan-1-yl-2-(5,6,7,8-tetrahydro-benzo[4,5]thieno[2,3-d]pyrimidin-4-ylsulfanyl)-acetamide; 1-(3,4-Dihydro-2H-quinoline-1-carbonyl)-4,7,7-trimethyl-2-oxa-bicyclo[2.2.1]heptan-3-one; 1-(3,4-Dihydro-1H-isoquinoline-2-carbonyl)-4,7,7-trimethyl-2-oxa-bicyclo[2.2.1]heptan-3-one; Azepan-1-yl-(6,7-dimethyl-4-oxa-tricyclo[4.3.0.0 3,7 ]non-3-yl)-methanone; 2,5-Dimethyl-furan-3-carboxylic acid (1-adamantan-1-yl-ethyl)-amide; 1-Cyclohexyl-5-oxo-pyrrolidine-3-carboxylic acid (3-cyano-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)-amide; 2-(2-Cyano-phenylsulfanyl)-N-cyclopentyl-benzamide; [5-(2-Methoxy-4-propyl-phenoxymethyl)-furan-2-yl]-(3-methyl-piperidin-1-yl)-methanone; (4-tert-Butyl-phenyl)-(3,5-dimethyl-piperidin-1-yl)-methanone; [4-(2-Methoxy-naphthalen-1-ylmethyl)-piperazin-1-yl]-(4-methoxy-phenyl)-methanone; (3,4-Dichloro-phenyl)-(3,5-dimethyl-piperidin-1-yl)-methanone; (4-Ethoxy-phenyl)-(4-methyl-piperidin-1-yl)-methanone; 2-Phenethyl-N-(tetrahydro-furan-2-ylmethyl)-benzamide; N-Cycloheptyl-2-phenoxy-benzamide; Adamantane-1-carboxylic acid (2-ethoxy-phenyl)-amide; N-Adamantan-2-yl-2-o-tolyloxy-acetamide; (2-Chloro-phenyl)-(3,5-dimethyl-piperidin-1-yl)-methanone; 1-Morpholin-4-yl-2-[3-(4-nitro-phenyl)-adamantan-1-yl]-ethanone; 2-Dimethylamino-N-(2-nitro-phenyl)-benzamide; N-Benzyl-2-(4,4,6-trimethyl-1-p-tolyl-1,4-dihydro-pyrimidin-2-ylsulfanyl)-acetamide; [4-(3,5-Dinitro-phenoxy)-phenyl]-(2-ethyl-piperidin-1-yl)-methanone; 1-(4-Chloro-benzoyl)-2,3-dihydro-1H-benzo[g]quinolin-4-one; 2-[(Adamantane-1-carbonyl)-amino]-3-phenyl-propionic acid methyl ester; [Benzyl-(4-nitro-benzoyl)-amino]-acetic acid ethyl ester; 9-Oxo-9H-fluorene-3-carboxylic acid methyl-(4-nitro-phenyl)-amide; Adamantane-1-carboxylic acid [2-(4-methoxy-phenyl)-ethyl]-amide; (10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-(4-fluoro-phenyl)-methanone; 2-Benzylsulfanyl-N-[2-(2-methoxy-phenoxy)-ethyl]-acetamide; N-Adamantan-1-yl-2-(2-oxo-4-phenyl-pyrrolidin-1-yl)-acetamide; 2-Bromo-N-tricyclo[3.2.1.0 2,4 ]oct-6-ylmethyl-benzamide; Adamantane-1-carboxylic acid (2,6-dimethoxy-pyrimidin-4-yl)-amide; Hexanedioic acid (2,7,7-trimethyl-bicyclo[2.2.1]hept-1-yl)-amide(1,7,7-trimethyl-bicyclo[2.2.1]hept-2-yl)-amide; 2-Chloro-N-(2-cyclohexyl-ethyl)-benzamide; 2-[3-(2-Ethyl-piperidin-1-yl)-3-oxo-propyl]-isoindole-1,3-dione; N-Adamantan-1-yl-2-hydroxy-2,2-diphenyl-acetamide; Adamantane-1-carboxylic acid (naphthalen-1-ylmethyl)-amide; Adamantane-1-carboxylic acid (benzo[1,3]dioxol-5-ylmethyl)-amide; 1-(Azepane-1-carbonyl)-fluoren-9-one; 2-(Quinolin-2-ylsulfanyl)-N-p-tolyl-acetamide; 2,4-Dichloro-N-[3-(piperidine-1-carbonyl)-phenyl]-benzamide; 2-Chloro-4,5-difluoro-N-(3,3,5-trimethyl-cyclohexyl)-benzamide; 2-(2-Chloro-benzylsulfanyl)-N-p-tolyl-acetamide; [4-(4-Chloro-phenylsulfanylmethyl)-phenyl]-pyrrolidin-1-yl-methanone; N-Adamantan-1-yl-N-methyl-isonicotinamide; Azepan-1-yl-[4-(4-chloro-phenylsulfanylmethyl)-phenyl]-methanone; (2-Chloro-phenyl)-(1,5,7-trimethyl-3,7-diaza-bicyclo[3.3.1]non-3-yl)-methanone; (3-Chloro-benzo[b]thiophen-2-yl)-(4-methyl-piperidin-1-yl)-methanone; Benzoic acid 1-benzoyl-decahydro-quinolin-4-yl ester; 2-(3-Bromo-benzylsulfanyl)-1-[4-(2-methoxy-phenyl)-piperazin-1-yl]-ethanone; 4-Methyl-N-[2-(phenoxazine-10-carbonyl)-phenyl]-benzenesulfonamide; 2-[1-(Azepane-1-carbonyl)-2-methyl-propyl]-isoindole-1,3-dione; 2-(3-Bromo-benzylsulfanyl)-1-piperidin-1-yl-ethanone; 1-[3-(4-Bromo-phenyl)-1-furan-2-yl-3-oxo-propyl]-pyrrolidin-2-one; 2-Chloro-N-cyclooctyl-4,5-difluoro-benzamide; 2,4-Dichloro-N-(2-furan-2-ylmethyl-cyclohexyl)-benzamide; N-(4-Benzoyl-furazan-3-yl)-2-fluoro-benzamide; N-Adamantan-1-yl-2-(3-cyano-4-methoxymethyl-6-methyl-pyridin-2-ylsulfany)-acetamide; 4-tert-Butyl-N-cyclooctyl-benzamide; N-Adamantan-1-yl-2-phenyl-butyramide; (3-Chloro-6-methoxy-benzo[b]thiophen-2-yl)-piperidin-1-yl-methanone; (3,7-Dichloro-6-methoxy-benzo[b]thiophen-2-yl)-piperidin-1-yl-methanone; Acetic acid 1-benzoyl-decahydro-quinolin-4-yl ester; 2-Bromo-N-methyl-N-phenyl-benzamide; N-Benzo[1,3]dioxol-5-yl-2,4-dichloro-benzamide; (3-Chloro-6-fluoro-benzo[b]thiophen-2-yl)-piperidin-1-yl-methanone; N-(1,2,3,5,6,7-Hexahydro-s-indacen-1-yl)-2-piperidin-1-yl-acetamide; 2-[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionylamino]-3-methyl-butyric acid methyl ester; 2-(6-Oxo-6-piperidin-1-yl-hexyl)-isoindole-1,3-dione; 2-[2-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-3-phenyl-propionylamino]-3-methyl-butyric acid methyl ester; Adamantane-1-carboxylic acid (2,6-dihydroxy-pyrimidin-4-yl)-amide; Adamantane-1-carboxylic acid methyl-phenyl-amide; 3-Chloro-benzo[b]thiophene-2-carboxylic acid dibenzylamide; N-Adamantan-1-yl-2-(3-cyano-6-methyl-4-trifluoromethyl-pyridin-2-ylsulfanyl)-acetamide; 2-(3-Oxo-3-phenyl-propenyl)-isoindole-1,3-dione; N-[5-(5-Chloro-benzooxazol-2-yl)-2-methyl-phenyl]-2-methoxy-benzamide; N-[2-(2-Bromo-phenyl)-benzooxazol-5-yl]-2-methoxy-benzamide; 2-(4-Chloro-phenoxy)-N-(4-chloro-3-trifluoromethyl-phenyl)-acetamide; 2,2-Dimethyl-N-(5-propyl-[1,3,4]thiadiazol-2-yl)-propionamide; 2-[2-(2,6-Dimethyl-morpholin-4-yl)-1-methyl-2-oxo-ethyl]-isoindole-1,3-dione; 2-(2-Cyano-phenylsulfanyl)-N-(2-trifluoromethyl-phenyl)-benzamide; Azepan-1-yl-(3,6-dichloro-benzo[b]thiophen-2-yl)-methanone; Benzo[1,3]dioxol-5-yl-(4-benzyl-piperidin-1-yl)-methanone; Azepan-1-yl-(3-chloro-6-methyl-benzo[b]thiophen-2-yl)-methanone; N-(5-Hexyl-[1,3,4]thiadiazol-2-yl)-isobutyramide; (3-Chloro-phenyl)-(10,11-dihydro-dibenzo[b,f]azepin-5-yl)-methanone; (2-Chloro-phenyl)-(10,11-dihydro-dibenzo[b,f]azepin-5-yl)-methanone; 2-Amino-5-(azepane-1-carbonyl)-4-methyl-thiophene-3-carboxylic acid ethyl ester; Adamantan-1-yl-(4-cyclopropyl-1,4,6,7-tetrahydro-imidazo[4,5-c]pyridin-5-yl)-methanone; Adamantan-1-yl-(4-trifluoromethyl-1,4,6,7-tetrahydro-imidazo[4,5-c]pyridin-5-yl)-methanone; Adamantan-1-yl-[4-(1H-benzoimidazol-2-ylsulfanyl)-piperidin-1-yl]-methanone; Adamantan-1-yl-(1,4,6,7-tetrahydro-imidazo[4,5-c]pyridin-5-yl)-methanone; [4-(1H-Imidazol-4-yl)-piperidin-1-yl]-(4-pentyl-phenyl)-methanone; 3-Cyclohexyl-1-[4-(1H-imidazol-4-yl)-piperidin-1-yl]-propan-1-one; 1-(4-Propyl-piperazin-1-yl)-3-(4-trifluoromethyl-phenyl)-propan-1-one; N-(2-Hydroxy-benzyl)-3-thiophen-3-yl-N-(2-thiophen-2-yl-ethyl)-acrylamide; N-(1,3-Dimethyl-pentyl)-2-(3-fluoro-phenyl)-N-(4-hydroxy-benzyl)-acetamide; N-Cyclobutyl-2-(3-fluoro-phenyl)-N-(4-hydroxy-benzyl)-acetamide; N-Cyclobutyl-N-(4-hydroxy-benzyl)-4-trifluoromethyl-benzamide; N-(3-Hydroxy-benzyl)-2-methyl-3-nitro-N-(4-sulfamoyl-benzyl)-benzamide; N-(4-Bromo-benzyl)-N-(4-hydroxy-benzyl)-2-naphthalen-1-yl-acetamide; 6-(2-Bromo-phenylsulfanyl)-hexanoic acid (3-amino-2,2-dimethyl-propyl)-amide; N-(3-Amino-2,2-dimethyl-propyl)-4-[2-(2-isopropyl-phenylsulfanyl)-ethyl]-benzamide; N-(3-Amino-2,2-dimethyl-propyl)-4-[4-(4-chloro-phenyl)-pyrimidin-2-ylsulfanylmethyl]-3-nitro-benzamide; 4-(4-Bromo-phenyl)-N-(2-hydroxy-benzyl)-4-oxo-N-thiophen-2-ylmethyl-butyramide; N-[2-(2,4-Dichloro-phenyl)-ethyl]-N-(4-hydroxy-benzyl)-2-thiophen-3-yl-acetamide; N-(2-Chloro-benzyl)-N-(4-hydroxy-benzyl)-2-thiophen-2-yl-acetamide; Heptanoic acid benzyl-(4-hydroxy-benzyl)-amide; N-(4-Fluoro-benzyl)-N-(4-hydroxy-benzyl)-2-thiophen-3-yl-acetamide; 4-Methyl-pentanoic acid (4-fluoro-benzyl)-(4-hydroxy-benzyl)-amide; N-Allyl-2-(4-chloro-phenyl)-N-(4-hydroxy-benzyl)-acetamide; N-Allyl-2-benzo[b]thiophen-3-yl-N-(4-hydroxy-benzyl)-acetamide; Heptanoic acid (3-ethoxy-propyl)-(4-hydroxy-benzyl)-amide; Dec-3-enoic acid (4-hydroxy-benzyl)-(4-trifluoromethyl-benzyl)-amide; 6-Oxo-6-phenyl-hexanoic acid (4-hydroxy-benzyl)-(4-trifluoromethyl-benzyl)-amide; 2-(3,4-Difluoro-phenyl)-N-(4-hydroxy-benzyl)-N-thiophen-2-ylmethyl-acetamide; 2-Methyl-pent-4-enoic acid (3-hydroxy-benzyl)-[2-(2-methoxy-phenyl)-ethyl]-amide; Heptanoic acid (3-hydroxy-benzyl)-(4-isopropyl-benzyl)-amide; 5-(2,6-Dichloro-phenylsulfanyl)-pentanoic acid (naphthalen-1-ylmethyl)-amide; N-(6,6-Dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-4-[2-(5-methyl-1H-benzoimidazol-2-ylsulfanyl)ethyl]-benzamide; N-(6,6-Dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-4-[2-(4-phenoxy-pyrimidin-2-ylsulfanyl)-ethyl]-benzamide; N-(6,6-Dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-4-[2-(4-fluoro-phenylsulfanyl)-ethyl]-benzamide; 4-(2,6-Dichloro-phenylsulfanyl)-N-(6,6-dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-butyramide; 5-(3-Methylsulfanyl-[1,2,4]thiadiazol-5-ylsulfanyl)-pentanoic acid (6,6-dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-amide; 5-(2,6-Dichloro-phenylsulfanyl)-pentanoic acid [2-(3-trifluoromethyl-phenyl)-ethyl]-amide; 4-[2-(2,6-Dichloro-phenylsulfanyl)-ethyl]-N-[2-(2-fluoro-phenyl)-ethyl]-benzamide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (3-chloro-4-hydroxy-phenyl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (1,2-dimethyl-propyl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (1-ethyl-propyl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid [3-(1-hydroxy-ethyl)-phenyl]-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (1-ethynyl-cyclohexyl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (2-methoxy-dibenzofuran-3-yl)-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid [2-(4-hydroxy-phenyl)-ethyl]-amide; 2-Cyclohexylamino-thiazole-4-carboxylic acid (4-hydroxy-cyclohexyl)-amide; 2-(2,6-Difluoro-benzylamino)-N-[2-(3-trifluoromethyl-phenyl)-ethyl]-acetamide; 4-{4-[2-(4-Dimethylamino-phenyl)-acetyl]-piperazin-1-yl}-3-(2-phenyl-propylamino)-benzamide; 2-(2-Ethyl-phenylsulfanyl)-3-[methyl-(2-pyridin-4-yl-ethyl)-amino]-N-prop-2-ynyl-propionamide; 4-Methyl-cyclohexanecarboxylic acid {[2-(2-chloro-6-fluoro-benzylsulfanyl)-ethylcarbamoyl]-methyl}-prop-2-ynyl-amide; 2-Benzylsulfanyl-N-{[2-(2-chloro-6-fluoro-benzylsulfanyl)-ethylcarbamoyl]-methyl}-N-(2-methoxyethyl)-acetamide; 4-[2-(5-Cyclopropylmethylsulfanyl-[1,3,4]thiadiazol-2-ylsulfanyl)-ethyl]-N-(6,6-dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-benzamide; N-(6,6-Dimethyl-bicyclo[3.1.1]hept-2-ylmethyl)-2-p-tolyloxy-acetamide; Bicyclo[2.2.1]hept-5-ene-2-carboxylic acid [4-(2,5-difluoro-phenoxy)-butyl]-amide; 4-Trifluoromethyl-cyclohexanecarboxylic acid [6-(2,6-difluoro-phenoxy)-hexyl]-amide; N-Cyclopropyl-3-methoxy-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)-benzamide; 3-Methoxy-N-(2-methoxy-ethyl)-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)-benzamide; 3-Methoxy-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)-N-(tetrahydro-furan-2-ylmethyl)benzamide; 3-Methoxy-N-(2-oxo-azepan-3-yl)-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)-benzamide; 3-Methoxy-N-[3-(2-oxo-pyrrolidin-1-yl)-propyl]-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)benzamide; 3-Methoxy-N-methyl-N-(2-piperidin-4-yl-ethyl)-5-(pyridine-2-carbonyl)-benzamide; [2-({Cyclopropyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-phenoxy]-acetic acid;
(2-{[[3-Methoxy-5-(pyridine-2-carbonyl)-benzoyl]-(3-methyl-butyl)-amino]-methyl}-phenoxy)acetic acid;
[2-({Cyclopentyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-phenoxy]-acetic acid; [2-({(2-Methoxy-ethyl)-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-phenoxy]-acetic acid; [2-({Carbamoylmethyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-phenoxy]-acetic acid; [2-({[3-Methoxy-5-(pyridine-2-carbonyl)-benzoyl]-pyridin-4-yl-amino}-methyl)-phenoxy]-acetic acid; [2-({Cyclopropylmethyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-phenoxy]-acetic acid; [2-({[3-Methoxy-5-(pyridine-2-carbonyl)-benzoyl]-methyl-amino}-methyl)-phenoxy]-acetic acid; [4-(4-Hydroxy-benzyl)-piperazin-1-yl]-[3-methoxy-5-(pyridine-2-carbonyl)-phenyl]-methanone; {Carbamoylmethyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-acetic acid; {(3-Imidazol-1-yl-propyl)-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-acetic acid; {[3-Methoxy-5-(pyridine-2-carbonyl)-benzoyl]-pyridin-4-yl-amino}-acetic acid; [[3-Methoxy-5-(pyridine-2-carbonyl)-benzoyl]-(2-oxo-azepan-3-yl)-amino]-acetic acid; 3-Methoxy-N-(2-methoxy-ethyl)-N-piperidin-3-ylmethyl-5-(pyridine-2-carbonyl)-benzamide; 4-[3-Methoxy-5-(pyridine-2-carbonyl)-benzoylamino]-piperidine-1-carboxylic acid ethyl ester; 3-Methoxy-N-[3-(2-oxo-pyrrolidin-1-yl)-propyl]-5-(pyridine-2-carbonyl)-benzamide; 3-({Carbamoylmethyl-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-benzoic acid; 3-({(3-Imidazol-1-yl-propyl)-[3-methoxy-5-(pyridine-2-carbonyl)-benzoyl]-amino}-methyl)-benzoic acid; 4-Amino-N-(3-hydroxy-benzyl)-N-indan-2-yl-2-propionylamino-butyramide; 5-Amino-2-propionylamino-pentanoic acid (3-hydroxy-benzyl)-indan-2-yl-amide; N-Ethyl-2-hexylamino-N-(4-hydroxy-benzyl)-acetamide; 2-Hexylamino-N-(4-hydroxy-benzyl)-N-methyl-acetamide; 1-[1-(6-Phenyl-hexanoyl)-piperidin-4-yl]-1,3-dihydro-benzoimidazol-2-one; 1-[1-(3-Cyclohexyl-propionyl)-piperidin-4-yl]-1,3-dihydro-benzoimidazol-2-one; N-(2-Hydroxy-benzyl)-N-isobutyl-benzamide; N-(2-Hydroxy-benzyl)-2-(4-hydroxy-phenyl)-N-isobutyl-acetamide; N-(2-Hydroxy-benzyl)-N-(3-methyl-butyl)-benzamide; N-(4-Hydroxy-benzyl)-N-isobutyl-benzamide; 4-Hydroxy-N-(4-hydroxy-benzyl)-N-isobutyl-benzamide; N-(4-Hydroxy-benzyl)-2-(4-hydroxy-phenyl)-N-isobutyl-acetamide; N-(4-Hydroxy-benzyl)-N-(3-methyl-butyl)-benzamide; N-(2-Ethoxy-ethyl)-4-hydroxy-N-(4-hydroxy-benzyl)-benzamide; N-(4-Hydroxy-benzyl)-N-(3-isopropoxy-propyl)-benzamide; N-(3-Hydroxy-benzyl)-N-(4-methyl-pentyl)-benzamide; N-(3-Hydroxy-benzyl)-2-(4-hydroxy-phenyl)-N-(4-methyl-pentyl)-acetamide; N-(3-Hydroxy-benzyl)-N-(3-isopropoxy-propyl)-benzamide; N-(2-Hydroxy-benzyl)-N-(3-methyl-butyl)-4-propyl-benzamide; N-(4-Hydroxy-benzyl)-N-(6-hydroxy-hexyl)-4-propyl-benzamide; N-(4-Hydroxy-benzyl)-N-(3-methyl-butyl)-4-propyl-benzamide; and N-[2-(4-Fluoro-benzylamino)-thiazol-4-ylmethyl]-N-phenethyl-butyramide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
16 . A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 3 , together with one or more pharmaceutically acceptable carriers or excipients.
17 . The pharmaceutical composition according to claim 16 , wherein the pharmaceutical composition is for oral, nasal, buccal, transdermal, pulmonal or parenteral administration.
18 . The pharmaceutical composition according to claim 16 , wherein the pharmaceutical composition is in unit dosage form, comprising from about 0.05 mg to about 2000 mg/day, from about 0.1 mg to about 1000 mg, or from about 0.5 mg to about 500 mg per day of the compound.
19 . A method for the treatment, prevention and/or prophylaxis of conditions, disorders or diseases wherein a modulation or an inhibition of the activity of 11βHSD1 is beneficial, the method comprising administering to a subject in need thereof an effective amount of a compound according to claim 3 .
20 . The method according to claim 19 , wherein the treatment, prevention and/or prophylaxis is of any conditions, disorders and diseases that are influenced by intracellular glucocorticoid levels.
21 . The method according to claim 19 or 20 , wherein the condition, disorder or disease is the metabolic syndrome, insulin resistance, dyslipidemia, hypertension and obesity.
22 . The method according to claim 19 or 20 , wherein the condition, disorder or disease is type 2 diabetes, impaired glucose tolerance (IGT), impaired fasting glucose (IFG).
23 . The method according to claim 19 or 20 , for the delaying or prevention of the progression from IGT to type 2 diabetes.
24 . The method according to claim 19 or 20 , for the delaying or prevention of the progression of the metabolic syndrome into type 2 diabetes.
25 . The method according to claim 19 or 20 , wherein the condition, disorder or disease is diabetic late complications including cardiovascular diseases; arteriosclerosis; atherosclerosis.
26 . The method according to claim 19 or 20 , wherein the condition, disorder or disease is neurodegenerative and psychiatric disorders.
27 . The method according to claim 19 or 20 , for the treatment, prevention and/or prophylaxis of adverse effects of glucocorticoid receptor agonist treatment or therapy.
28 . A compound of formula (II)
wherein
R 1 is C 3 -C 10 cycloalkyl or C 3 -C 10 hetcycloalkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 4 ;
R 2 is hydrogen, C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 5 ; or
R 1 and R 2 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 14 ;
R 3 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl or hetaryl, wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 ;
R 4 and R 5 independently are hydrogen, hydroxy, oxo, cyano, halo, methylendioxo, NR 8 R 9 , C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethyloxy, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkenyl, aryl, hetaryl, hetarylSO n , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, arylC 1 -C 6 alkyl-R 6 —C 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylSO n , C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 15 ;
R 6 is oxygen, sulphur, SO n or NR 16 ;
R 7 is hydrogen, halo, hydroxy, cyano, nitro, COOR 17 , C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, methylendioxo, trihalomethyl, trihalomethyloxy, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, NR 8 R 9 , SO m NR 8 R 9 , NR 4 R 5 carbonylC 1 -C 6 alkyl, arylthio, hetarylthio, R 18 carbonylNR 8 , arylSO n , hetarylSO n , R 19 SO m NR 8 , arylthioC 1 -C 6 alkyl, hetarylthioC 1 -C 6 alkyl or arylC 1 -C 6 alkylR 6 C 1 -C 6 alkyl; wherein the aryl and hetaryl groups independently are optionally substituted with one or more R 10 ;
R 8 and R 9 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, C 1 -C 6 alkylSO m , arylSO m , arylC 1 -C 6 alkylSO m , arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 11 ; or
R 8 and R 9 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system optionally being substituted with at least one halo, cyano, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, hydroxy, oxo, halo, cyano, nitro, C 1 -C 8 alkyl, C 1 -C 6 alkyl-oxy, NR 12 R 13 , methylendioxo, trihalomethyl or trihalomethyloxy;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl or arylC 1 -C 6 alkyl;
R 14 is hydrogen, halo, hydroxy, oxo, nitro, cyano, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy or aryloxy;
R 15 is hydrogen, halo, hydroxy, oxo, nitro, cyano, CONR 8 R 9 or COOR 17 ;
R 16 is hydrogen, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, aryloxyC 1 -C 6 alkyl, hetaryloxyC 1 -C 6 alkyl, arylthioC 1 -C 6 alkyl or hetarylthioC 1 -C 6 alkyl; wherein the alkyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 10 ;
R 17 is hydrogen, C 1 -C 8 alkyl, aryl or arylC 1 -C 6 alkyl;
R 18 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy or R 8 R 9 NC 1 -C 6 alkyl wherein the alkyl, alkenyl, cycloalkyl, hetcycloalkyl, aryl and hetaryl groups are optionally substituted with R 15 ;
R 19 is C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, aryl, arylC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl;
m is 1 or 2;
n is 0, 1 or 2; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
29 . A compound according to claim 28 , wherein R 1 is C 3 -C 10 cycloalkyl or C 3 -C 10 hetcycloalkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 4 .
30 . A compound according to claim 28 , wherein R 2 is hydrogen or C 1 -C 8 alkyl.
31 . A compound according to claim 28 , wherein R 1 and R 2 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 14 .
32 . A compound according to claim 28 , wherein R 3 is aryl or hetaryl, wherein the aryl and hetaryl groups independently are optionally substituted with one or more of R 7 .
33 . A compound according to claim 28 , wherein R 4 and R 5 independently are hydrogen, hydroxy, oxo, halo, C 1 -C 8 alkyl, wherein the alkyl group is optionally substituted with one or more of R 15 .
34 . A compound according to claim 28 , wherein R 7 is hydrogen, halo, hydroxy, cyano, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, trihalomethyl, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, NR 8 R 9 , R 18 carbonylNR 8 , R 19 SO m NR 8 ; wherein the aryl and hetaryl groups independently are optionally substituted with one or more R 10 .
35 . A compound according to claim 28 , wherein R 8 and R 9 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulfur, the ring system optionally being substituted with at least one halo, cyano, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy, hetarylcarboxy, arylC 1 -C 6 alkylcarboxy or hetarylC 1 -C 6 alkylcarboxy.
36 . A compound according to claim 28 , wherein R 15 is CONR 8 R 9 .
37 . A compound according to claim 28 , wherein R 18 is C 1 -C 6 alkyl.
38 . A compound according to claim 28 , which is:
(4-Tetrazol-1-yl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-Cyclohexyl-N-methyl-2-phenoxymethyl-benzamide; 4-Amino-N-cyclohexyl-N-methyl-benzamide; N-Cycloheptyl-N-methyl-2-phenoxymethyl-benzamide; N-Cyclohexyl-N-methyl-benzamide; 2-Chloro-N-cyclohexyl-6-fluoro-N-methyl-benzamide; N-Cyclohexyl-N-methyl-4-trifluoromethoxy-benzamide; N-Cyclohexyl-2,3, N-trimethyl-benzamide; 3,5-Dichloro-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-N-methyl-2-phenoxy-benzamide; 2,4-Bis-benzyloxy-N-cyclohexyl-N-methyl-benzamide; 2-Benzyloxy-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-N-methyl-4-phenoxy-benzamide; 4-Benzyloxy-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-N-methyl-4-phenoxymethyl-benzamide; 2-Chloro-N-cyclohexyl-N-ethyl-4-nitro-benzamide; 4-Chloro-N-cyclohexyl-N-ethyl-3-nitro-benzamide; 6-Fluoro-4H-benzo[1,3]dioxine-8-carboxylic acid cyclohexyl-methyl-amide; Azepan-1-yl-(2-chloro-phenyl)-methanone; Azepan-1-yl-(3-chloro-phenyl)-methanone; Azepan-1-yl-phenyl-methanone; 2-(Biphenyl-4-yloxy)-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-2-(3,5-dimethoxy-phenoxy)-N-methyl-benzamide; N-Cyclohexyl-2-(2,3-dimethoxy-phenoxy)-N-methyl-benzamide; 2,4-Dichloro-N-(3,3-dimethyl-1,5-dioxa-spiro[5.5]undec-9-yl)-N-methyl-benzamide; 2,4-Dichloro-N-methyl-N-(4-oxo-cyclohexyl)-benzamide; N-Cyclohexyl-2-hydroxy-N-methyl-benzamide; N-Cyclohexyl-3-methoxy-N-methyl-benzamide; Benzo[1,3]dioxole-5-carboxylic acid cyclohexyl-methyl-amide; 3-Benzyloxy-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-3-hydroxy-N-methyl-benzamide; [4-(Morpholine-4-sulfonyl)-phenyl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-Benzyl-3-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-benzenesulfonamide; [4-Fluoro-3-(morpholine-4-sulfonyl)-phenyl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Thiophene-2-sulfonic acid [4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-amide; N-Phenyl-4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-benzenesulfonamide; (4-Phenoxy-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-(2,4-Dimethyl-phenyl)-3-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)benzenesulfonamide; (2-Phenoxymethyl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 4-(3-Aza-bicyclo[3.2.2]nonane-3-carbonyl)-N,N-dipropyl-benzenesulfonamide; 2-Bromo-N-cyclohexyl-N-methyl-benzamide; N-[4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-acetamide; (4-Dimethylamino-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Pyrrol-1-yl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Imidazol-1-yl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Amino-2-methoxy-phenyl)-(trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Methanesulfonyl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Methanesulfonyl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Benzenesulfonyl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Azepan-1-yl-[4-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-phenyl]-methanone; Azepan-1-yl-(4-morpholin-4-ylmethyl-phenyl)-methanone; [4-(3-Trifluoromethyl-pyrazol-1-yl)-phenyl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-[1,2,4]Triazol-1-yl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (4-Pyrazol-1-yl-phenyl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 2-Benzyloxymethyl-N-cyclohexyl-N-methyl-benzamide; N-Cyclohexyl-N-methyl-4-(3-methyl-5-oxo-4,5-dihydro-pyrazol-1-yl)-benzamide; 5-Methyl-2-[4-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-2,4-dihydropyrazol-3-one; (9H-Carbazol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; [4-(3,5-Dimethyl-pyrazol-1-yl)-phenyl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Phenyl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Azepan-1-yl-(2-bromo-phenyl)-methanone; (3-Aza-bicyclo[3.2.2]non-3-yl)-(2-bromo-phenyl)-methanone; (4-Benzyl-piperidin-1-yl)-quinolin-2-yl-methanone; (2-Methyl-piperidin-1-yl)-quinolin-2-yl-methanone; (3-Aza-bicyclo[3.2.2]non-3-yl)-quinolin-2-yl-methanone; Quinoline-2-carboxylic acid cyclohexyl-methyl-amide; Quinolin-2-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 1-[4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-phenyl]-pyrrolidine-2,5-dione; Pyridin-3-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Pyridin-4-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Pyridin-2-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Pyrazol-1-yl-pyridin-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-benzoic acid; Imidazo[2,1-b]thiazol-6-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 8-(4-Dimethylamino-benzoyl)-8-aza-bicyclo[3.2.1]octan-3-one; (4-Dimethylamino-phenyl)-(3-hydroxy-8-aza-bicyclo[3.2.1]oct-8-yl)-methanone; (4-Dimethylamino-phenyl)-(3-hydroxy-3-methyl-8-aza-bicyclo[3.2.1]oct-8-yl)-methanone; and Trifluoro-acetic acid 8-(4-dimethylamino-benzoyl)-8-aza-bicyclo[3.2.1]oct-3-yl ester; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
39 . A compound of formula (III):
wherein
R 1 is aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl optionally substituted with one or more of R 6 independently;
R 2 is halo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, trihalomethyl, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 -alkylNR 5 C 1 -C 6 alkyl, arylC 1 -C 6 alkylNR 5 C 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, alkenyl, alkynyl, cycloalkyl and aryl groups independently are optionally substituted with one or more R 7 ;
R 3 is C 1 -C 6 alkyl optionally substituted with one or more of R 8 ;
R 4 is C 6 -C 10 cycloalkyl, C 6 -C 10 hetcycloalkyl, C 6 -C 10 cycloalkylC 1 -C 6 alkyl or C 6 -C 10 hetcycloalkylC 1 -C 6 alkyl wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 8 ; or
R 3 and R 4 together with the nitrogen to which they are attached, are forming a saturated or partially saturated bicyclic/bridge ring system containing from 7 to 12 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy or hetarylC 1 -C 6 alkyloxy, wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 9 ;
R 5 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 -cycloalkylC 1 -C 6 alkyl, C 3 -C 10 hetcycloalkylC 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl wherein the alkyl, alkenyl, alkynyl, aryl, hetaryl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 9 ;
R 6 and R 7 independently are hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 -alkyloxy, trihalomethyl, trihalomethoxy, NR 10 R 11 , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 -alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkyloxycarbonyl, aryloxycarbonyl, arylC 1 -C 6 alkyloxycarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 8 and R 9 independently are hydrogen, C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 -alkyl, hydroxy, oxo, cyano, NR 10 R 11 , C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, hetaryloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl; or
R 10 and R 11 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1-6 -alkylcarboxy; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
40 . A compound according to claim 39 , wherein
R 1 is aryl or hetaryl optionally substituted with one or more R 6 independently; R 2 is halo, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylNR 5 C 1 -C 6 alkyl, arylC 1 -C 6 alkylNR 5 C 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, alkenyl, alkynyl, cycloalkyl and aryl groups independently are optionally substituted with one or more R 7 ; R 3 is C 1 -C 6 alkyl optionally substituted with one or more of R 8 ; R 4 is C 6 -C 10 cycloalkyl, C 6 -C 10 hetcycloalkyl, C 6 -C 10 cycloalkylC 1 -C 6 alkyl or C 6 -C 10 hetcycloalkylC 1 -C 6 alkyl wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 8 ; R 5 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 -cycloalkylC 1 -C 6 alkyl, C 3 -C 10 hetcycloalkylC 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl wherein the alkyl, alkenyl, alkynyl, aryl, hetaryl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 9 ; R 6 and R 7 independently are hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 -alkyloxy, trihalomethyl, trihalomethoxy, NR 10 R 11 , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 -alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkyloxycarbonyl, aryloxycarbonyl, arylC 1 -C 6 alkyloxycarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; R 8 and R 9 independently are hydrogen, C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 -alkyl, hydroxy, oxo, cyano, NR 10 R 11 , C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, hetaryloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkyl-carbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkyl-carbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; R 10 and R 11 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl; or R 10 and R 11 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetaryl C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1-6 -alkylcarboxy; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
41 . A compound according to claim 39 , wherein R 1 is aryl, arylC 1 -C 6 alkyl or hetaryl optionally substituted with one or more of R 6 .
42 . A compound according to claim 39 , wherein R 2 is C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, trihalomethyl, arylC 1 -C 6 alkyl, or hetarylC 1 -C 6 alkyl wherein the alkyl, cycloalkyl and aryl groups independently are optionally substituted with one or more R 7 .
43 . A compound according to claim 39 , wherein R 3 is C 1 -C 6 alkyl optionally substituted with one or more of R 8 .
44 . A compound according to claim 39 , wherein R 4 is C 6 -C 10 cycloalkyl, or C 6 -C 10 hetcycloalkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 3 .
45 . A compound according to claim 39 , wherein R 6 and R 7 independently are hydrogen, hydroxy, oxo, halo, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, NR 10 R 11 , arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkyloxycarbonyl, aryloxycarbonyl or arylC 1 -C 6 alkyloxycarbonyl.
46 . A compound according to claim 39 , wherein R 8 and R 9 independently are hydrogen, C 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy or arylC 1 -C 6 alkyloxy.
47 . A compound according to claim 39 , wherein R 10 and R 11 independently are hydrogen or C 1 -C 8 alkyl.
48 . A compound according to claim 39 , which is 1-(4-Chloro-phenyl)-5-propyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide, or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
49 . A compound according to claim 39 , selected from the group consisting of: 1-(4-Chlorophenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; [1-(4-Methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; [1-(4-Chloro-phenyl)-5-propyl-1H-pyrazol-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and [1-(3,5-Dichloro-phenyl)-5-propyl-1H-pyrazol-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
50 . A compound according to claim 39 , selected from the group consisting of:
1-(Phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(4-Fluoro-phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(4-Methoxy-phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(4-Chloro-phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(2-Methyl-phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(4-Amino-phenyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; 1-(2-Pyridyl)-5-methyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; and 1-(2-Pyridyl)-5-propyl-1H-pyrazole-4-carboxylic acid cyclohexyl-methyl-amide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
51 . A compound of formula (IV):
wherein
R 1 is hydrogen, trihalomethyl, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkylthio, aryl, arylC 1 -C 6 alkyl, hetaryl or hetaralkyl, wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 8 ;
R 2 , R 3 , R 4 and R 5 independently are hydrogen, halo, nitro, cyano, hydroxy, NR 9 R 10 , trihalomethyl, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkylthio, aryl, arylC 1 -C 6 alkyl, hetaryl or hetaralkyl, wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 8 ; or
R 2 together with R 3 are forming a saturated or partially saturated cyclic ring system containing from 3 to 6 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy or hetarylC 1 -C 6 alkyloxy; or
R 3 together with R 4 are forming a saturated or partially saturated cyclic ring system containing from 3 to 6 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy or hetarylC 1 -C 6 alkyloxy; or
R 4 together with R 5 are forming a saturated or partially saturated cyclic ring system containing from 3 to 6 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy or hetarylC 1 -C 6 alkyloxy;
R 6 is aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl, wherein the alkyl, aryl and cycloalkyl groups independently are optionally substituted with one or more of R 11 ;
R 7 is C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl, wherein the alkyl, aryl and cycloalkyl groups independently are optionally substituted with one or more of R 11 ; or
R 6 and R 7 , together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1-6 -alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 8 ;
R 9 and R 10 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl, wherein the alkyl, aryl and cycloalkyl groups independently are optionally substituted with one or more of R 11 ; or
R 9 and R 10 , together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 -alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 8 ;
R 8 and R 11 independently are hydrogen, halo, hydroxy, oxo, nitro, cyano, C 1 -C 8 alkyl, C 1 -C 6 -alkyloxy or aryloxy; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
52 . A compound according to claim 51 , wherein R 1 is hydrogen or C 1 -C 6 alkyl, wherein the alkyl group is optionally substituted with one or more of R 8 .
53 . A compound according to claim 51 , wherein R 2 , R 3 , R 4 and R 5 are hydrogen.
54 . A compound according to claim 51 , wherein R 6 and R 7 , together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional nitrogen or oxygen atoms, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 -alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 8 .
55 . A compound according to claim 51 , which is:
pyrazolo[1,5-a]pyridin-3-yl-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
56 . A compound according to claim 51 , which is selected from:
(2-Methyl-pyrazolo[1,5-a]pyridin-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and Pyrazolo[1,5-a]pyridine-3-carboxylic acid cyclohexyl-methyl-amide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
57 . A compound of formula (V):
wherein
R 1 is hydrogen, C 1 -C 8 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, C 1 -C 6 SO 2 , arylSO 2 , hetarylSO 2 , arylC 1 -C 6 alkylSO 2 or hetarylC 1 -C 6 alkylSO 2 optionally substituted with one or more R 8 ;
R 2 and R 5 independently are hydrogen, halo, nitro, cyano, trihalomethyl, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl, arylalkyl, hetaryl and hetarylalkyl groups independently are substituted with one or more R 9 ; and
either R 3 is hydrogen; and R 4 is C(O)NR 7 R 8 ; or
R 3 is C(O)NR 7 R 8 ; and R 4 is hydrogen;
R 6 is hydrogen, halo, cyano, trihalomethyl, NR 12 R 13 , C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl, arylalkyl, hetaryl and hetarylalkyl groups independently are substituted with one or more R 9 ; and
R 7 and R 8 independently are C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 10 ; or
R 7 and R 8 together with the nitrogen to which they are attached, are forming a saturated or partially saturated bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen or oxygen, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 11 ;
R 9 is hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethoxy, NR 12 R 13 , C(O)NR 12 R 13 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 8 alkylcarbonyl, hetarylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl; or
R 12 and R 13 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
58 . A compound according to claim 57 , of formula (Va):
wherein
R 1 is hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl optionally substituted with one or more R 8 ;
R 2 and R 5 independently are hydrogen, halo, nitro, cyano, trihalomethyl, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl, arylalkyl, hetaryl and hetarylalkyl groups independently are substituted with one or more R 8 ; and
either R 3 is hydrogen; and R 4 is C(O)NR 6 R 7 ; or R 3 is C(O)NR 6 R 7 ; and R 4 is hydrogen;
R 6 and R 7 independently are C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 9 ; or
R 6 and R 7 together with the nitrogen to which they are attached, are forming a saturated or partially saturated bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen or oxygen, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 10 ;
R 8 is hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethoxy, NR 11 R 12 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 9 and R 10 independently are hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl;
R 11 and R 12 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkyl-carboxyC 1 -C 6 alkyl; or
R 11 and R 12 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkyl-carbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
59 . A compound according to claim 57 , wherein R 1 is hydrogen, C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, arylSO 2 , hetarylSO 2 , arylC 1 -C 6 alkylSO 2 or hetarylC 1 -C 6 alkylSO 2 all of which is optionally substituted with one or more R 8 .
60 . A compound according to claim 57 , wherein R 2 and R 5 are hydrogen.
61 . A compound according to claim 57 , wherein R 3 is hydrogen and R 4 is C(O)NR 7 R 8 .
62 . A compound according to claim 57 , wherein R 3 is C(O)NR 7 R 8 and R 4 is hydrogen.
63 . A compound according to claim 57 , wherein R 6 is hydrogen, NR 12 R 13 , C 1 -C 6 alkyl, aryl or hetaryl wherein the alkyl, aryl and hetaryl independently are substituted with one or more R 9 .
64 . A compound according to claim 57 , wherein R 7 and R 8 independently are C 1 -C 8 alkyl or C 3 -C 10 cycloalkyl, wherein the alkyl and cycloalkyl groups independently are optionally substituted with one or more of R 10 .
65 . A compound according to claim 57 , wherein R 9 is hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethoxy, NR 12 R 13 , C(O)NR 12 R 13 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl.
66 . A compound according to claim 57 , wherein R 10 and R 11 independently are hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl.
67 . A compound according to claim 57 , which is:
1H-Benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide, or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
68 . A compound according to claim 57 , selected from the group consisting of:
1-Benzyl-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; and (1H-Benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
69 . A compound according to claim 57 , selected from the group consisting of:
Isopropyl-2-trifluoromethyl-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; 1-Benzyl-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; 2-Methyl-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; 2-Hydroxymethyl-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; 2-(4-Amino-phenyl)-1H-benzoimidazole-5-carboxylic acid cyclohexyl-methyl-amide; (1H-Benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (2-Methyl-1H-benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (2-Amino-1H-benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (2-Benzo[1,3]dioxol-5-yl-1H-benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 3-[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-benzoimidazol-2-yl]-benzoic acid methyl ester; (2-Thiophen-2-yl-1H-benzoimidazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and [2-(2-Nitro-phenyl)-1H-benzoimidazol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
70 . A compound of formula (VI):
wherein
X is oxygen or (CR 1 R 2 ) n ;
R 1 , R 2 , R 3 , and R 4 independently are hydrogen, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl optionally substituted with one or more R 8 independently; or
R 1 and either R 3 or R 4 together are forming a saturated or partially saturated ring system containing from 4 to 8 carbon atoms, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, hydroxy, oxo, aryl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl; or
R 1 and either R 3 or R 4 together with the single bond are forming a carbon-carbon double bond;
R 5 is C 1 -C 8 alkyl optionally substituted with one or more of R 9 ;
R 6 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 9 ; or
R 5 and R 6 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 10 ;
R 7 is hydrogen, halo, nitro, NR 12 R 13 , cyano, trihalomethyl, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, hetaryl, hetarylC 1 -C 6 alkyl, hetaryloxy or hetarylC 1 -C 6 -alkyloxy optionally substituted with one or more R 11 independently;
R 8 and R 9 independently are hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 -alkyloxy, trihalomethyl, trihalomethoxy, NR 12 R 13 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 10 is hydrogen, C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy;
R 11 is hydrogen, halo, hydroxy, oxo, nitro, cyano, C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, aryloxy or hetaryloxy;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 1 -C 6 alkylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 3 -C 10 cycloalkylC 1 -C 6 -alkyl, C 1 -C 6 alkyloxycarbonyl; or
R 12 and R 13 are together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1-6 alkylcarboxy;
n is 1 or 2; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
71 . A compound according to claim 70 , wherein X is (CR 1 R 2 ) n .
72 . A compound according to claim 70 , wherein X is oxygen.
73 . A compound according to claim 70 , wherein R 1 , R 2 , R 3 , and R 4 independently are hydrogen, C 1 -C 6 alkyl or arylC 1 -C 6 alkyl, optionally substituted with one or more R 8 .
74 . A compound according to claim 70 , wherein R 1 and either R 3 or R 4 together with the single bond are forming a carbon-carbon double bond.
75 . A compound according to claim 70 , wherein R 5 is C 1 -C 8 alkyl optionally substituted with one or more of R 9 .
76 . A compound according to claim 70 , wherein R 6 is C 3 -C 10 cycloalkyl or C 3 -C 10 hetcycloalkyl, each of which is optionally substituted with one or more of R 9 .
77 . A compound according to claim 70 , wherein R 5 and R 6 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 10 .
78 . A compound according to claim 70 , wherein R 7 is hydrogen, halo, NR 12 R 13 , trihalomethyl, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, hetaryloxy optionally substituted with one or more R 11 independently.
79 . A compound according to claim 70 , wherein R 8 and R 9 independently are hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl or NR 12 R 13 .
80 . A compound according to claim 70 , wherein R 10 is hydrogen or C 1 -C 8 alkyl.
81 . A compound according to claim 70 , selected from the group consisting of:
2,3-Dimethyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2,5-Dimethyl-3-phenyl-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2,2-Dimethyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2-Methyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; (2,3-Dimethyl-2,3-dihydro-benzofuran-7-yl)-(2,4,4-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 4-Methoxy-2-methyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2-Methyl-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; (2-Methyl-2,3-dihydro-benzofuran-7-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2,3-Dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 3,3-Dimethyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; and Chroman-8-carboxylic acid cyclohexyl-methyl-amide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
82 . A compound according to claim 70 , selected from the group consisting of: 2,3-Dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; Benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2-Methyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2-Methyl-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 3,3-Dimethyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; (2,3-Dimethyl-2,3-dihydro-benzofuran-7-yl)-(2,4,4-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 4-Methoxy-2-methyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; 2,2-Dimethyl-2,3-dihydro-benzofuran-7-carboxylic acid cyclohexyl-methyl-amide; (2-Methyl-2,3-dihydro-benzofuran-7-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and
Chroman-8-carboxylic acid cyclohexyl-methyl-amide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
83 . A compound of formula (VII):
wherein
R 1 is hydrogen, C 1 -C 8 alkyl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl optionally substituted with one or more R 9 ;
R 2 , R 3 , R 4 , R 5 and R 6 independently are hydrogen, halo, nitro, cyano, trihalomethyl, carboxy, N(R 12 R 13 ), C(O)NR 7 R 8 , C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, N(R 12 R 13 )C 1 -C 6 alkyl, C 1 -C 6 alkylcarboxy, arylcarboxy, arylC 1 -C 6 alkylcarboxy, C 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, aryloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxy, arylC 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, hetaryl, hetarylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyloxy, hetaryloxyC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyloxyC 1 -C 6 alkyl wherein the alkyl, aryl, arylalkyl, hetaryl and hetarylalkyl groups independently are substituted with one or more R 9 ;
R 7 is hydrogen or C 1 -C 8 alkyl optionally substituted with one or more of R 10 ;
R 8 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 10 ; or
R 7 and R 8 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen or oxygen, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyl-oxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 11 ;
R 9 is hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethoxy, NR 12 R 13 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy;
R 10 and R 11 independently are hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl;
R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 3 -C 10 cycloalkylcarbonyl, C 3 -C 10 hetcycloalkylcarbonyl or C 3 -C 10 cycloalkylC 1 -C 6 alkylcarbonyl wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 11 , wherein R 11 is as defined above; or
R 12 and R 13 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
84 . A compound according to claim 83 , wherein
R 1 is hydrogen, C 1 -C 8 alkyl, hetaryl, arylC 1 -C 6 alkyl or hetarylC 1 -C 6 alkyl optionally substituted with one or more R 9 ; R 2 and R 5 independently are hydrogen, halo, nitro, cyano, trihalomethyl, C 1 -C 6 alkyl, C 1 -C 6 -alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, aryloxy, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 -alkyloxy, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, hetaryl or hetarylC 1 -C 6 alkyl wherein the alkyl, aryl, arylalkyl, hetaryl and hetarylalkyl groups independently are substituted with one or more R 9 ; and either R 3 is C(O)NR 7 R 8 , and R 4 is hydrogen; or R 3 is hydrogen, and R 4 is C(O)NR 7 R 8 ; R 6 is C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, N(R 12 R 13 )C 1 -C 6 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 -alkyl, aryloxyC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxy or arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl; R 7 is C 1 -C 8 alkyl optionally substituted with one or more of R 10 ; R 8 is C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 10 ; or R 7 and R 8 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen or oxygen, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyl-oxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 11 ; R 9 is hydrogen, hydroxy, oxo, halo, nitro, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyloxy, trihalomethyl, trihalomethoxy, NR 12 R 13 , arylC 1 -C 6 alkyloxy, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; R 10 and R 11 independently are hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl; R 12 and R 13 independently are hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, arylC 1 -C 6 alkylcarbonyl, C 3 -C 10 cycloalkylcarbonyl, C 3 -C 10 hetcycloalkylcarbonyl or C 3 -C 10 cycloalkylC 1 -C 6 alkylcarbonyl; or R 12 and R 13 together with the nitrogen to which they are attached, are forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyl-oxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
85 . A compound according to claim 83 , wherein R 2 is C(O)NR 7 R 8 and R 3 , R 4 , and R 5 are hydrogen.
86 . A compound according to claim 83 , wherein R 3 is C(O)NR 7 R 8 and R 4 is hydrogen.
87 . A compound according to claim 83 , wherein R 4 is C(O)NR 7 R 8 and R 3 is hydrogen.
88 . A compound according to 83, wherein R 5 is C(O)NR 7 R 8 and R 2 , R 3 , and R 4 are hydrogen.
89 . A compound according to claim 83 , wherein R 6 is C(O)NR 7 R 8 .
90 . A compound according to claim 83 , selected from the group consisting of:
(1H-Indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and 1H-Indole-6-carboxylic acid cyclohexyl-methyl-amide; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
91 . A compound according to claim 83 , selected from the group consisting of:
(1H-Indol-7-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1H-Indol-6-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 1H-Indole-6-carboxylic acid adamantan-2-ylamide; (6-Aza-bicyclo[3.2.1]oct-6-yl)-(1H-indol-6-yl)-methanone; 1H-Indole-6-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide; 1H-Indole-5-carboxylic acid adamantan-2-ylamide; (6-Aza-bicyclo[3.2.1]oct-6-yl)-(1H-indol-5-yl)-methanone; (1H-Indol-4-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1H-Indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1H-Indol-2-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1-Methyl-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Aza-bicyclo[3.2.2]non-3-yl)-(1H-indol-3-yl)-methanone; 1-Methyl-1H-indole-3-carboxylic acid cycloheptylamide; 1-Methyl-1H-indole-3-carboxylic acid adamantan-1-ylamide; (3-Aza-bicyclo[3.2.2]non-3-yl)-(1-methyl-1H-indol-3-yl)-methanone; (1-Methyl-1H-indol-3-yl)-(4-methyl-piperazin-1-yl)-methanone; 1-Methyl-1H-indole-3-carboxylic acid (3-hydroxy-adamantan-1-yl)-amide; 1-Methyl-1H-indole-3-carboxylic acid azepan-1-ylamide; 1-Methyl-1H-indole-3-carboxylic acid (2-oxo-azepan-3-yl)-amide; (4-Benzyl-piperidine-1-yl)-(1-methyl-1H-indol-3-yl)-methanone; 1-Methyl-1H-indole-3-carboxylic acid (2,6-dimethyl-piperidin-1-yl)-amide; 1-Methyl-1H-indole-3-carboxylic acid (2-methyl-piperidin-1-yl)-amide; (1-Cyclopropylmethyl-6-fluoro-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; Azepan-1-yl-(1-methyl-1H-indol-3-yl)-methanone; (5-Benzyloxy-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (5H-[1,3]Dioxolo[4,5]indol-7-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (5-Chloro-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Trifluoromethyl-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Methyl-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Nitro-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (5-Methoxy-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Fluoro-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (6-Methoxy-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (7-Nitro-1H-indol-3-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1H-Indol-4-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 2-(1H-Indol-3-yl)-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-ethanone; 1-(3-Aza-bicyclo[3.2.2]non-3-yl)-2-(1H-indol-3-yl)-ethanone; 1-(3-Aza-bicyclo[3.2.2]non-3-yl)-2-(1-methyl-1H-indol-3-yl)-ethanone; 2-(1-Methyl-1H-indol-3-yl)-1-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-ethanone; [3-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indol-6-yloxy]-acetic acid tert-butyl ester; 6-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid; 6-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid ethyl ester; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid ethyl ester; 4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid; 4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid ethyl ester; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid ethyl ester; 4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid; 4-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid ethyl ester; [3-(Piperidine-1-carbonyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid cyanomethyl-amide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid benzylamide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid dimethylamide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid allylamide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (2-dimethylamino-ethyl)-methyl-amide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (2-methoxy-ethyl)-amide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid 4-methoxy-benzylamide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (tetrahydro-furan-2-ylmethyl)-amide; [3-(2-Methoxymethyl-pyrrolidine-1-carbonyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo-[3.2.1]oct-6-yl)-methanone; [3-(2,6-Dimethyl-morpholine-4-carbonyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (1,1-dioxo-tetrahydro-thiophen-3-yl)-amide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid [3-(4-methyl-piperazin-1-yl)-propyl]-amide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid 4-trifluoromethyl-benzylamide; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (furan-2-ylmethyl)-amide; [3-(2,3,5,6-Tetrahydro-[1,2′]bipyrazinyl-4-carbonyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (2H-tetrazol-5-ylmethyl)-amide; [3-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 3-{[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carbonyl]-amino}-propionic acid ethyl ester; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid (4-methoxy-phenyl)-amide; 3-{[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carbonyl]-amino}-propionic acid; Azepan-1-yl-(1H-indol-5-yl)-methanone; 1H-Indole-5-carboxylic acid dibenzylamide; (3-Aza-bicyclo[3.2.2]non-3-yl)-(1H-indol-5-yl)-methanone; (4-Benzyl-piperidin-1-yl)-(1H-indol-5-yl)-methanone; 8-(1H-Indole-5-carbonyl)-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one; [4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-(1H-indol-5-yl)-methanone; 1-[1-(1H-Indole-5-carbonyl)-piperidin-4-yl]-1,3-dihydro-benzoimidazol-2-one; (4-tert-Butyl-piperidin-1-yl)-(1H-indol-5-yl)-methanone; 1-(1H-Indole-5-carbonyl)-4-phenyl-piperidine-4-carbonitrile; (1H-Indol-5-yl)-(4-phenyl-piperidin-1-yl)-methanone; (5-Benzyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-(1H-indol-5-yl)-methanone; (1H-Indol-5-yl)-(4-pyrrolidin-1-yl-piperidin-1-yl)-methanone; 1H-Indole-5-carboxylic acid (5-hydroxy-1,3,3-trimethyl-cyclohexylmethyl)-amide; 1H-Indole-5carboxylic acid (3,4-dihydrospiro(1H-indene-1,4-piperidine)-amide; (3-Methanesulfonylmethyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Dimethylaminomethyl-1H-indol-6-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 1-{3-Acetyl-2-[5-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indol-3-yl]-2,3-dihydro-imidazol-1-yl}-ethanone; 1-Ethyl-3-[5-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indol-3-yl]-pyrrolidine-2,5-dione; (3-Thiazol-2-yl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Iodo-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 6-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carbonitrile; 5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carbonitrile; 6-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indole-3-carboxylic acid amide; [3-(2H-Tetrazol-5-yl)-1H-indol-6-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; N-[3-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-1H-indol-7-yl]-acetamide; (1-Benzenesulfonyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1-Benzenesulfonyl-2-methyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1-methyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (1-Benzyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; [6-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-indol-1-yl]-acetic acid ethyl ester; [1-(2-Ethoxy-ethyl)-1H-indol-6-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; {1-[2-(2-Methoxy-ethoxy)-ethyl]-1H-indol-6-yl}-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 3-[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-indol-1-yl]-propionic acid ethyl ester; (1-Phenethyl-1H-indol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; [1-(Tetrahydro-furan-2-ylmethyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 2-[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-indol-1-yl]-acetamide; [1-(4-Trifluoromethoxy-benzyl)-1H-indol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; 3-[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-indol-1-ylmethyl]-benzoic acid methyl ester; and 4-[5-(1,3,3-Trimethyl-6-aza-bicyclo[3.2.1]octane-6-carbonyl)-indol-1-ylmethyl]-benzonitrile; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
92 . A compound of formula (VIII):
wherein
X is NR 4 , S or O;
R 1 and R 2 independently are hydrogen, halo, cyano, trihalomethyl, C 1 -C 6 alkyl or C 1 -C 6 alkyloxy, wherein the alkyl groups independently are optionally substituted with one or more of R 7 ;
R 3 is hydrogen, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkylthio, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl, wherein the alkyl, cycloalkyl, aryl, hetaryl and hetarylalkyl groups independently are optionally substituted with one or more of R 7 ;
R 4 is hydrogen, C 1 -C 8 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryl, hetaryl, hetarylC 1 -C 6 alkyl, arylC 1 -C 6 alkyl, arylC 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 alkylcarboxyC 1 -C 6 alkyl wherein the alkyl, aryl, hetaryl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 7 ;
R 5 is hydrogen, and R 6 is adamantyl optionally substituted with hydroxy, C 1 -C 6 alkyloxy, aryl, arylC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, hetaryl, hetaryloxy or hetarylC 1 -C 6 alkyloxy wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 ; or
R 5 and R 6 are together with the nitrogen to which they are attached, forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylalkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 7 ;
R 7 are independently hydrogen, halo, hydroxy, oxo, nitro, NR 9 R 10 , cyano, COOR 8 , CONR 9 R 10 , C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, aryloxy, arylC 1 -C 6 alkyloxy, hetaryloxy or hetarylC 1 -C 6 alkyloxy;
R 8 is hydrogen, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetarylalkyl, wherein the alkyl, aryl and hetarylalkyl groups independently are optionally substituted with one or more of R 7 ;
R 9 and R 10 independently are hydrogen, C 1 -C 8 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, wherein the alkyl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 7 ; or
R 9 and R 10 together with the nitrogen to which they are attached, are forming a saturated or partially saturated bicyclic or tricyclic ring system containing from 4 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen or oxygen, the ring system optionally being substituted with at least one of C 1 -C 8 alkyl, arylC 1 -C 6 alkyl, hetarylC 1 -C 6 alkyl, hydroxy, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 -alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 11 ;
R 11 is hydrogen, halo, oxo, hydroxy, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl;
provided that hetcycloalkyl is not 7-aza[2,2,1]bicycloheptane; or
a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
93 . A compound according to claim 92 , wherein
X is NR 4 , S or O; R 1 and R 2 independently are hydrogen, halo, cyano, trihalomethyl, C 1 -C 6 alkyl or C 1 -C 6 alkyloxy, wherein the alkyl groups independently are optionally substituted with one or more of R 7 ; R 3 is hydrogen, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 1 -C 6 alkyloxy, C 1 -C 6 alkylthio, aryl, arylC 1 -C 6 alkyl, hetaryl or hetarylalkyl, wherein the alkyl, cycloalkyl, aryl, hetaryl and hetarylalkyl groups independently are optionally substituted with one or more of R 7 ; R 4 is hydrogen, C 1 -C 8 alkyl, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, arylC 1 -C 6 -alkyloxyC 1 -C 6 alkyl, C 3 -C 10 cycloalkyl, C 3 -C 10 hetcycloalkyl, C 3 -C 10 cycloalkylC 1 -C 6 alkyl, C 1 -C 6 -alkylcarboxyC 1 -C 6 alkyl wherein the alkyl, aryl, hetaryl, cycloalkyl and hetcycloalkyl groups independently are optionally substituted with one or more of R 7 ; R 5 is hydrogen, and R 6 is adamantyl optionally substituted with hydroxy, C 1 -C 6 alkyloxy, aryl, arylC 1 -C 6 alkyl, aryloxy, arylC 1 -C 6 alkyloxy, hetaryl, hetaryloxy or hetarylC 1 -C 6 alkyloxy wherein the alkyl, aryl and hetaryl groups independently are optionally substituted with one or more of R 7 ; or R 5 and R 6 are together with the nitrogen to which they are attached, forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylalkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 7 ; R 7 are independently hydrogen, halo, hydroxy, oxo, nitro, NR 5 R 6 , cyano, COOR 8 , CONR 5 R 6 , C 1 -C 8 alkyl, C 1 -C 6 alkyloxy, aryloxy or hetaryloxy; R 8 is hydrogen, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 alkyl, hetarylalkyl, wherein the alkyl, aryl and hetarylalkyl groups independently are optionally substituted with one or more of R 7 ; provided that hetcycloalkyl is not 7-aza[2,2,1]bicycloheptane; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
94 . A compound according to claim 92 , wherein X is NR 4 or S.
95 . A compound according to claim 92 , wherein R 1 and R 2 independently are hydrogen, halo, trihalomethyl or C 1 -C 6 alkyl, wherein the alkyl group is optionally substituted with one or more of R 7 wherein R 7 .
96 . A compound according to claim 92 , wherein R 3 is hydrogen, C 1 -C 6 alkyl, aryl, arylC 1 -C 6 -alkyl, hetaryl or hetarylalkyl, wherein the alkyl, cycloalkyl, aryl, hetaryl and hetarylalkyl groups independently are optionally substituted with one or more of R 7 wherein R 7 .
97 . A compound according to claim 92 , wherein R 4 is hydrogen, C 1 -C 8 alkyl, aryl, hetaryl, hetarylC 1 -C 6 alkyl, arylC 1 -C 6 alkyl, wherein the alkyl, aryl, hetaryl, groups independently are optionally substituted with one or more of R 7 wherein R 7 .
98 . A compound according to claim 92 , wherein R 5 and R 6 are together with the nitrogen to which they are attached, forming a saturated or partially saturated cyclic, bicyclic or tricyclic ring system containing from 6 to 10 carbon atoms and from 0 to 2 additional heteroatoms selected from nitrogen, oxygen or sulphur, the ring system optionally being substituted with at least one of C 1 -C 6 alkyl, aryl, hetaryl, arylC 1 -C 6 alkyl, hetarylalkyl, hydroxy, oxo, cyano, C 1 -C 6 alkyloxy, arylC 1 -C 6 alkyloxy, hetarylC 1 -C 6 alkyloxy, C 1 -C 6 alkyloxyC 1 -C 6 alkyl, C 1 -C 6 alkylcarbonyl, arylcarbonyl, hetarylcarbonyl, arylC 1 -C 6 alkylcarbonyl, hetarylC 1 -C 6 alkylcarbonyl, C 1 -C 6 alkylcarboxy, arylcarboxy or arylC 1 -C 6 alkylcarboxy wherein the alkyl and aryl groups independently are optionally substituted with one or more of R 7 .
99 . A compound according to claim 92 , which is selected from:
(4-Methyl-2-phenyl-thiazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (2,4-Dimethyl-thiazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and (4-Methyl-2-pyrazin-2-yl-thiazol-5-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, a prodrug thereof, or tautomeric forms thereof.
100 . A compound according to claim 92 , selected from the group consisting of:
[4-Methyl-2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Aza-bicyclo[3.2.2]non-3-yl)-(2,4-dimethyl-thiazol-5-yl)-methanone; (1H-Imidazol-4-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; (3-Aza-bicyclo[3.2.2]non-3-yl)-(4-methyl-2-phenyl-thiazol-5-yl)-methanone; 2,4-Dimethyl-thiazole-5-carboxylic acid cycloheptylamide; Azepan-1-yl-(2,4-dimethyl-thiazol-5-yl)-methanone; 2,4-Dimethyl-thiazole-5-carboxylic acid adamantan-1-ylamide; (3-Aza-bicyclo[3.2.2]non-3-yl)-(1H-imidazol-4-yl)-methanone; 2,4-Dimethyl-thiazole-5-carboxylic acid (3-hydroxy-adamantan-1-yl)-amide; (1-Methyl-1H-imidazol-4-yl)-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; [1-(6-Methyl-pyridin-2-yl)-1H-imidazol-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; and [1-(4-Chloro-benzyl)-5-methyl-1H-imidazol-4-yl]-(1,3,3-trimethyl-6-aza-bicyclo[3.2.1]oct-6-yl)-methanone; or a salt thereof with a pharmaceutically acceptable acid or base, or optical isomer or mixture of optical isomers, racemic mixture, or tautomeric forms thereof.
101 . A compound according to any one of claims 28 , 38 , 39 , 48 , 49 , 50 , 51 , 55 , 56 , 57 , 58 , 67 , 68 , 69 , 70 , 81 , 82 , 83 , 90 , 91 , 92 , 99 or 100 , which is an agent useful for the treatment, prevention and/or prophylaxis of any conditions, disorders and diseases wherein a modulation or an inhibition of the activity of 11βHSD1 is beneficial.
102 . A compound according to any one of claims 28 , 38 , 39 , 48 , 49 , 50 , 51 , 55 , 56 , 57 , 58 , 67 , 68 , 69 , 70 , 81 , 82 , 83 , 90 , 91 , 92 , 99 or 100 , which is an agent useful for the treatment, prevention and/or prophylaxis of any conditions, disorders and diseases that are influenced by intracellular glucocorticoid levels.
103 . A compound according to claim 101 or 102 , which is an agent useful for the treatment, prevention and/or prophylaxis of conditions, disorders or diseases selected from the group consisting of the metabolic syndrome, insulin resistance, dyslipidemia, hypertension and obesity.
104 . A compound according to claim 101 or 102 , which is an agent useful for the treatment, prevention and/or prophylaxis of type 2 diabetes, impaired glucose tolerance (IGT), impaired fasting glucose (IFG).
105 . A compound according to claim 101 or 102 , which is an agent useful for the delaying or prevention of the progression from IGT into type 2 diabetes.
106 . A compound according to claim 101 or 102 , which is an agent useful for delaying or prevention of the progression of the metabolic syndrome into type 2 diabetes.
107 . A compound according to claim 101 or 102 , which is an agent useful for the treatment, prevention and/or prophylaxis of adverse effects of glucocorticoid receptor agonist treatment or therapy.
108 . A pharmaceutical composition comprising, as an active ingredient, at least one compound according to any one of claims 28 , 38 , 39 , 48 , 49 , 50 , 51 , 55 , 56 , 57 , 58 , 67 , 68 , 69 , 70 , 81 , 82 , 83 , 90 , 91 , 92 , 99 or 100 , together with one or more pharmaceutically acceptable carriers or excipients.
109 . The pharmaceutical composition according to claim 108 which is for oral, nasal, buccal, transdermal, pulmonal or parenteral administration.
110 . The pharmaceutical composition according to claim 108 or 109 , in unit dosage form, comprising from 0.05 mg to 2000 mg/day, from 0.1 mg to 1000 mg or from 0.5 mg to 500 mg per day of the compound.
111 . A method for the treatment, prevention and/or prophylaxis of any conditions, disorders or diseases wherein a modulation or an inhibition of the activity of 11βHSD1 is beneficial, the method comprising administering to a subject in need thereof an effective amount of a compound according to any one of claims 28 , 38 , 39 , 48 , 49 , 50 , 51 , 55 , 56 , 57 , 58 , 67 , 68 , 69 , 70 , 81 , 82 , 83 , 90 , 91 , 92 , 99 or 100 .
112 . The method according to claim 111 , wherein the conditions, disorders or diseases are selected from the group consisting of the metabolic syndrome, insulin resistance, dyslipidemia, hypertension and obesity.Cited by (0)
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