US2004192728A1PendingUtilityA1
Quinoline-derived amide modulators of vanilloid VR1 receptor
Priority: Feb 3, 2003Filed: Feb 2, 2004Published: Sep 30, 2004
Est. expiryFeb 3, 2023(expired)· nominal 20-yr term from priority
A61P 37/08A61P 43/00A61P 9/00A61P 31/00A61P 35/00A61P 25/00A61P 25/02A61P 25/06A61P 29/00C07D 491/10A61P 17/00C07D 401/12A61P 13/02A61P 13/10C07D 405/12A61P 19/02A61P 11/14A61P 1/18A61P 17/02A61P 1/00C07D 409/12A61P 1/04C07D 215/38A61P 19/08C07D 215/60A61P 11/06A61P 11/00A61P 1/16A61P 11/04A61P 13/08
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Claims
Abstract
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
Claims
exact text as granted — not AI-modified1 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 0, 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is a direct bond or C 1-4 alkyldiyl optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, halogen, C 1-8 alkanyloxy, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl and cyclohexyl;
R 4 is independently selected from the group consisting of C 1-12 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 1-6 fluorinated alkanyl and —N(R 5 )(R 6 ); or when n is 2 or 3, optionally two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl;
wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 1, 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
2 . The compound according to claim 1 wherein L is a direct bond.
3 . The compound according to claim 1 wherein L is C 1-4 alkyldiyl.
4 . The compound according to claim 1 wherein R 3 is phenyl.
5 . The compound according to claim 1 wherein R 3 is pyridyl.
6 . The compound according to claim 1 wherein R 3 is thienyl.
7 . The compound according to claim 1 wherein n is 1.
8 . The compound according to claim 1 wherein n is 2 or 3 and R 4 is C 1-12 alkanyl.
9 . The compound according to claim 1 wherein R 4 is —N(R 5 )(R 6 ).
10 . The compound according to claim 9 wherein R 5 and R 6 are different.
11 . The compound according to claim 1 wherein L is Cl-4alkyldiyl, R 3 is phenyl, n is 1 and R 4 is C 1-12 alkanyl.
12 . The compound according to claim 1 wherein R 3 is phenyl, n is 1 and R 4 is —N(R 5 )(R 6 ).
13 . The compound according to claim 1 wherein R 3 is phenyl, n is 2 or 3, and two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkyl.
14 . The compound according to claim 1 wherein Z is O.
15 . The compound according to claim 1 wherein m is 0.
16 . The compound according to claim 1 wherein R 2 is hydrogen.
17 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 0, 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is a C 1-4 alkyldiyl optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, halogen, C 1-8 alkanyloxy, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl and cyclohexyl;
R 4 is independently selected from the group consisting of C 1-12 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 1-6 fluorinated alkanyl, and —N(R 5 )(R 6 ); or when n is 2 or 3, optionally two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl;
wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 1, 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
18 . The compound according to claim 17 wherein R 3 is phenyl.
19 . The compound according to claim 17 wherein R 3 is pyridyl.
20 . The compound according to claim 17 wherein R 3 is thienyl.
21 . The compound according to claim 17 wherein n is 1.
22 . The compound according to claim 17 wherein n is 2 or 3 and R 4 is C 1-12 alkanyl.
23 . The compound according to claim 17 wherein R 4 is —N(R 5 )(R 6 ).
24 . The compound according to claim 23 wherein R 5 and R 6 are different.
25 . The compound according to claim 17 wherein L is C 1-4 alkyldiyl, R 3 is phenyl, n is 1 and R 4 is C- 1-12 alkanyl.
26 . The compound according to claim 17 wherein R 3 is phenyl, n is 1 and R 4 is —N(R 5 )(R 6 ).
27 . The compound according to claim 17 wherein R 3 is phenyl, n is 2 or 3, and two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkyl.
28 . The compound according to claim 17 wherein Z is O.
29 . The compound according to claim 17 wherein m is 0.
30 . The compound according to claim 17 wherein R 2 is hydrogen.
31 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 0, 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is a direct bond or C 1-4 alkyldiyl optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, halogen, C 1-8 alkanyloxy, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl and cyclohexyl;
R 4 is independently selected from the group consisting of C 1-8 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 1-6 fluorinated alkanyl, and —N(R 5 )(R 6 ); or both R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl;
wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
32 . The compound according to claim 31 wherein L is a direct bond.
33 . The compound according to claim 31 wherein L is C 1-4 alkyldiyl.
34 . The compound according to claim 31 wherein R 3 is phenyl.
35 . The compound according to claim 31 wherein R 3 is pyridyl.
36 . The compound according to claim 31 wherein R 3 is thienyl.
37 . The compound according to claim 31 wherein R 4 is C 1-12 alkanyl.
38 . The compound according to claim 31 wherein R 4 is —N(R 5 )(R 6 ).
39 . The compound according to claim 38 wherein R 5 and R 6 are different.
40 . The compound according to claim 31 wherein L is C 1-4 alkyldiyl, R 3 is phenyl, and one R 4 is C 1-12 alkanyl.
41 . The compound according to claim 31 wherein R 3 is phenyl, and one R 4 is —N(R 5 )(R 6 ).
42 . The compound according to claim 31 wherein R 3 is phenyl and two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkyl.
43 . The compound according to claim 31 wherein Z is O.
44 . The compound according to claim 31 wherein m is 0.
45 . The compound according to claim 31 wherein R 2 is hydrogen.
46 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is a direct bond or C 1-4 alkyldiyl optionally substituted with a substituent selected from the group consisting of C 1-8 alkanyl, C 3-8 cycloalkanyl and phenyl optionally substituted with one to three substituents independently selected from the group consisting of C 1-8 alkanyl, halogen, C 1-8 alkanyloxy, hydroxy, fluorinated alkanyl, fluorinated alkanyloxy, amino, di(C 1-3 )alkanylamino, and C 1-3 alkanylamino;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl and cyclohexyl;
R 4 is independently selected from the group consisting of C 1-8 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 16 fluorinated alkanyl, and —N(R 5 )(R 6 ); or both R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl;
wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 1, 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
47 . The compound according to claim 46 wherein L is a direct bond.
48 . The compound according to claim 46 wherein L is C 1-4 alkyldiyl.
49 . The compound according to claim 46 wherein R 3 is phenyl.
50 . The compound according to claim 46 wherein R 3 is pyridyl.
51 . The compound according to claim 46 wherein R 3 is thienyl.
52 . The compound according to claim 46 wherein R 4 is C 1-12 alkanyl.
53 . The compound according to claim 46 wherein R 4 is —N(R 5 )(R 6 ).
54 . The compound according to claim 46 wherein R 5 and R 6 are different.
55 . The compound according to claim 46 wherein L is C 1-4 alkyldiyl, R 3 is phenyl, and one R 4 is C 1-12 alkanyl.
56 . The compound according to claim 46 wherein R 3 is phenyl, and one R 4 is —N(R 5 )(R 6 ).
57 . The compound according to claim 46 wherein R 3 is phenyl and two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkyl.
58 . The compound according to claim 46 wherein Z is O.
59 . The compound according to claim 46 wherein m is 0.
60 . The compound according to claim 46 wherein R 2 is hydrogen.
61 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 0, 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is ethen-1,2-diyl;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl and cyclohexyl;
R 4 is independently selected from the group consisting of C 1-12 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 1-6 fluorinated alkanyl, halogen, and —N(R 5 )(R 6 ); or when n is 2 or 3, optionally two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl;
wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 1, 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
62 . The compound according to claim 61 wherein R 3 is phenyl.
63 . The compound according to claim 61 wherein R 3 is pyridyl.
64 . The compound according to claim 61 wherein R 3 is thienyl.
65 . The compound according to claim 61 wherein n is 1.
66 . The compound according to claim 61 wherein n is 2 or 3 and R 4 is C 1-12 alkanyl.
67 . The compound according to claim 61 wherein n is 2, one R 4 is halogen, and the other R 4 is C 1-6 fluorinated alkanyl.
68 . The compound according to claim 61 wherein R 4 is C 1-6 fluorinated alkanyl.
69 . The compound according to claim 61 R 4 is halogen.
70 . The compound according to claim 61 wherein R 4 is —N(R 5 )(R 6 ).
71 . The compound according to claim 67 wherein R 5 and R 6 are different.
72 . The compound according to claim 61 wherein L is C 1-4 alkyldiyl, R 3 is phenyl, n is 1 and R 4 is C 1-12 alkanyl.
73 . The compound according to claim 61 wherein R 3 is phenyl, n is 1 and R 4 is —N(R 5 )(R 6 ).
74 . The compound according to claim 61 wherein R 3 is phenyl, n is 2 or 3, and two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkyl.
75 . The compound according to claim 61 wherein Z is O.
76 . The compound according to claim 61 wherein m is 0.
77 . The compound according to claim 61 wherein R 2 is hydrogen.
78 . A compound of Formula (I):
wherein:
R 1 is a substituent independently selected from the group consisting of hydrogen; hydroxy; halogen; C 1-8 alkanyl optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 1-8 alkanyloxy optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; fluorinated alkanyloxy; fluorinated alkanyl; C 1-8 alkanylthio optionally substituted with one or more substituents independently selected from the group consisting of halogen, fluorinated alkanyl and C 1-8 alkanyloxy; C 3-8 cycloalkanyl; C 3-8 cycloalkanyloxy; nitro; amino; C 1-8 alkanylamino; C 1-8 dialkanylamino; C 3-8 cycloalkanylamino; cyano; carboxy; C 1-7 alkanyloxycarbonyl; C 1-7 alkanylcarbonyloxy; C 1-7 alkanylaminocarbonyl; C 1-7 alkanylcarbonylamino; diC 1-7 alkanylaminocarbonyl; and formyl; wherein the heteroatom contained in the quinoline ring of Formula (I) is optionally substituted with an oxo substituent;
m is 0, 1 or 2;
R 2 is hydrogen or C 1-8 alkanyl;
L is a direct bond;
R 3 is selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, and cyclohexyl;
R 4 is selected from the group consisting of C 1-12 alkanyl, C 4-8 alkanyloxy, C 3-8 cycloalkanyloxy, C 1-8 alkanylamino, C 3-8 cycloalkanylamino, C 3-14 cyclic heteroalkanyl, C 1-6 fluorinated alkanyl, and —N(R 5 )(R 6 ), wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 is optionally substituted with thienyl or phenyl; or when n is 2 or 3, optionally two R 4 substituents taken together form a C 3-14 cyclic heteroalkyl or C 3-14 cyclic alkanyl;
R 5 is hydrogen, C 1-16 alkyl, alkanylcarbonyl or arylcarbonyl;
R 6 is C 4-16 alkyl, alkanylcarbonyl, C 1-3 alkyl substituted with a substituent selected from the group consisting of pyrrolyl, pyridyl, furyl, thienyl, phenyl, and furyl, or arylcarbonyl; or optionally R 6 and one of R 4 taken together form a saturated or partially unsaturated cyclic heteroalkyl or a heteroaryl; or R 5 and R 6 optionally taken together form a bridged or non-bridged cyclic heteroalkanyl, wherein said heteroalkanyl is optionally substituted with C 1-6 alkanylcarbonyl; wherein the alkanyls in any of the foregoing alkanyl-containing substituents of R 4 , R 5 or R 6 are optionally and independently substituted with pyrrolyl, pyridyl, furyl, thienyl, phenyl, furyl, C 1-4 alkylpyrrolyl, C 1-4 alkylpyridyl, C 1-4 alkylthienyl, C 1-4 alkylphenyl, or C 1-4 alkylfuryl;
n is 1, 2 or 3;
Z is O or S; and
enantiomers, diastereomers, tautomers, solvates, and pharmaceutically acceptable salts thereof.
79 . The compound according to claim 78 wherein L is a direct bond.
80 . The compound according to claim 78 wherein R 3 is pyridyl.
81 . The compound according to claim 78 wherein R 3 is thienyl.
82 . The compound according to claim 78 wherein R 3 is furyl.
83 . The compound according to claim 78 wherein R 3 is cyclohexyl.
84 . The compound according to claim 78 wherein n is 1.
85 . The compound according to claim 78 wherein n is 2 or 3 and R 4 is C 1-12 alkanyl.
86 . The compound according to claim 78 wherein R 4 is —N(R 5 )(R 6 ).
87 . The compound according to claim 86 wherein R 5 and R 6 are different.
88 . The compound according to claim 78 wherein Z is O.
89 . The compound according to claim 78 wherein m is 0.
90 . The compound according to claim 78 wherein R 2 is hydrogen.
91 . A compound selected from the group consisting of
1-Acetyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Benzoyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Butyryl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexanecarbonyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Isopropyl-2-trifluoromethyl-1H-benzoimidazole-5-carboxylic acid quinolin-3-ylamide; 1-Methyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid quinolin-3-ylamide; 1-Methyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Pentyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid quinolin-3-ylamide; 1-Pentyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Pentyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Propyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 2-(4-Dipentylamino-phenyl)-N-quinolin-3-yl-acetamide; 2-(4-Pentyl-phenyl)-N-quinolin-3-yl-acetamide; 2-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acetamide; 2-(Heptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 2-(Methyl-pentyl-amino)-N-quinolin-3-yl-benzamide; 2,3-Dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 2-{4-(Methyl-pentyl-amino)-phenyl}-N-quinolin-3-yl-acetamide; 2-Chloro-4-(cyclohexylmethyl-amino)-N-quinolin-3-yl-benzamide; 2-Chloro-4-pentylamino-N-quinolin-3-yl-benzamide; 2-Heptylamino-N-quinolin-3-yl-benzamide; 2-Pentylamino-N-quinolin-3-yl-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-propionamide; 3-(1-Cyclohexylmethyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-propionamide; 3-(1-Propyl-1H-indol-5-yl)-N-quinolin-3-yl-propionamide, 3-(1-Propyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-propionamide; 3-(2,2-Dimethyl-chroman-6-yl)-N-quinolin-3-yl-acrylamide; 3-(2,2-Dimethyl-chroman-6-yl)-N-quinolin-3-yl-propionamide; 3-(4-Azepan-1-yl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-Azepan-1-yl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-Cyclohexylmethyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-Dipentylamino-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-Pentyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-Pentyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-sec-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-benzamide; 3-(Heptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 3-(Methyl-pentyl-amino)-N-quinolin-3-yl-benzamide; 3,4,5,6-Tetrahydro-2H-[1,2′]bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 3,4,5,6-Tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 3-[4-(Methyl-phenethyl-amino)-phenyl]-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-3-phenyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-phenyl}-N-quinolin-3-yl; 3-{4-(1,1-Dimethyl-propyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Cyclohexyl-1-methyl-ethyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Methyl-pentyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Methyl-pentyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(Benzyl-methyl-amino)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(Cyclohexyl-methyl-amino)-phenyl}-N-quinolin-3-yl-acrylamide; 3-{4-(Cyclohexyl-methyl-amino)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(Cyclohexyl methyl-methyl-amino)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(Methyl-pentyl-amino)-phenyl}-N-quinolin-3-yl-acrylamide; 3-{4-(Methyl-pentyl-amino)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(Methyl-propyl-amino)-phenyl}-N-quinolin-3-yl-propionamide; 3-{5-(1,1-Dimethyl-propyl)-thiophen-2-yl}-N-quinolin-3-yl-propionamide; 3-Cyclohexylamino-N-quinolin-3-yl-benzamide; 3-Dipentylamino-N-quinolin-3-yl-benzamide; 3-Heptylamino-N-quinolin-3-yl-benzamide; 3-Indan-5-yl-N-quinolin-3-yl-propionamide; 3-Methyl-4-(methyl-pentyl-amino)-N-quinolin-3-yl-benzamide; 3-Methyl-4-pentylamino-N-quinolin-3-yl-benzamide; 3-Pentylamino-N-quinolin-3-yl-benzamide; 4-(1,3-Dihydro-isoindol-2-yl)-N-quinolin-3-yl-benzamide; 4-(1,4-Dioxa-8-aza-spiro[4.5]dec-8-yl)-N-quinolin-3-yl-benzamide; 4-(2,6-Dimethyl-morpholin-4-yl)-N-quinolin-3-yl-benzamide; 4-(3,5-Dimethyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-benzamide; 4-(3-Methyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(4-Benzoyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(4-Benzyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(4-Phenylacetyl-piperazin-1-yl)-N-quinolin-3-yl-benzamide; 4-(4-Phenyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(4-Propyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(Acetyl-cyclohexyl-amino)-N-quinolin-3-yl-benzamide; 4-(Benzyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Benzyl-pentyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cycloheptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexanecarbonyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-ethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl methyl-amino)-3-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-3-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-N-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl methyl-methyl-amino)-3-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl methyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexylmethyl-phenethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-propyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclopentyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Dec-4-enyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Hept-4-enyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Heptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-butyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-hexyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-non-6-enyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-nonyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-pentyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-phenethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-propyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-tetradecyl-amino)-N-quinolin-3-yl-benzamide; 4-(Octyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Phenethyl-propyl-amino)-N-quinolin-3-yl-benzamide; 4-[1,4′]Bipiperidinyl-1′-yl-N-quinolin-3-yl-benzamide; 4-{(3,3-Dimethyl-butyl)-methyl-amino}-N-quinolin-3-yl-benzamide; 4-{4-(1,1-Dimethyl-pentyl)-phenyl}-but-3-enoic acid quinolin-3-ylamide; 4-{4-(1,1-Dimethyl-pentyl)-phenyl}-N-quinolin-3-yl-butyramide; 4-{4-(1,1-Dimethyl-propyl)-phenyl}-but-3-enoic acid quinolin-3-ylamide; 4-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-butyramide; 4-{Methyl-(3-methyl-butyl)-amino}-N-quinolin-3-yl-benzamide; 4-{Methyl-(3-phenyl-allyl)-amino}-N-quinolin-3-yl-benzamide; 4-{Methyl-(3-phenyl-propyl)-amino}-N-quinolin-3-yl-benzamide; 4-{Methyl-(tetrahydro-pyran4-yl)-amino}-N-quinolin-3-yl-benzamide; 4-{Methyl-{3-(5-methyl-furan-2-yl)-butyl}-amino}-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azocan-1-yl-N-quinolin-3-yl-benzamide; 4-Azonan-1-yl-N-quinolin-3-yl-benzamide; 4-Benzyl-3,4,5,6-tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 4-Butoxy-N-quinolin-3-yl-benzamide; 4-Butyl-cyclohexanecarboxylic acid quinolin-3-ylamide; 4-Butyl-cyclohexanecarboxylic acid quinolin-3-ylamide; 4-Cycloheptylamino-N-quinolin-3-yl-benzamide; 4-Cyclohexylamino-N-methyl-N-quinolin-3-yl-benzamide; 4-Cyclohexylamino-N-quinolin-3-yl-benzamide; 4-Cyclopentylamino-N-quinolin-3-yl-benzamide; 4-Dibenzylamino-N-quinolin-3-yl-benzamide; 4-Dibutylamino-N-quinolin-3-yl-benzamide; 4-Dihexylamino-N-quinolin-3-yl-benzamide; 4-Dipentylamino-N-quinolin-3-yl-benzamide; 4-Dipropylamino-N-quinolin-3-yl-benzamide; 4-Morpholin-4-yl-N-quinolin-3-yl-benzamide; 4-Pentylamino-N-quinolin-3-yl-benzamide; 4-Phenethylamino-N-quinolin-3-yl-benzamide; 4-Piperazin-1-yl-N-quinolin-3-yl-benzamide; 4-Piperidin-1-yl-N-quinolin-3-yl-benzamide; 4-Propyl-3,4,5,6-tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 4-Pyrrolidin-1-yl-N-quinolin-3-yl-benzamide; 4-tert-Butyl-cyclohexanecarboxylic acid quinolin-3-ylamide; 4-tert-Butyl-cyclohexanecarboxylic acid quinolin-3-ylamide; 5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carboxylic acid quinolin-3-ylamide; 5,6,7,8-Tetrahydro-naphthalene-2-carboxylic acid quinolin-3-ylamide; 5-Chloro-1H-indole-2-carboxylic acid quinolin-3-ylamide; 5-Pentyl-thiophene-2-carboxylic acid quinolin-3-ylamide; 6-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-nicotinamide; 6-(Benzyl-methyl-amino)-N-quinolin-3-yl-nicotinamide; 6-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-nicotinamide; 6-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-nicotinamide; 6-(Heptyl-methyl-amino)-N-quinolin-3-yl-nicotinamide; 6-(Methyl-pentyl-amino)-N-quinolin-3-yl-nicotinamide; 6-(Methyl-phenethyl-amino)-N-quinolin-3-yl-nicotinamide; 6-Azepan-1-yl-N-quinolin-3-yl-nicotinamide; 6-Azocan-1-yl-N-quinolin-3-yl-nicotinamide; 6-Cyclohexylamino-N-quinolin-3-yl-nicotinamide; 6-Pentylamino-N-quinolin-3-yl-nicotinamide; cis-4-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-benzamide; cis-6-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-nicotinamide; N-Quinolin-3-yl-3-(3-trifluoromethyl-phenyl)-acrylamide; N-Quinolin-3-yl-3-(4-tricyclo{5.3.1.13,9}dodec-1-yl-phenyl)-propionamide; N-Quinolin-3-yl-3-(4-trifluoromethyl-phenyl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propionamide; N-Quinolin-3-yl-3-(5,6,7,8-tetrahydro-naphthalen-2-yl)-propionamide; N-Quinolin-3-yl-4-(tetrahydro-pyran4-ylamino)-benzamide; N-Quinolin-3-yl-4-thiomorpholin-4-yl-benzamide; R-4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; S4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; trans-4-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-benzamide; trans-6-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-nicotinamide; 4-tert-Butyl-N-(4-hydroxy-quinolin-3-yl)-benzamide; 3-(4-tert-Butyl-phenyl)-N-(4-hydroxy-quinolin-3-yl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; N-(2-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; 4-tert-Butyl-N-(2-methoxy-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(4-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(2-chloro-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(2-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(4-chloro-quinolin-3-yl)-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-2,3-dihydro-1H-indol-5-yl)-acrylamide; 3-(1-Cyclohexyl-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (4-chloro-quinolin-3-yl)-amide; 1-Cyclohexyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 4-(Cyclohexyl-methyl-amino)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(5-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(5-fluoro-quinolin-3-yl)-benzamide; 3-Phenyl-propynoic acid quinolin-3-ylamide; trans-2-Phenyl-cyclopropanecarboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-propynoic acid quinolin-3-ylamide; and 2-(4-tert-Butyl-phenyl)-cyclopropanecarboxylic acid quinolin-3-ylamide.
92 . A compound selected from the group consisting of
1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Pentyl-1,2,3,4-tetrahydro-quinoline-6-carboxylic acid quinolin-3-ylamide; 1-Pentyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Propyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 3-(4-sec-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3,4,5,6-Tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 3-{4-(1,1-Dimethyl-3-phenyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-phenyl}-N-quinolin-3-yl; 3-{4-(1,1-Dimethyl-propyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Cyclohexyl-1-methyl-ethyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Methyl-pentyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{5-(1,1-Dimethyl-propyl)-thiophen-2-yl}-N-quinolin-3-yl-propionamide; 4-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-benzamide; 4-(4-Benzyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(Cycloheptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-ethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-3-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexylmethyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclopentyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Dec-4-enyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Hept-4-enyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Heptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-non-6-enyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-nonyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-phenethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Octyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-{(3,3-Dimethyl-butyl)-methyl-amino}-N-quinolin-3-yl-benzamide; 4-{Methyl-{3-(5-methyl-furan-2-yl)-butyl}-amino}-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azocan-1-yl-N-quinolin-3-yl-benzamide; 4-Azonan-1-yl-N-quinolin-3-yl-benzamide; 4-Benzyl-3,4,5,6-tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carboxylic acid quinolin-3-ylamide; 6-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-nicotinamide; 6-Azocan-1-yl-N-quinolin-3-yl-nicotinamide; cis-4-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-benzamide; cis-6-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-nicotinamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propionamide; R-4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; S4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; trans-4-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-benzamide; trans-6-(Octahydro-isoquinolin-2-yl)-N-quinolin-3-yl-nicotinamide; 4-tert-Butyl-N-(4-hydroxy-quinolin-3-yl)-benzamide; 3-(4-tert-Butyl-phenyl)-N-(4-hydroxy-quinolin-3-yl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; N-(2-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; 4-tert-Butyl-N-(2-methoxy-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(4-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(2-chloro-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(2-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(4-chloro-quinolin-3-yl)-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-2,3-dihydro-1H-indol-5-yl)-acrylamide; 3-(1-Cyclohexyl-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (4-chloro-quinolin-3-yl)-amide; 1-Cyclohexyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 4-(Cyclohexyl-methyl-amino)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(5-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(5-fluoro-quinolin-3-yl)-benzamide; 3-Phenyl-propynoic acid quinolin-3-ylamide; trans-2-Phenyl-cyclopropanecarboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-propynoic acid quinolin-3-ylamide; and 2-(4-tert-Butyl-phenyl)-cyclopropanecarboxylic acid quinolin-3-ylamide.
93 . A compound selected from the group consisting of
1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Pentyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Propyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 3-(4-sec-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3,4,5,6-Tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 3-{4-(1,1-Dimethyl-3-phenyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Methyl-pentyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{5-(1,1-Dimethyl-propyl)-thiophen-2-yl}-N-quinolin-3-yl-propionamide; 4-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-benzamide; 4-(4-Benzyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(Cycloheptyl-methyl-amino)-N-quinolin-3-yl-benzamide;; 4-(Cyclohexyl-ethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-3-methyl-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexylmethyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclopentyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Dec4-enyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Heptyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-nonyl-amino)-N-quinolin-3-yl-benzamide; 4-(Methyl-phenethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Octyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-{(3,3-Dimethyl-butyl)-methyl-amino}-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azocan-1-yl-N-quinolin-3-yl-benzamide; 4-Azonan-1-yl-N-quinolin-3-yl-benzamide; 4-Benzyl-3,4,5,6-tetrahydro-2H-{1,2′}bipyridinyl-5′-carboxylic acid quinolin-3-ylamide; 6-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-nicotinamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propionamide; R 4 -{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; S-4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; 4-tert-Butyl-N-(4-hydroxy-quinolin-3-yl)-benzamide; 3-(4-tert-Butyl-phenyl)-N-(4-hydroxy-quinolin-3-yl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; N-(2-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; 4-tert-Butyl-N-(2-methoxy-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(4-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(2-chloro-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(2-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(4-chloro-quinolin-3-yl)-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-2,3-dihydro-1H-indol-5-yl)-acrylamide; 3-(1-Cyclohexyl-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (4-chloro-quinolin-3-yl)-amide; 1-Cyclohexyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 4-(Cyclohexyl-methyl-amino)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(5-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(5-fluoro-quinolin-3-yl)-benzamide; 3-Phenyl-propynoic acid quinolin-3-ylamide; trans-2-Phenyl-cyclopropanecarboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-propynoic acid quinolin-3-ylamide; and 2-(4-tert-Butyl-phenyl)-cyclopropanecarboxylic acid quinolin-3-ylamide.
94 . A compound selected from the group consisting of
1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Propyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 3-(4-sec-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-3-phenyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-pentyl)-2,6-dimethoxy-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{4-(1-Methyl-pentyl)-phenyl}-N-quinolin-3-yl-propionamide; 3-{5-(1,1-Dimethyl-propyl)-thiophen-2-yl}-N-quinolin-3-yl-propionamide; 4-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-benzamide; 4-(4-Benzyl-piperidin-1-yl)-N-quinolin-3-yl-benzamide; 4-(Cycloheptyl-methyl-amino)-N-quinolin-3-yl-benzamide;; 4-(Cyclohexyl-ethyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Cyclohexylmethyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-(Octyl-methyl-amino)-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 4-Azocan-1-yl-N-quinolin-3-yl-benzamide; 4-Azonan-1-yl-N-quinolin-3-yl-benzamide; 6-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-nicotinamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propionamide; R-4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; S4-{(3,7-Dimethyl-oct-6-enyl)-methyl-amino}-N-quinolin-3-yl-benzamide; 5 4-tert-Butyl-N-(4-hydroxy-quinolin-3-yl)-benzamide; 3-(4-tert-Butyl-phenyl)-N-(4-hydroxy-quinolin-3-yl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; N-(2-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; 4-tert-Butyl-N-(2-methoxy-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(4-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(2-chloro-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(2-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(4-chloro-quinolin-3-yl)-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-2,3-dihydro-1H-indol-5-yl)-acrylamide; 3-(1-Cyclohexyl-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (4-chloro-quinolin-3-yl)-amide; 1-Cyclohexyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 4-(Cyclohexyl-methyl-amino)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(5-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(5-fluoro-quinolin-3-yl)-benzamide; 3-Phenyl-propynoic acid quinolin-3-ylamide; trans-2-Phenyl-cyclopropanecarboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-propynoic acid quinolin-3-ylamide; and 2-(4-tert-Butyl-phenyl)-cyclopropanecarboxylic acid quinolin-3-ylamide.
95 . A compound selected from the group consisting of
1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-acrylamide; 3-(4-tert-Butyl-phenyl)-N-quinolin-3-yl-propionamide; 3-{4-(1,1-Dimethyl-propyl)-phenyl}-N-quinolin-3-yl-propionamide; 4-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-benzamide; 4-Azepan-1-yl-N-quinolin-3-yl-benzamide; 6-(3-Aza-bicyclo{3.3.1}non-3-yl)-N-quinolin-3-yl-nicotinamide; 4-tert-Butyl-N-(4-hydroxy-quinolin-3-yl)-benzamide; 3-(4-tert-Butyl-phenyl)-N-(4-hydroxy-quinolin-3-yl)-acrylamide; N-Quinolin-3-yl-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-acrylamide; N-(4-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; N-(2-Chloro-quinolin-3-yl)-4-(cyclohexyl-methyl-amino)-benzamide; 4-tert-Butyl-N-(2-methoxy-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(4-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(2-chloro-quinolin-3-yl)-benzamide; 4-Azepan-1-yl-N-(2-chloro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(4-chloro-quinolin-3-yl)-benzamide; 3-(1-Cyclohexyl-2,3-dihydro-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; 1-Cyclohexyl-2,3-dihydro-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-2,3-dihydro-1H-indol-5-yl)-acrylamide; 3-(1-Cyclohexyl-1H-indol-5-yl)-N-quinolin-3-yl-acrylamide; N-(4-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (4-chloro-quinolin-3-yl)-amide; 1-Cyclohexyl-1H-indole-5-carboxylic acid quinolin-3-ylamide; 1-Cyclohexyl-1H-indole-5-carboxylic acid (2-chloro-quinolin-3-yl)-amide; N-(2-Chloro-quinolin-3-yl)-3-(1-cyclohexyl-1H-indol-5-yl)-acrylamide; 4-(Cyclohexyl-methyl-amino)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(8-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(6-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-(Cyclohexyl-methyl-amino)-N-(7-trifluoromethyl-quinolin-3-yl)-benzamide; 4-Azocan-1-yl-N-(5-fluoro-quinolin-3-yl)-benzamide; 4-(3-Aza-bicyclo[3.2.2]non-3-yl)-N-(5-fluoro-quinolin-3-yl)-benzamide; 3-Phenyl-propynoic acid quinolin-3-ylamide; trans-2-Phenyl-cyclopropanecarboxylic acid quinolin-3-ylamide; 3-(4-tert-Butyl-phenyl)-propynoic acid quinolin-3-ylamide; and 2-(4-tert-Butyl-phenyl)-cyclopropanecarboxylic acid quinolin-3-ylamide.
96 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 1 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
97 . A veterinary composition comprising a compound, salt or solvate according to claim 1 admixed with a veterinarily acceptable carrier, excipient or dilluent.
98 . A method of treating or preventing a disease or condition in a mammal which disease or condition is affected by the modulation of one or more vanilloid receptors, which method comprises administering to a mammal in need of such treatment or prevention a therapeutically effective amount of a compound, salt or solvate of claim 1 .
99 . A method for preventing or treating a chronic-pain causing disease or condition, an acute-pain causing disease or condition, or a pulmonary dysfunction comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 1 .
100 . A method for preventing or treating a disease or condition, wherein said disease or condition causes inflammatory pain, burning pain, itch urinary incontinence, or chronic obstructive pulmonary disease, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 1 .
101 . A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 1 .
102 . The method of claim 101 wherein the disease or condition is ulcerative colitis.
103 . The method of claim 101 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
104 . The method of claim 101 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
105 . The method of claim 101 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
106 . A kit comprising in one or more containers an amount of the composition of claim 1 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma.
107 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 17 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
108 . A veterinary composition comprising a compound, salt or solvate according to claim 17 admixed with a veterinarily acceptable carrier, excipient or dilluent.
109 . A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 17 .
110 . The method of claim 109 wherein the disease or condition is ulcerative colitis.
111 . The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
112 . The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
113 . The method of claim 109 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
114 . A kit comprising in one or more containers an amount of the composition of claim 17 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma.
115 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 31 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
116 . A veterinary composition comprising a compound, salt or solvate according to claim 31 admixed with a veterinarily acceptable carrier, excipient or dilluent.
117 . A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 31 .
118 . The method of claim 117 wherein the disease or condition is ulcerative colitis.
119 . The method of claim 117 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
120 . The method of claim 117 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
121 . The method of claim 117 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
122 . A kit comprising in one or more containers an amount of the composition of claim 31 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma.
123 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 61 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
124 . A veterinary composition comprising a compound, salt or solvate according to claim 61 admixed with a veterinarily acceptable carrier, excipient or dilluent.
125 . A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 61 .
126 . The method of claim 125 wherein the disease or condition is ulcerative colitis.
127 . The method of claim 125 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
128 . The method of claim 125 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
129 . The method of claim 125 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
130 . A kit comprising in one or more containers an amount of the composition of claim 61 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma.
131 . A pharmaceutical composition comprising a compound, salt or solvate according to claim 78 admixed with a pharmaceutically acceptable carrier, excipient or diluent.
132 . A veterinary composition comprising a compound, salt or solvate according to claim 78 admixed with a veterinarily acceptable carrier, excipient or dilluent.
133 . A method for preventing or treating a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma, said method comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound, salt or solvate of claim 78 .
134 . The method of claim 133 wherein the disease or condition is ulcerative colitis.
135 . The method of claim 133 wherein said therapeutically effective amount comprises a dose range of from about 0.001 mg to about 1,000 mg.
136 . The method of claim 133 wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 500 mg.
137 . The method of claim 133 wherein said therapeutically effective amount comprises a dose range of from about 1 mg to about 250 mg.
138 . A kit comprising in one or more containers an amount of the composition of claim 133 effective to treat or prevent a disease or condition selected from the group consisting of osteoarthritis, rheumatoid arthritis, fibromyalgia, migraine, headache, toothache, burn, sunburn, snake bite (in particular, venomous snake bite), spider bite, insect sting, neurogenic bladder, benign prostatic hypertrophy, interstitial cystitis, urinary tract infection, cough asthma, pharyngitis, mucositis, pancreatitis, enteritis, cellulites, peripheral neuropathy, bilateral peripheral neuropathy, diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, causalgia, sciatic neuritis, mandibular joint neuralgia, peripheral neuritis, polyneuritis, stump pain, phantom limb pain, bony fractures, post-operative ileus, Irritable Bowel Syndrome, Crohn's Disease, ulcerative colitis, cholecystitis, pancreatitis, postmastectomy pain syndrome, oral neuropathic pain, Charcot's pain, reflex sympathetic dystrophy, Guillain-Barre syndrome, meralgia paresthetica, burning-mouth syndrome, optic neuritis, postfebrile neuritis, migrating neuritis, segmental neuritis, Gombault's neuritis, neuronitis, cervicobrachial neuralgia, cranial neuralgia, geniculate neuralgia, glossopharyngial neuralgia, migrainous neuralgia, idiopathic neuralgia, intercostals neuralgia, mammary neuralgia, Morton's neuralgia, nasociliary neuralgia, occipital neuralgia, red neuralgia, Sluder's neuralgia, splenopalatine neuralgia, supraorbital neuralgia, vidian neuralgia, sinus headache, tension headache, labor, childbirth, intestinal gas, menstrual cramps, cancer, and trauma.Join the waitlist — get patent alerts
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