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    NAPHTHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)
    1.
    发明公开
    NAPHTHYL BENZOFURAN DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) 审中-公开
    萘磺酸衍生物ALS PLASMINOGEN ACTIVATOR INHIBITOR-1（PAI-1）INHIBITOREN

    公开(公告)号：EP1401822A1

    公开(公告)日：2004-03-31

    申请号：EP02747904.7

    申请日：2002-06-18

    申请人： Wyeth

    发明人： ELOKDAH, Hassan, Mahmoud ,  MCFARLANE, Geraldine, Ruth ,  MAYER, Scott, Christian ,  CRANDALL, David, LeRoy

    IPC分类号： C07D307/79 ,  C07D405/12 ,  A61K31/34

    CPC分类号： C07D405/12 ,  C07D307/80

    摘要： This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula (1), wherein: R, R1, R2, and R3 are H, alkyl, cycloalkyl, -CH2-(cycloalkyl), alkanoyl, halo, hydroxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, perfluoroalkyl, alkoxy, amino, -NH(alkyl), -N(alkyl)2, or perfluoroalkoxy; R4 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl, aryl, -CH2R5, -CH(OH)R5, -C(O)R5, -CH(SH)R5, or -G(S)R5; R5 is H, alkyl, perflouroalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, alkenyl, alkenyl-aryl; R6 is H, alkyl, cycloalkyl, -CH2-cycloalkyl, alkylaryl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; n is an integer of 0-6; A is COOH, or an acid mimic; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds to treat or prevent conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis, and processes for the preparation of such compounds.

    6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1)
    4.
    发明公开
    6-(ARYL-AMIDO OR ARYL-AMIDOMETHYL)-NAPHTHALEN-2-YLOXY-ACIDIC DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 (PAI-1) 有权
    6-（ARYL-AMIDO ODER ARYL-AMIDOMETHYL）-NAPHTHOL-2-YLOXY-SURUREDERIVATE ALS INHIBITOREN DES PLASMINOGEN切割器抑制剂TYP-1（PAI-1）

    公开(公告)号：EP1397341A1

    公开(公告)日：2004-03-17

    申请号：EP02746561.6

    申请日：2002-06-18

    申请人： Wyeth

    发明人： COMMONS, Thomas, Joseph ,  CROCE, Susan, Christman ,  WOODWORTH, Richard Page ,  TRYBULSKI, Eugene, John ,  ELOKDAH, Hassan, Mahmoud ,  CRANDALL, David, LeRoy

    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

    CPC分类号： C07D403/12 ,  C07C233/73 ,  C07C235/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D231/14 ,  C07D307/68 ,  C07D307/84 ,  C07D307/85 ,  C07D405/12

    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.

    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; 和n = 0或1; 或其药学上可接受的盐或酯形式。