US2003187256A1PendingUtilityA1
Benoxazinones/benzothiazinones as serine protease inhibitors
Priority: Mar 31, 1998Filed: Nov 12, 2002Published: Oct 2, 2003
Est. expiryMar 31, 2018(expired)· nominal 20-yr term from priority
Inventors:Kent Alan BerrymanDennis M. DowningDanette DudleyJeremy John EdmundsLakshmi Sourirajan NarasimhanStephen Taras Rapundalo
A61P 7/02A61P 43/00A61P 9/00C07D 279/16C07D 265/36
43
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Claims
Abstract
This invention discloses benzoxazinone and benzothiazinone compounds which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound according to Formula 1
or stereoisomers or pharmaceutically acceptable salt forms or prodrugs thereof, wherein:
A is selected from O, S, S(═O), S(═O)(═O), OCH 2 , CH 2 O, SCH 2 , S(═O)CH 2 , S(═O)(═O)CH 2 , CH 2 S, CH 2 S(═O), CH 2 S(═O)(═O);
B is selected from cycloalkyl, heteroalkyl, cycloalkylalkyl, heteroalkylalkyl, aryl, arylalkyl, heterocycle, heterocycloalkyl, each optionally substituted with R 1 and R 2 ;
D is selected from H, alkyl, cycloalkyl, heteroalkyl, cycloalkylalkyl, heteroalkylalkyl, aryl, arylalkyl, heterocycle, heterocycloalkyl, each optionally substituted with R 1 and R 2 ;
E is absent or selected from O, S, NH;
F is selected from N, NCH 2 , CH 2 N;
G is absent or selected from alkyl, alkyl interrupted by one or more heteroatoms, cycloalkyl, cycloalkyl interrupted by one or more heteroatoms;
J is absent or selected from aryl or heterocycle each optionally substituted with R 1 and R 2 ;
K is absent or selected from an alkyl, alkyl interrupted by one or more heteroatoms, cycloalkyl interrupted by one or more heteroatoms, cycloalkylalkyl interrupted by one or more heteroatoms, each optionally substituted with R 1 and R 2 ;
L is selected from H, chlorine, fluorine, bromine, iodine, OH, O(alkyl), amine, alkyl, fluoroalkyl, amide, NO 2 , SH, S(O) n (alkyl), SO 3 H, SO 3 alkyl, aldehyde, ketone, acid, ester, urea, Oalkylamide, Oalkylester, Oalkylacid, Nalkylacid, alkylamine, alkylamide, alkylketone, alkylacid, alkylester, alkylurea, Nalkylamide, Nalkylester, NC(═O)alkyl, NC(═O)aryl, NC(═O)cycloalkyl, NC(═O)cycloalkylalkyl, NC(═O) alkylaryl, R 1 . R 2 , nitrile;
R 1 is selected from H, amine, alkylamine, amide, C(═NH)NHNH 2 , alkylC(═NH)NHNH 2 , C(═NH)NHOH, alkylC(═NH)NHOH, NHC(═NH)NH 2 , alkylNHC(═NH)NH 2 , C(═S)NH 2 , alkylC(═S)NH 2 , C(═NH)alkyl, alkylC(═NH)alkyl, C(═NR 3 )N(R 4 )(R 5 ), alkylC(═NR 3 )N(R 4 )(R 5 );
R 2 is selected from H, chlorine, fluorine, bromine, iodine, OH, Oalkyl, amine, alkylaldehyde, alkylamide, alkylester, alkylketone, alkylacid, Oalkylamide, Oalkylacid, Oalkylester, aninealkylacid, aminealkylamide, aminealkylester, NC(═O)alkyl, NC(═O)aryl, NC(═O)cycloalkyl, NC(═O)alkylaryl, alkylamine, amide, aldehyde, ester, ketone, NO 2 , SH, S(O) n (C 1-10 alkyl), SO 3 H, SO 3 alkyl, CHO, acid, alkyl, C(═NH)alkyl, C(═NH)NHNH 2 , alkylC(═NH)NHNH 2 , C(═NH)NHOH, alkylC(═NH)NHOH, NHC(═NH)NH 2 , alkylNHC(═NH)NH 2 , C(═S)NH 2 , alkylC(═S)NH 2 , alkylC(═NH)alkyl, C(═NR 3 )N(R 4 )(R 5 ), alkylC(═NR 3 )N(R 4 )(R 5 );
R 3 , R 4 , and R 5 are a hydrogen atom, alkyl group having 1 to 4 carbon atoms optionally interrupted by a heteroatom, or R 4 and R 5 are bonded to form —(CH 2 ) p —W—(CH 2 ) q —, wherein p and q are an integer of 2 or 3, a certain position on the methylene chain is unsubstituted or substituted by an alkyl group having 1 to 4 carbon atoms, W is a direct bond, —CH 2 —, —O—, —N(R 6 )—, or —S(O) r — wherein R 6 is H or alkyl, and r is 0 or 1 or 2;
n is selected from 0, 1,2;
X 1 is C or N;
X 2 is C or N;
X 3 is C or N; and
X 4 is C or N.
2 . A compound according to claim 1 wherein the compound is according to Formula 2
or stereoisomers or pharmaceutically acceptable salts, esters, amides or prodrugs thereof, wherein A, B, E, G, J, K, and L are defined as above.
3 . A compound according to claim 1 wherein the compound is according to Formula 3
or stereoisomers or pharmaceutically acceptable salts, esters, amides or prodrugs thereof, wherein B, G, J, K, and L are defined as above.
4 . A compound according to claim 1 wherein the compound is according to Formula 4
or stereoisomers or pharmaceutically acceptable salts, esters, amides or prodrugs thereof, wherein B, G, J, K, and L are defined as above.
5 . A compound according to claim 1 wherein the compound is according to Formula 5
or stereoisomers or pharmaceutically acceptable salts, esters, amides or prodrugs thereof, wherein R 1 , R 2 , G, J, K, and L are as defined above.
6 . A compound according to claim 1 wherein the compound is according to Formula 6
or stereoisomers or pharmaceutically acceptable salts, esters, amides or prodrugs thereof, wherein R 1 , R 2 , G, J, K, and L are as defined above.
7 . A compound according to Formulas 7 and 8
or stereoisomers or pharmaceutically acceptable salt forms or prodrugs thereof,
wherein
R 7 is (3-amidino)phenyl, (3-hydroxy)phenyl, [3-hydroxylamino(imino)methyl]-phenyl, [3-hydrazino(imino)methyl]-phenyl, (3-aminomethyl)phenyl, (3-amino)phenyl, (3-methylamino)phenyl, (3-dimethylamino)phenyl, (5-amidino-2-hydroxy)phenyl, (5-amidino-2-methoxy)phenyl, (1-amidino)piperid-3-yl, (1-amidino)pyrrolid-3-yl, (5-amidino)thien-2-yl, (5-amidino)furan-2-yl, (5-amidino)-1,3-oxazol-2-yl, (2-amidino)-1,3-oxazol-5-yl, 1H-pyrazol-5-yl, tetrahydro-1H-pyrazol-3-yl, (1-amidino)tetrahydro-1H-pyrazol-3-yl, (2-amidino)-1H-imidazol-4-yl, (2-amino)-1H-imidazol-4-yl, (5-amidino)-1H-imidazol-2-yl, (5-amino)-1H-imidazol-2-yl, pyridin-3-yl, (4-amino)pyridin-3-yl, (4-dimethylamino)pyridin-3-yl, (6-amino)pyridin-2-yl, (6-amidino)pyridin-2-yl, (2-amino)pyridin-4-yl, (2-amidino)pyridin-4-yl, (2-amidino)pyrimid-4-yl, (2-amino)pyrimidin-4-yl, (4-amidino)pyrimid-2-yl, (4-amino)pyrimidin-2-yl, (6-amidino)pyrazin-2-yl, (6-amino)pyrazin-2-yl, (4-amidino)-1,3,5-triazin-2-yl, (4-amino)-1,3,5-triazin-2-yl, (3-amidino)-1,2,4-triazin-5-yl, (3-amino)-1,2,4-triazin-5-yl, (3-amidino)benzyl, (3-amino)benzyl, (3-aminomethyl)benzyl, (1-amidino)piperid-3-ylmethyl, (1-amidino)pyrrolid-3-ylmethyl, (5-amidino)thien-2-ylmethyl, (5-amidino)furan-2-ylmethyl, (5-amidino)oxazol-2-ylmethyl, (2-amidino)imidazol-5-ylmethyl, (5-amidino)imidazol-2-ylmethyl, (6-amidino)pyridin-2-ylmethyl, (6-amino)pyridin-2-ylmethyl, (2-amidino)pyrimidin-4-ylmethyl, (2-amino)pyrimidin-4-ylmethyl, (4-amidino)pyrimidin-2-ylmethyl, (4-amino)pyrimidin-2-ylmethyl, (6-amidino)pyrazin-2-ylmethyl, (6-amino)pyrazin-2-ylmethyl, 3-aminocyclohexyl, 3-amidinocyclohexyl, 3-aminocyclohexylmethyl, 3-amidinocyclohexylmethyl, 3-aminocyclopentyl, 3-amidinocyclopentyl, and 3-aminocyclopentylmethyl, and 3-amidinocyclopentylmethyl;
R 8 is Br, I, C 2 H 5 , H, Cl, F, SH, SMe, CF 3 , CH 3 ; CO 2 H, CO 2 Me, CN, C(═NH)NH 2 , C(═NH)NHOH, C(═NH)NHNH 2 , C(═O)NH 2 , CH 2 OH, CH 2 NH 2 , NO 2 , OH, OMe, OCH 2 Ph, OCH 2 CO 2 H, O(CH 2 ) 2 CO 2 H, O(CH 2 ) 3 CO 2 H, NHCH 2 CO 2 H, NH(CH 2 ) 2 CO 2 H, NH(CH 2 ) 3 CO 2 H, OCH 2 CH 2 OH, OCH 2 (1H-tetrazol-5-yl), NH 2 , NHButyl, NMe2, NHPh, NHCH 2 Ph, NHC(═O)Me, NHC(═O)c-Hexyl, NHC(═O)CH 2 c-Hexyl, NHC(═O)Ph, NHC(═O)CH 2 Ph, NHS(═O) 2 Me, NHS(═O) 2 c-Hexyl, NHS(═O) 2 CH 2 c-Hexyl, NHS(═O) 2 Ph, and NHS(═O) 2 CH 2 Ph;
R 9 is (CH 2 ) 5 , (CH 2 ) 4 , (CH 2 ) 6 , CH 2 C(═O)NHCH 2 CH 2 , CH 2 CH 2 NHC(═O)CH 2 , (CH 2 ) 2 NH(CH 2 ) 2 , (CH 2 ) 2 O(CH 2 ) 2 , C 6 H 4 , CH 2 C 6 H 4 , C 6 H 4 CH 2 , C 6 H 10 , CH 2 C 6 H 10 , C 6 H 10 CH 2 , C 5 H 8 , CH 2 C 5 H 8 , C 5 H 8 CH 2 , and CH 2 CH═CHCH 2 CH 2 ; and
R 10 is 2,6-dimethylpiperidinyl, 2,2,6,6-tetramethyl-piperidinyl-4-one, piperidinyl, 2,2,6,6-tetramethylpiperidinyl, (2-carboxy)piperidinyl, (3-carboxy)piperidinyl, (4-carboxy)piperidinyl, 3,5-dimethylpiperidinyl, (4-hydroxy)piperidinyl, (2-imino)piperidinyl, piperidin-4-one-yl, (2-dimethylaminomethyl)-piperidinyl, (4-dimethylamino)-piperidinyl, (4-sulphonyloxy)-piperidinyl, (2-phenyl)piperidinyl, 2,5-dimethylpyrrolidinyl, pyrrolidinyl, (2-carboxy)pyrrolidinyl, (3-N-acetyl-N-methyl)pyrrolidinyl, (3-amino)pyrrolidinyl, (2,5-bis-methoxymethyl)-pyrrolidinyl, 2-hydroxymethyl-pyrrolidinyl, 2-hydroxymethyl-5-methyl-pyrrolidinyl, diisopropylamino, diethylamino, methylamino, 1-methyl-4,5-dihydro-1H-imidazol-2-yl, 2,5-dimethyl-1H-1-imidazolyl, morpholinyl, 2,6-dimethylmorpholinyl, piperazinyl, 2,6-dimethylpiperazinyl, 1H-pyrazolyl, tetrahydro-1H-pyrazol yl, and 2,5-dimethyltetrahydro-1H-1-pyrazolyl.
8 . A compound according to claim 7 wherein R 7 is (2-hydroxy, 5-amidino)phenyl.
9 . A compound according to claim 7 wherein R 8 is H.
10 . A compound according to claim 7 wherein R 9 is (CH 2 ) 5 .
11 . a compound according to claim 7 wherein R 10 is 2,6-dimethylpiperidinyl.
12 . A compound according to claim 7 wherein R 8 is H, R 9 is (CH 2 ) 5 , and R 10 is 2,6-dimethylpiperidinyl.
13 . A compound according to claim 7 wherein R 8 is H, R 9 is (CH 2 ) 5 , and R 10 is 2,5-dimethylpyrrolidinyl.
14 . A compound which is:
3-(4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-4-methoxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-(3-hydroxyphenyl)-2H-1,4-benzothiazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-N-hydroxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-N-hydroxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidohydrazide; 2-[3-(Aminomethyl)phenyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-(3-Aminophenyl)-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-[3-(methylamino)phenyl]-2H-1,4-benzothiazin-3(4H)-one; 2-[3-(Dimethylamino)phenyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-(4-5 -[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-4-hydroxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)tetrahydro-1(2H)-pyridinecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-pyrrolidinecarboximidamide; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl -3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-thiophenecarboximidamide; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-furancarboximidamide; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1,3-oxazole-5-carboximidamide; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1,3-oxazole-2-carboximidamide; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-( 1H-pyrazol-5-yl )-2H-1,4-benzothiazin-3(4H)-one; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1-pyrazolidinecarboximidamide; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1H-imidazole-2-carboximidamide; 2-(2-Amino-1H-imidazol-4-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1H-imidazole-5-carboximidamide; 2-(5-Amino-1H-imidazol-2-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-(3-pyridinyl)-2H-1,4-benzothiazin-3(4H)-one; 2-(4-Amino-3-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-[4-(Dimethylamino)-3-pyridinyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-(6-Amino-2-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 6-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-pyridinecarboximidamide; 2-(2-Amino-4-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-pyridinecarboximidamide; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-pyrimidinecarboximidamide; 2-(2-Amino-4-pyrimidinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-4-pyrimidinecarboximidamide; 2-(4-Amino-2-pyrimidinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 6-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-2-pyrazinecarboximidamide; 2-(6-Amino-2-pyrazinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1,3,5-triazine-2-carboximidamide; 2-(4-Amino-1,3,5-triazin-2-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)-1,2,4-triazine-3-carboximidamide; 2-(3-Amino-1,2,4-triazin-5-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]benzenecarboximidamide; 2-(3-Aminobenzyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-[3-(Aminomethyl)benzyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]tetrahydro-1(2H)-pyridinecarboximidamide; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-1-pyrrolidinecarboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-2-thiophenecarboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-2-furancarboximidamide; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-1,3-oxazole-5-carboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-1H-imidazole-2-carboximidamide; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-1H-imidazole-5-carboximidamide; 6-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-2-pyridinecarboximidamide; 2-[(6-Amino-2-pyridinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 4-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-2-pyrimidinecarboximidamide; 2-[(2-Amino-4-pyrimidinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-4-pyrimidinecarboximidamide; 2-[(4-Amino-2-pyrimidinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 6-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]-2-pyrazinecarboximidamide; 2-[(6-Amino-2-pyrazinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 2-(3-Aminocyclohexyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)cyclohexanecarboximidamide; 2-[(3-Aminocyclohexyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]cyclohexanecarboximidamide; 2-(3-Aminocyclopentyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)cyclopentanecarboximidamide; 2-[(3-Aminocyclopentyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzothiazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)methyl]cyclopentanecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]butyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-6-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]hexyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 2-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)-N-2-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]ethylacetamide; 3-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)-N-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]methylpropanamide; 3-4-[2-(2-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]ethylamino)ethyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-[4-(2-2-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]ethoxyethyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]phenyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]benzyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylphenyl)-3-oxo-3,4-dihydro-2H1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclohexyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclohexylmethyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylcyclohexyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclopentyl-3-oxo-3,4-dihydro-2H1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-[4-(3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclopentylmethyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-[4-(3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylcyclopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-(E)-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]-2-pentenyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-[3-Oxo-4-(5-piperidinopentyl)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-3-Oxo-4-[5-(2,2,6,6-tetramethylpiperidino)pentyl]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]-2-piperidinecarboxylic acid; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]-3-piperidinecarboxylic acid; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]-4-piperidinecarboxylic acid; 3-4-[5-(3,5-Dimethylpiperidino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(4-Hydroxypiperidino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(2-Iminopiperidino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-(4-oxopiperidino)pentyl]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-[4-(5-2-[(Dimethylamino)methyl]piperidinopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-5-[4-(Dimethylamino)piperidino]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]-4-piperidinesulfonic acid; 3-3-Oxo-4-[5-(2-phenylpiperidino)pentyl]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(2,5-Dimethyl-1-pyrrolidinyl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-( 1-pyrrolidinyl)pentyl]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]-2-pyrrolidinecarboxylic acid; N-1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzothiazin-4-yl)pentyl]tetrahydro-1H-pyrrol-3-yl-N-methylacetamide; 3-4-[5-(3-Amino-1-pyrrolidinyl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-(4-5-[2,5-Bis(methoxymethyl)-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[2-(Hydroxymethyl)-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[2-(Hydroxymethyl)-5-methyl-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-4-[5-(Diisopropylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(Diethylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(Methylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(1-Methyl-1H-imidazol-2-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-4-[5-(2,5-Dimethyl-1H-imidazol-1-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-[4-(5-Morpholinopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-4-[5-(3,5-Dimethylmorpholino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-[3-Oxo-4-(5-piperazinopentyl)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-4-[5-(2,6-Dimethylpiperazino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-(1H-pyrazol-1-yl)pentyl]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-[3-Oxo-4-(5-tetrahydro-1H-pyrazol-1-ylpentyl)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-4-[5-(2,5-Dimethyltetrahydro-1H-pyrazol-1-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-(6-Chloro-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-fluoro-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-sulfanyl-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(methylsulfanyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-(trifluoromethyl)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-methyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid; Methyl 2-3-[amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylate; 3-(6-Cyano-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboximidamide; 2-3-[amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-N-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboximidamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-[hydrazino(imino)methyl]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxamide; 3-[4-5 -[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(hydroxymethyl)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(6-(Aminomethyl)-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-nitro-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-methoxy-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-(Benzyloxy)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 2-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)oxy]acetic acid; 3-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)oxy]propanoic acid; 4-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)oxy]butanoic acid; 2-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)amino]acetic acid; 3-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)amino]propanoic acid; 4-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)amino]butanoic acid; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(2-hydroxyethoxy)-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-(2H-1,2,3,4-tetraazol-5-ylmethoxy)-3,4-dihydro-2H-1,4-benzothiazin-2-yl]benzenecarboximidamide; 3-(6-Amino-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-(Butylamino)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-(Dimethylamino)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-Anilino-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-(Benzylamino)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)acetamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)cyclohexanecarboxamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)-2-cyclohexylacetamide; N-(2-3-[Amino(imino)methyl]phenyl -4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)benzenecarboxamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-6-yl)-2-phenylacetamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-[(methylsulfonyl)amino]-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; 3-(6-[(Cyclohexylsulfonyl)amino]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-(6-[(Cyclohexylmethyl)sulfonyl]amino-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-[(phenylsulfonyl)amino]-3,4-dihydro-2H-1,4-benzothiazin-2-ylbenzenecarboximidamide; or 3-(6-[(Benzylsulfonyl)amino]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzothiazin-2-yl)benzenecarboximidamide;
15 . A compound which is:
3-(4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-methoxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-(3-hydroxyphenyl)-2H-1,4-benzoxazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-N-hydroxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidohydrazide; 2-[3-(Aminomethyl)phenyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-(3-Aminophenyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-[3-(methylamino)phenyl]-2H-1,4-benzoxazin-3(4H)-one; 2-[3-(Dimethylamino)phenyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)tetrahydro-1(2H)-pyridinecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)-1-pyrrolidinecarboximidamide; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-thiophenecarboximidamide; 5-(4-5 -[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-furancarboximidamide; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-1,3-oxazole-5-carboximidamide; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)-1,3-oxazole-2-carboximidamide; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-(1H-pyrazol-5-yl)-2H-1,4-benzoxazin-3(4H)-one; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-tetrahydro-1H-pyrazol-3-yl-2H1,4-benzoxazin-3(4H)-one; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-1-pyrazolidinecarboximidamide; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-1H-imidazole-2-carboximidamide; 2-(2-Amino-1H-imidazol-4-yl)-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)-1H-imidazole-5-carboximidamide; 2-(5-Amino-1H-imidazol-2-yl)-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2-(3-pyridinyl)-2H-1,4-benzoxazin-3(4H)-one; 2-(4-Amino-3-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-[4-(Dimethylamino)-3-pyridinyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-(6-Amino-2-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 6-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-pyridinecarboximidamide; 2-(2-Amino-4-pyridinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-pyridinecarboximidamide; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-pyrimidinecarboximidamide; 2-(2-Amino-4-pyrimidinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-pyrimidinecarboximidamide; 2-(4-Amino-2-pyrimidinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 6-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-2-pyrazinecarboximidamide; 2-(6-Amino-2-pyrazinyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 4-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-1,3,5-triazine-2-carboximidamide; 2-(4-Amino-1,3,5-triazin-2-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 5-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-1,2,4-triazine-3-carboximidamide; 2-(3-Amino-1,2,4-triazin-5-yl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]benzenecarboximidamide; 2-(3-Aminobenzyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-[3-(Aminomethyl)benzyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]tetrahydro-1(2H)-pyridinecarboximidamide; 3-[(4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-1-pyrrolidinecarboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-2-thiophenecarboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-2-furancarboximidamide; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-1,3-oxazole-5-carboximidamide; 5-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-1H-imidazole-2-carboximidamide; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)methyl]-1H-imidazole-5-carboximidamide; 6-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-2-pyridinecarboximidamide; 2-[(6-Amino-2-pyridinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 4-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-2-pyrimidinecarboximidamide; 2-[(2-Amino-4-pyrimidinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]-4-pyrimidinecarboximidamide; 2-[(4-Amino-2-pyrimidinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 6-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)methyl]-2-pyrazinecarboximidamide; 2-[(6-Amino-2-pyrazinyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 2-(3-Aminocyclohexyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)cyclohexanecarboximidamide; 2-[(3-Aminocyclohexyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]cyclohexanecarboximidamide; 2-(3-Aminocyclopentyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)cyclopentanecarboximidamide; 2-[(3-Aminocyclopentyl)methyl]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-2H-1,4-benzoxazin-3(4H)-one; 3-[(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)methyl]cyclopentanecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]butyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-6-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]hexyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 2-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)-N-2-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]ethylacetamide; 3-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)-N-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]methylpropanamide; 3-4-[2-(2-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]ethylamino)ethyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-[4-(2-2-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]ethoxyethyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]phenyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]benzyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylphenyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclohexyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclohexylmethyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-[4-(4-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylcyclohexyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclopentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-[4-(3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]cyclopentylmethyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-[4-(3-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]methylcyclopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-(E)-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]-2-pentenyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-[3-Oxo-4-(5-piperidinopentyl)-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-3-Oxo-4-[5-(2,2,6,6-tetramethylpiperidino)pentyl]-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]-2-piperidinecarboxylic acid; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]-3-piperidinecarboxylic acid; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]-4-piperidinecarboxylic acid; 3-4-[5-(3,5-Dimethylpiperidino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(4-Hydroxypiperidino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(2-Iminopiperidino)pentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-(4-oxopiperidino)pentyl]-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-[4-(5-2-[(Dimethylamino)methyl]piperidinopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-5-[4-(Dimethylamino)piperidino]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]-4-piperidinesulfonic acid; 3-3-Oxo-4-[5-(2-phenylpiperidino)pentyl]-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(2,5-Dimethyl-1-pyrrolidinyl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-(1-pyrrolidinyl)pentyl]-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 1-[5-(2-3 -[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]-2-pyrrolidinecarboxylic acid; N-1-[5-(2-3-[Amino(imino)methyl]phenyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)pentyl]tetrahydro-1H-pyrrol-3-yl-N-methylacetamide; 3-4-[5-(3 -Amino-1-pyrrolidinyl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-(4-5-[2,5-Bis(methoxymethyl)-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[2-(Hydroxymethyl)-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[2-(Hydroxymethyl)-5-methyl-1-pyrrolidinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-4-[5-(Diisopropylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(Diethylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(Methylamino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(1-Methyl-1H-imidazol-2-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-4-[5-(2,5-Dimethyl-1H-imidazol-1-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-[4-(5-Morpholinopentyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-4-[5-(3,5-Dimethylmorpholino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-[3-Oxo-4-(5-piperazinopentyl)-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-4-[5-(2,6-Dimethylpiperazino)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-3-Oxo-4-[5-(1H-pyrazol-1-yl)pentyl]-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-[3-Oxo-4-(5-tetrahydro-1H-pyrazol-1-ylpentyl)-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-4-[5-(2,5-Dimethyltetrahydro-1H-pyrazol-1-yl)pentyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-(6-Chloro-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-fluoro-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-sulfanyl-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(methylsulfanyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-(trifluoromethyl)-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carboxylic acid; Methyl 2-3-[amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carboxylate; 3-(6-Cyano-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-N-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carboximidamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-[hydrazino(imino)methyl]-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-ylbenzenecarboximidamide; 2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-6-carboxamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(hydroxymethyl)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(6-(Aminomethyl)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-nitro-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-methoxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-(Benzyloxy)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 2-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)oxy]acetic acid 3-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)oxy]propanoic acid; 4-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)oxy]butanoic acid; 2-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)amino]acetic acid; 3-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1 (2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)amino]propanoic acid; 4-[(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)amino]butanoic acid; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-(2-hydroxyethoxy)-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-[4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-(2H-1,2,3,4-tetraazol-5-ylmethoxy)-3,4-dihydro-2H-1,4-benzoxazin-2-yl]benzenecarboximidamide; 3-(6-Amino-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-(Butylamino)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-(Dimethylamino)-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-Anilino-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-(Benzylamino)-4-5 -[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)acetamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)cyclohexanecarboxamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)-2-cyclohexylacetamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)benzenecarboxamide; N-(2-3-[Amino(imino)methyl]phenyl-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)-2-phenylacetamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-6-[(methylsulfonyl)amino]-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-ylbenzenecarboximidamide; 3-(6-[(Cyclohexylsulfonyl)amino]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-(6-[(Cyclohexylmethyl)sulfonyl]amino-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; 3-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-6-[(phenyl sulfonyl)amino]-3,4-dihydro-2H1,4-benzoxazin-2-ylbenzenecarboximidamide; or 3-(6-[(Benzylsulfonyl)amino]-4-5-[(2R,6S)-2,6-dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)benzenecarboximidamide.
16 . A compound which is:
3-((2R)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-methoxybenzenecarboximidamide; 3-((2S)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-methoxybenzenecarboximidamide; 3-((2R)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl -3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide; 3-((2S)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide; 3-((2R)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide; or 3-((2S)-4-5-[(2R,6S)-2,6-Dimethyltetrahydro-I (2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)benzenecarboximidamide.
17 . A compound which is:
3-((2S)-4-5 -[(2R,6S)-2,6-Dimethyltetrahydro-1(2H)-pyridinyl]pentyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)-4-hydroxybenzenecarboximidamide.
18 . A compound of which is:
2H-1,4-Benzoxazin-3(4H)-one, 4-[3-(2,6-dimethyl-1-piperidinyl)propyl]-2-phenyl-; 4-[5-(2,5-Dimethyl-pyrrolidin-1-yl)-pentyl]-2-phenyl-4H-benzo[1,4]oxazin-3-one; 2H-1,4-Benzoxazin-3(4H)-one, 4-[5-[bis(1-methylethyl)amino]pentyl]-2-phenyl-; 2H-1,4-Benzoxazin-3(4H)-one, 4-[3-(2,5-dimethyl-1-pyrrolidinyl)propyl]-2-phenyl-; 2H-1,4-Benzoxazin-3(4H)-one, 4-[3-[bis(1-methylethyl)amino]propyl]-2-phenyl-; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-phenyl-4H-benzo[1,4]oxazin-3-one; 4-(5-Diethylamino-pentyl)-2-phenyl-4H-benzo[1,4]oxazin-3-one; 2-Phenyl-4-(5-pyrrolidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-[5-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-pentyl]-isoindole-1,3-dione; 4-(5-Imidazol-1-yl-pentyl)-2-phenyl-4H-benzo[1,4]oxazin-3-one; 2-(4-Chloro-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-(2-Chloro-phenyl)-4-[5-(2,5-dimethyl-pyrrolidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-(2-Chloro-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 5-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-pentanamidine; 2-Phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-(4-Chloro-phenyl)-4-[5-(2,5-dimethyl-pyrrolidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-Phenyl-4-(5-pyrrolidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; compound with trifluoro-acetic acid; 3-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl)-benzonitrile; 4-[6-(2,5-Dimethyl-pyrrolidin-1-yl)-hexyl]-2-phenyl-4H-benzo[1,4]oxazin-3-one; 3-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl)-benzamidine; 2-Naphthalen-2-yl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 4-(5-Amino-pentyl)-2-phenyl-4H-benzo[1,4]oxazin-3-one; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-phenyl-4H-benzo[1,4]oxazin-3-one; 6-Methyl-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 7-Methoxy-2-phenyl -4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 8-Chloro-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 3-Oxo-2-phenyl-4-(5-piperidin-1-yl-pentyl)-3,4-dihydro-2H-benzo[1,4]oxazine-6-carbonitrile; 4-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl)-benzamidine; 1-[5-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-pentyl]-piperidine-2,6-dione; 3-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-propionitrile; 4-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-butyronitrile; 5-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-pentanenitrile; N-[3-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-propyl]-guanidine; N-[5-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-yl)-pentyl]-guanidine; 4-(3-Oxo-2-phenyl-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl)-benzamidine; 2-(4-Methoxy-phenyl)-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 7-Methyl-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 5-Methyl-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 6-Methoxy-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; N-Hydroxy-4-(3-oxo-2-phenyl-2,3-dihydro-benzo [1,4]oxazin-4-ylmethyl)-benzamidine; 6-Chloro-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-(4-Methoxy-phenyl)-4-(5-piperazin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-(4-Hydroxy-phenyl)-4-(5 -piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(4-hydroxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 2-(4-Methoxy-phenyl)-4-[5-(4-methyl-piperazin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzonitrile; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-thiobenzamide; [2-(4-Methoxy-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-yl]-acetic acid; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-N-hydroxy-benzamidine; Benzenecarboximidic acid, 4-[3,4-dihydro-4-[5-(2,6-dimethyl-1-piperidinyl)pentyl]-3-oxo-2H-1,4-benzoxazin-2-yl]-, hydrazide; 6-Amino-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 4-(5-Bromo-pentyl)-2-(3,4-dimethoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 4-(5-Bromo-pentyl)-2-(3,4,5-trimethoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 4-(5-Bromo-pentyl)-2-(4-methoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; N-[2-(2,6-Dimethyl-piperidin-1-yl)-ethyl]-2-[2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-yl]-acetamide; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(3,4,5-trimethoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 2-(3,4-Dimethoxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-(4-Bromo-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 8-Methyl-2-phenyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-(4-Benzylamino-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-(4-Methoxy-phenyl)-4-[5-(2,2,6,6-tetramethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 4-(2-Bromo-ethyl)-2-(4-methoxy-phenyl)-4H-benzo[1,4]oxazin-3-3-one; 4-(5-Bromo-pentyl)-2-(3,4-dichloro-phenyl)-4H-benzo[1,4]oxazin-3-one; 4-(2-Hydroxy-ethyl)-2-(4-methoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 2-(3,4-Dichloro-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 4-[3-(2,6-Dimethyl-piperidin-1-ylmethyl)-benzyl]-2-(4-methoxy-phenyl)-4H-benzo 1,4]oxazin-3-one; 4-(2-Amino-ethyl)-2-(4-methoxy-phenyl)-4H-benzo[1,4]oxazin-3-3-one; 2-(2,6-Dimethyl-piperidin-1-yl)-N-{2-[2-(4-methoxy-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-yl]-ethyl}-acetamide; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-5-oxo-pentyl]-2-(4-methoxy-phenyl)-4H-benzo[1,4]oxazin-3-one; 3-{4-[4-(2,6-Dimethyl-piperidin-1-yl)-butyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-{4-[6-(2,6-Dimethyl-piperidin-1-yl)-hexyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 2-(5-Aminomethyl-2-hydroxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 2-(3-Aminomethyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-7-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-4-methoxy-benzamidine; 2-(5-Aminomethyl-2-methoxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]oxazin-3-one; 3-(4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-N-hydroxy-4-methoxy-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-N-hydroxy-benzamidine; 3-{7-Chloro-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 4-(5-Bromo-pentyl)-2-phenyl-4H-benzo[1,4]oxazin-3-one; 3-[3-Oxo-4-(5-piperidin-1-yl-pentyl)-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; N-{2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl}-acetamide; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-4-hydroxy-benzamidine; 3-[4-(5-Diisopropylamino-pentyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; 3-(4-{4-[(Diisopropylamino)-methyl]-benzyl}-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl)-benzamidine; 3-{4-[4-(2,6-Dimethyl-piperidin-1-ylmethyl)-benzyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-4-hydroxy-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-N-methyl-benzamidine; {2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl}-acetic acid; 3-(4-{3-[(Diisopropylamino)-methyl]-benzyl}-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl)-benzamidine; 3-{4-[3-(2,6-Dimethyl-piperidin-1-ylmethyl)-benzyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-7-carboxylic acid; 3-{3-Oxo-4-[4-(pyridin-2-ylamino)-butyl]-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-7-carboxylic acid methyl ester; 3-[4-(5-Dihexylamino-pentyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; 3-{4-[4-(Methyl-pyridin-2-yl-amino)-butyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-[3-(imino-morpholin-4-yl-methyl)-phenyl]-4H-benzo[1,4]oxazin-3-one; 3-{3-Oxo-4-[4-(pyrimidin-2-ylamino)-butyl]-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-[4-(4-Cyclohexylamino-butyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; 3-{4-[5-(2,5-Dimethyl-pyrrolidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-[4-(5-Morpholin-4-yl-pentyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-2,3-dihydroxy-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 4-[2-(3-Carbamimidoyl-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl]-N,N-dimethyl-benzamide; 2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-6-carboxylic acid; 3-[2-(3-Carbamimidoyl-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl]-N,N-dimethyl-benzamide; 3-{4-[5-(2,6-Dimethyl -piperidin-1-yl)-pent-2-enyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 3-[4-(5-Amino-pentyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzamidine; 2-(3-Carbamimidoyl-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-6-carboxylic acid methyl ester; 4-Methoxy-3-[4-(4-methoxy-benzyl)-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl]-benzonitrile; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pent-3-enyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 4-[2-(3-Cyano-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl]-N,N-dimethyl-benzamide; p 1 3-[2-(3-Carbamimidoyl-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl]-5-(2,6-dimethyl-piperidin-1-ylmethyl)-benzoic acid; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}1-4-hydroxy-benzamidine; 3-Acetyl-2-(2-methoxy-phenyl)-thiazolidine-4-carboxylic acid 4-cyano-2-{4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-phenyl ester; 3-[2-(3-Carbamimidoyl-phenyl)-3-oxo-2,3-dihydro-benzo[1,4]oxazin-4-ylmethyl]-5-(2,6-dimethyl-piperidin-1-ylmethyl)-N-hydroxy-benzamide; 4-(2-Dimethylamino-ethyl)-7-nitro-2-phenyl-4H-benzo[1,4]thiazin-3-one; 4-(2-Diethylamino-ethyl)-7-nitro-2-phenyl-4H-benzo[1,4]thiazin-3-one; 2H-1,4-Benzothiazin-3(4H)-one, 4-[2-(dimethylamino)ethyl]-7-nitro-2-phenyl-, monohydrochloride; 2H-1,4-Benzothiazin-3(4H)-one, 4-[2-(diethylamino)ethyl]-7-nitro-2-phenyl-, monohydrochloride; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(4-methoxy-phenyl)-4H-benzo[1,4]thiazin-3-one; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzonitrile; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-thiobenzamide; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(4-methoxy-phenyl)-4H-benzo[1,4]thiazin-3-one; compound with trifluoro-acetic acid; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzonitrile; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzamide; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(3-methoxy-phenyl)-2-(4-methoxy-phenyl)-4H-benzo[1,4]thiazin-3-one; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-(4-methoxy-phenyl)-1,1-dioxo-1,4-dihydro-2H-1l>6_-benzo[1,4]thiazin-3-one; 2-(4-Benzyloxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]thiazin-3-one; 2-(4-Butoxy-phenyl)-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]thiazin-3-one; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-thiobenzamide; 4-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-N-hydroxy-benzamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzamidine; 3-{4-[5-(2-Hydroxymethyl-pyrrolidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]thiazin-2-yl}-benzamidine; 4-Allyl-2,2-diphenyl-4H-benzo[1,4]thiazin-3-one; 4-(2-Diethylamino-ethyl)-7-nitro-2-phenyl-4H-benzo[1,4]thiazin-3-one; 2-(3-Diethylamino-propylamino)-4-methyl-2-phenyl-4H-benzo[1,4]thiazin-3-one; 4-(2-Diethylamino-ethyl)-2,2-diphenyl-4H-benzo[1,4]thiazin-3-one; 2-Benzyl-4-(5-piperidin-1-yl-pentyl)-4H-benzo[1,4]oxazin-3-one; 2-Cyclohexyl-4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-4H-benzo[1,4]thiazin-3-one; 2H-1,4-Benzothiazin-3(4H)-one, 4-methyl-2,2-diphenyl-; 4-Ethyl-2-phenyl-2-piperidin-1-yl-4H-benzo[1,4]thiazin-3-one; 4-Methyl-2-phenyl-2-piperidin-1-yl-4H-benzo[1,4]thiazin-3-one; 3-{4-[5-(2,6-dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-piperidine-1-carboxamidine; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-piperidin-3-yl-4H-benzo[1,4]oxazin-3-one; 3-Oxo-2-phenyl-2,4-bis-(5-piperidin-1-yl-pentyl)-3,4-dihydro-2H-benzo[1,4]oxazine-6-carbonitrile; 4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-2-pyridin-2-yl-4H-benzo[1,4]oxazin-3-one; N-Hydroxy-3-oxo-2-phenyl-4-(5-piperidin-1-yl-pentyl)-3,4-dihydro-2H-benzo[1,4]oxazine-6-carboxamidine; 3-Oxo-2-phenyl-4-(5-piperidin-1-yl-pentyl)-3,4-dihydro-2H-benzo[1,4]oxazine-6-carboxamidine; 3-{4-[5-(2,6-Dimethyl-piperidin-1-yl)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-thiobenzamide; 3-{4-[5-(Adamantan-1-yl amino)-pentyl]-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-2-yl}-benzamidine; 2-(3-Diethylamino-propylamino)-4-methyl-2-phenyl-4H-benzo[1,4]oxazin-3-one; 4-[3-(2,6-Dimethyl-1-piperidinyl)propyl]-2-phenyl-2H/-1,4-benzoxazin-3(4H/)-one; or 4-Methyl-2-phenyl-2H/-1,4-benzoxazin-3(4H/)-one.
19 . A method for the treatment or prophylaxis of thrombotic disorders in a mammal comprising administering to said mammal an effective amount of a compound according to claim 1 .
20 . A method according to claim 19 , wherein said disorder is venous thrombosis.
21 . A method according to claim 19 , wherein said disorder is arterial thrombosis.
22 . A method according to claim 19 , wherein said disorder is pulmonary embolism.
23 . A method according to claim 19 , wherein said disorder is myocardial infarction.
24 . A method according to claim 19 , wherein said disorder is cerebral infarction.
25 . A method according to claim 19 , wherein said disorder is restenosis.
26 . A method according to claim 19 , wherein said disorder is cancer.
27 . A method according to claim 19 , wherein said disorder is angina.
28 . A method according to claim 19 , wherein said disorder is diabetes.
29 . A method according to claim 19 , wherein said disorder is atrial fibrillation.
30 . A method according to claim 19 , wherein said disorder is heart failure.
31 . A pharmaceutical formulation comprising a compound of claim 1 admixed with a carrier, diluent or excipient.
32 . A pharmaceutical formulation comprising a compound of claim 2 together with a carrier, diluent or excipient.
33 . A pharmaceutical formulation comprising a compound of claim 14 together with a carrier, diluent or excipient.
34 . A pharmaceutical formulation comprising a compound of claim 15 together with a carrier, diluent or excipient.
35 . A method for inhibiting serine proteases comprising administering to a mammal an effective amount of serine protease inhibitor of claim 1 .
36 . A method according to claim 35 , wherein said serine protease is factor Xa.Cited by (0)
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