发明授权
EP1397341B1 6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1)
有权
6-(芳基酰氨基,或芳基 - 酰氨基甲基)萘酚-2-基氧基酸衍生物纤溶酶原激活物抑制物-1(PAI-1)的抑制剂
- 专利标题: 6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1)
- 专利标题(中): 6-(芳基酰氨基,或芳基 - 酰氨基甲基)萘酚-2-基氧基酸衍生物纤溶酶原激活物抑制物-1(PAI-1)的抑制剂
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申请号: EP02746561.6申请日: 2002-06-18
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公开(公告)号: EP1397341B1公开(公告)日: 2008-08-06
- 发明人: COMMONS, Thomas, Joseph , CROCE, Susan, Christman , WOODWORTH, Richard Page , TRYBULSKI, Eugene, John , ELOKDAH, Hassan, Mahmoud , CRANDALL, David, LeRoy
- 申请人: Wyeth
- 申请人地址: Five Giralda Farms Madison, NJ 07940-0874 US
- 专利权人: Wyeth
- 当前专利权人: Wyeth
- 当前专利权人地址: Five Giralda Farms Madison, NJ 07940-0874 US
- 代理机构: Bradley, Adrian
- 优先权: US299652P 20010620; US308656P 20010730
- 国际公布: WO2003000649 20030103
- 主分类号: C07C233/75
- IPC分类号: C07C233/75 ; C07D307/84 ; C07D307/68 ; C07D263/34 ; C07D257/04 ; C07D209/42 ; C07D231/14 ; C07D405/12 ; C07D403/12 ; C07D413/12 ; C07D307/85 ; A61P7/02 ; A61K31/195 ; A61K31/196 ; A61K31/341 ; A61K31/343 ; A61K31/422 ; A61K31/41 ; A61K31/404 ; A61K31/415
摘要:
This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula (I), wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by one or more groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6-, phenyl-(CH2)0-6O-,C3-C6 cycloalkyl, -(CH2)-C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from one or more groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl and trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6- where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3-, halo and C1-C3 perfluoroalkyl where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl and trifluoromethoxy; R4 is -CHR5CO2H or -CH2-tetrazole where R5 is H or benzyl; and n = 0 or 1; or a pharmaceutically acceptable salt or ester form thereof.
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