6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    10.
    发明授权
    6-(aryl-amido or aryl-amidomethyl)-naphthalen-2-yloxy-acidic derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    6-(芳基 - 酰胺基或芳基 - 酰氨基甲基) - 萘-2-基氧基 - 酸性衍生物作为纤溶酶原激活物抑制剂1型抑制剂(PAI-1)

    公开(公告)号:US06589970B2

    公开(公告)日:2003-07-08

    申请号:US10170558

    申请日:2002-06-13

    IPC分类号: A61K31343

    摘要: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: 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 1 to 3 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 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or 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 or 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 or 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.

    摘要翻译: 本发明提供新的化合物,药物组合物和治疗哺乳动物血栓形成障碍的方法,具有下式的化合物:其中:Ar是苯基,萘基,呋喃基,苯并呋喃基,吲哚基,吡唑基,恶唑基,芴基,苯基环烷烃,其中环烷烃可以是环丙基 ,环丁基,环戊基或环己基,Ar可以任选被1至3个选自C 1 -C 6烷基,C 1 -C 6烷氧基,羟基,苯基 - (CH 2)0-6-,苯基 - (CH 2) ,C 3 -C 6环烷基, - (CH 2)-C 3 -C 6环烷基,卤素,C 1 -C 3全芳基烷基和C 1 -C 3全氟烷氧基,其中苯基可以被1至3个选自C 1 -C 6烷基,C 1 -C 6烷氧基, 苯基,卤素,三氟甲基或三氟甲氧基; R 1是氢,C 1 -C 6烷基或苯基 - (CH 2)1-6 - ,其中苯基可以被C 1 -C 6烷基,C 1 -C 6烷氧基,卤素,三氟甲基或三氟甲氧基取代; R 2和R 3是H,C 1 -C 6烷基,苯基 - (CH 2)0-3-,卤素和C 1 -C 3全氟烷基,其中苯基可以被C 1 -C 6烷基,C 1 -C 6烷氧基,卤素,三氟甲基或三氟甲氧基取代; R4是-CHR5CO2H或-CH2-四唑,其中R5是H或苄基; 并且n = 0或1; 或其药学上可接受的盐或酯形式。