Factor IXa inhibitors
    1.
    发明授权

    公开(公告)号:US09708308B2

    公开(公告)日:2017-07-18

    申请号:US14652237

    申请日:2013-12-16

    摘要: The present invention provides a compound of Formula (I) wherein R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is 1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or 2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; and B is 1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or 2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses.

    MINERALOCORTICOID RECEPTOR ANTAGONISTS
    5.
    发明申请
    MINERALOCORTICOID RECEPTOR ANTAGONISTS 有权
    矿物胆碱受体拮抗剂

    公开(公告)号:US20150182503A1

    公开(公告)日:2015-07-02

    申请号:US14415210

    申请日:2013-07-15

    IPC分类号: A61K31/416 C07D231/56

    摘要: The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

    摘要翻译: 本发明涉及可用于治疗醛固酮介导的疾病的式I化合物及其药学上可接受的盐。 本发明还涉及该化合物的具体非对映异构体和对映异构体,制备式I化合物的方法,以及其用于治疗和预防上述疾病和用于制备用于此目的的药物的潜在用途,以及药物组合物 其包含式I的化合物。

    Factor IXa Inhibitors
    8.
    发明申请
    Factor IXa Inhibitors 有权
    因子IXa抑制剂

    公开(公告)号:US20150329562A1

    公开(公告)日:2015-11-19

    申请号:US14652174

    申请日:2013-12-16

    IPC分类号: C07D513/04 C07D413/14

    摘要: The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

    摘要翻译: 本发明提供式(I)的化合物,其中R 1,R 2,R 3和R 4独立地为H或C 1-6烷基,条件是当R 1,R 2和R 3为H时,R 4为C 1-6烷基, 中,R 2和R 4为H,R 3为C 1-6烷基,当R 1,R 3和R 4为H时,R 2为C 1-6烷基,当R 2,R 3和R 4为H时,R为C 1-6烷基 ; 和包含一种或多种所述化合物的药物组合物,以及使用所述化合物治疗或预防血栓形成,栓塞,高凝状态或纤维化改变的方法。