Patent ID: 6410536
Filing Date: 2002-06-25
Classification: A61P,C07D

Abstract:
A compound according to Formula V or stereoisomers or pharmaceutically acceptable salts, esters, or amides thereof, wherein X, Y, R7, R8, and - - -  are as follows:X is selected from (CH2)5, (CH2)4, (CH2)6, CH2C(&boxH;O)NHCH2CH2, CH2CH2NHC(&boxH;O)CH2, (CH2)2NH(CH2)2, (CH2)2O(CH2)2, C6H4, CH2C6H4, C6H4CH2, C6H10, CH2C6H10, C6H10CH2, C5H8, CH2C5H8, C5H8CH2, and CH2CH&boxH;CHCH2CH2; Y is selected from 2,6-dimethylpiperidinyl, piperidinyl, 2,2,6,6-tetramethyl-piperidinyl-4-one, (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, dimethylamino, 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-pyrazolyl, and 2,5-dimethyltetrahydro-1H-1-pyrazolyl; R7 is selected from (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, (1-amidino)piperid-3-yl, (1-amidino)pyrrolid-3-yl, (5-amidino)thien-2-yl, (5-amidino)furan-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, (3-amidino)benzyl, (3-amino)benzyl, (3-aminomethyl)benzyl, (1-amidino)pyrrolid-3-ylmethyl, (5-amidino)thien-2-ylmethyl, (5-amidino)furan-2-ylmethyl, (6-amidino)pyridin-2-ylmethyl, (6-amino)pyridin-2-ylmethyl, 3-aminocyclohexyl, 3-amidinocyclohexyl, 3-aminocyclohexylmethyl, 3-amidinocyclohexylmethyl, 3-aminocyclopentyl, 3-amidinocyclopentyl, 3-aminocyclopentylmethyl, and 3-amidinocyclopentylmethyl; and R8 is selected from H, Cl, F, SH, SMe, CF3, CH3, CO2H, CO2Me, CN, C(&boxH;NH)NH2, C(&boxH;NH)NHOH, C(&boxH;NH)NHNH2, C(&boxH;O)NH2, CH2OH, CH2NH2, NO2, OH, OMe, OCH2Ph, OCH2CO2H, O(CH2)2CO2H, O(CH2)3CO2H, NHCH2CO2H, NH(CH2)2CO2H, NH(CH2)3CO2H, OCH2CH2OH, OCH2(1H-tetrazol-5-yl), NH2, NHButyl, NMe2, NHPh, NHCH2Ph, NHC(&boxH;O)Me, NHC(&boxH;O)c-Hexyl, NHC(&boxH;O)CH2c-Hexyl, NHC(&boxH;O)Ph, NHC(&boxH;O)CH2Ph, NHS(&boxH;O)2Me, NHS(&boxH;O)2c-Hexyl, NHS(&boxH;O)2CH2c-Hexyl, NHS(&boxH;O)2Ph, and NHS(&boxH;O)2CH2Ph.