Factor Xa inhibitors
    9.
    发明授权
    Factor Xa inhibitors 有权
    因子Xa抑制剂

    公开(公告)号:US07767697B2

    公开(公告)日:2010-08-03

    申请号:US12166944

    申请日:2008-07-02

    IPC分类号: A61K31/4412 C07D401/14

    摘要: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

    摘要翻译: 本发明涉及作为因子Xa抑制剂的式(I)化合物及其药学上可接受的盐,酯和前药。 本发明还涉及用于制备这种化合物的中间体,含有这种化合物的药物组合物,预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

    2,4-dioxo-3-quinazolinylaryl sulfonylureas
    10.
    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

    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。