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    16.
    发明专利
    未知

    公开(公告)号：AT448222T

    公开(公告)日：2009-11-15

    申请号：AT04789522

    申请日：2004-09-29

    Applicant: PORTOLA PHARM INC

    Inventor： SCARBOROUGH ROBERT ,  HUANG WOLIN ,  PANDEY ANJALI ,  BAUER SHAWN ,  ZHANG XIAOMING ,  JIA ZHAOZHONG

    IPC: C07D409/12 ,  A61K20060101 ,  A61K31/517 ,  A61P7/02 ,  C07D409/14

    Abstract: 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C 1-6 alkyl; R 1 is a member selected from the group consisting of H, C 1-6 alkyl, C 1-6 haloalkyl, C 3-5 cycloalkyl and C 3-5 cycloalkyl-alkyl; R 2 is a member selected from the group consisting of H, halogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 haloalkyl, C 1-6 alkoxy, cyano and -C(O)R 2a , wherein R 2a is a member selected from the group consisting of C 1-6 alkoxy and (C 1-6 alkyl) 0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of -CH 2 -, -CH(CH 3 )-, -CH 2 CH 2 -, -CH 2 CH(CH 3 )- and -CH 2 CH 2 CH 2 -; L 1 is a linking group selected from the group consisting of a bond and -CH 2 -; L 2 is a linking group selected from the group consisting of a bond, -NH- and -CH 2 -; and Ar 1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.

    19.
    发明专利
    未知

    公开(公告)号：HK1121051A1

    公开(公告)日：2009-04-17

    申请号：HK09100322

    申请日：2009-01-13

    Applicant: PORTOLA PHARM INC

    Inventor： HUANG WOLIN ,  MEHROTRA MUKUND ,  ZHANG XIAOMING ,  CANNON HILARY ,  GRANT CRAIG M ,  SCARBOROUGH ROBERT M

    IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101

    Abstract: The present invention provides novel sulfonylurea compounds of formula (I) and pharmaceutically acceptable derivatives and polymorph and amorphous forms thereof. The compounds in their various forms are effective platelet ADP receptor inhibitors and may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also provides a method for preparing such compounds and forms and for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or forms thereof.

    [4-(6-HALO-7-SUSTITUIDO-2,4-DIOXO-1,4-DIHIDRO-2H-QUINAZOLIN-3-IL)-FENIL]-5-CLORO-TIOFEN-2-IL-SULFONILUREAS Y FORMAS Y METODOS RELACIONADOS CON LAS MISMAS
    20.
    发明专利
    [4-(6-HALO-7-SUSTITUIDO-2,4-DIOXO-1,4-DIHIDRO-2H-QUINAZOLIN-3-IL)-FENIL]-5-CLORO-TIOFEN-2-IL-SULFONILUREAS Y FORMAS Y METODOS RELACIONADOS CON LAS MISMAS 未知

    公开(公告)号：PE20081115A1

    公开(公告)日：2008-08-15

    申请号：PE2006001439

    申请日：2006-11-13

    Applicant: PORTOLA PHARM INC

    Inventor： SCARBOROUGH ROBERT M ,  HUANG WOLIN ,  MEHROTRA MUKUND ,  ZHANG XIAOMING ,  CANNON HILARY ,  GRANT CRAIG M

    IPC: A61K31/517 ,  C07D409/02

    Abstract: SE REFIERE A COMPUESTOS DERIVADOS DE SULFONILUREAS DE FORMULA (I) DONDE X ES F O I; R1 ES H, HALOGENO, OH, ALQUILO(C1-C10) O ALQUILAMINO(C1-C6); SIENDO UN COMPUESTO PREFERIDO [4-(6-FLUOR-7-METILAMINO-2,4-DIOXO-1,4-DIHIDRO-2H-QUINAZOLIN-3-IL)-FENIL]-5-CLORO-TIOFEN-2-IL-SULFONILUREA. SE REFIERE TAMBIEN A FORMAS CRISTALINAS DE DICHOS COMPUESTOS TALES COMO: A) LA FORMA CRISTALINA A QUE SE CARACTERIZA POR UN ESPECTRO INFRARROJO DE PICOS DE ABSORCION EN 3559, 3389, 3324, 1698, 1623, 1563, 1510, 1448, 1403, 1383, 1308, 1269, 1206, 1174, 1123, 1091, 1072, 1030, 987, 939, 909, 871, 842, 787, 780, 769, 747, 718, 701, 690 Y 667 cm-1; B) LA FORMA CRISTALINA B QUE SE CARACTERIZA POR UN ESPECTRO INFRARROJO DE PICOS DE ABSORCION EN 3584, 3327, 3189, 2935, 2257, 2067, 1979, 1903, 1703, 1654, 1630, 1590, 1557, 1512, 1444, 1429, 1406, 1375, 1317, 1346, 1317, 1288, 1276, 1243, 1217, 1182, 1133, 1093, 1072, 1033, 987 cm-1, ENTRE OTROS; Y C) UNA FORMA AMORFA. SE REFIERE TAMBIEN A PROCEDIMIENTOS DE PREPARACION DE LAS FORMAS CRISTALINAS Y A COMPOSICIONES FARMACEUTICAS DE LOS COMPUESTOS DE FORMULA (I) Y DE LAS FORMAS CRISTALINAS. DICHOS COMPUESTOS SON INHIBIDORES DE LOS RECEPTORES DE ADENOSINA 5'-DIFOSFATO (ADP) PLAQUETARIOS SIENDO UTILES EN EL TRATAMIENTO DE TROMBOSIS, INFARTO DE MIOCARDIO AGUDO, ANGINA, ACCIDENTES CEREBROVASCULARES, EMBOLISMO

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