Patent ID: 6534651
Filing Date: 2003-03-18
Classification: A61P,C07D,C07H

Abstract:
A compound having the formula: or a pharmaceutically acceptable base or acid addition salt, hydrate, stereoisomer, or mixture thereof, wherein:R14 is hydroxy, â€”OCH3, â€”CH2NH2 or â€”Qâ€”Bâ€”D; Q is NHCO, NHCONH, O, OCO, NH, CH2NH or NHCOâ€”C1-C8 straight or branched chain alkylene; B is C1-C8 straight or branched chain alkylene, CH&boxH;CH, cyclohexyl, phenyl, C1-C2 straight or branched chain alkyl-NH, NH, phenylene, phenyl-CH2, phenyl-NHCO, Oâ€”CH2, â€”COâ€”, â€”CO2â€”, â€”CONHâ€”, â€”C(O)â€”C(O)â€”, â€”CONHCH2â€”, â€”NHCOâ€” or â€”(CF2)3â€”; D is hydrogen, halogen, hydroxy, cyclohexyl, C1-C10 straight or branched chain alkyl, â€”C1-C4 straight or branched chain alkyl-N(R18)2, â€”N(R18)2, â€”CH&boxH;CHCOOR19, â€”NHC(&boxH;NH)NH2, â€”NHC(&boxH;NH)Nâ€”COO-t-butyl, â€”COOR19, â€”NHCOR19, â€”CONHR18, phenyl, piperidinyl, anilinyl, piperazinyl, pyrolyl, imidazolyl, benzimidazolyl, tetrazolyl, indolyl, isoquinolinyl, quinolinyl, pyrrolidinyl, purinyl, pyrimidinyl, morpholinyl, thiophenyl, furanyl, isoindolinyl, pyridinyl, prolinyl or nipecotyl; R18 is hydrogen, methyl, ethyl, benzyl, cyclohexyl, â€”COO-t-butyl, C1-C2 alkylene-piperidinyl, C1-C2 alkylene-pyridinyl or C1-C2 alkylene-benzimidazolyl; and R19 is hydrogen, methyl, ethyl or â€”CH(NH-cyclohexyl)2; wherein each alkyl, alkylene, phenyl, phenylene, piperidinyl, purinyl, isoquinolinyl, indolyl or imidazolyl group is independently unsubstituted or substituted with one or more of the following groups: -halogen, methyl, ethyl, â€”OCH3, â€”COOH, â€”COOCH3, nitro, â€”N(CH3)2, â€”CH2-halo, â€”NHCOCH2-halo, NHCOCH2â€”N(CH3)2, â€”Oâ€”Si(CH3)2(t-butyl), â€”Oâ€”CH3, â€”OC(O)CH3, â€”COO-t-butyl or â€”CH2â€”NHâ€”COO-t-butyl.