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    2,4-dioxo-3-quinazolinylaryl sulfonylureas
    9.
    发明授权
    2,4-dioxo-3-quinazolinylaryl sulfonylureas 失效
    2,4-二氧代-3-喹唑啉基芳基磺酰脲

    公开(公告)号：US07109332B2

    公开(公告)日：2006-09-19

    申请号：US10956004

    申请日：2004-09-29

    申请人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    发明人： Robert M. Scarborough ,  Wolin Huang ,  Anjali Pandey ,  Shawn M. Bauer ,  Xiaoming Zhang ,  Zhaozhong J. Jia

    IPC分类号： C07D409/12 ,  C07D409/14 ,  A61K31/517 ,  A61P7/02

    CPC分类号： C07D409/12 ,  C07D409/14

    摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 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.

    摘要翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物，其具有下式：其中R是选自H和C 1-6烷基的成员; R 1是选自H，C 1-6烷基，C 1-6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基， 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H，卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6烷基， C 1-6烷基，C 1-6烷氧基，氰基和-C（O）R 2a， 其中R 2a是选自C 1-6烷氧基和（C 1-6烷基）烷基的成员， 0-2氨基; L是选自-CH 2 - ， - CH（CH 3 CH 3） - ， - CH 2 - ， - CH 2 CH 2（CH 3 CH 3） - 和-CH 2 CH 2 CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。 和Ar 1是选自苯，吡啶和嘧啶的芳环; 被提供。 该化合物可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓相关病症或病症中。

    Platelet ADP receptor inhibitors
    10.
    发明授权
    Platelet ADP receptor inhibitors 有权
    血小板ADP受体抑制剂

    公开(公告)号：US06689786B2

    公开(公告)日：2004-02-10

    申请号：US10350883

    申请日：2003-01-23

    申请人： Robert M. Scarborough ,  Wolin Huang

    发明人： Robert M. Scarborough ,  Wolin Huang

    IPC分类号： C07D41712

    CPC分类号： C07D239/22 ,  C07D239/48 ,  C07D239/50 ,  C07D333/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04

    摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives 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 relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。