Spirocyclic molecules as protein kinase inhibitors
    42.
    发明授权
    Spirocyclic molecules as protein kinase inhibitors 有权
    螺环分子作为蛋白激酶抑制剂

    公开(公告)号:US09226923B2

    公开(公告)日:2016-01-05

    申请号:US14234586

    申请日:2012-07-26

    摘要: The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers. R2 is selected from

    摘要翻译: 本发明涉及式I的螺环化合物,即具有蛋白激酶抑制性的螺环(1H-吡唑-4-基)-3-(1-(2,6-二氯-3-氟苯基)乙氧基)吡啶-2-胺 活性,以及​​合成和使用这些化合物的方法。 优选的化合物是用于治疗异常细胞生长的c-Met和/或ALK抑制剂,例如癌症。 R2选自

    Indole derivatives as CRTH2 receptor antagonists
    44.
    发明授权
    Indole derivatives as CRTH2 receptor antagonists 有权
    吲哚衍生物作为CRTH2受体拮抗剂

    公开(公告)号:US07696222B2

    公开(公告)日:2010-04-13

    申请号:US11990378

    申请日:2006-08-07

    申请人: Zhaoyin Wang

    发明人: Zhaoyin Wang

    CPC分类号: C07D471/04 C07D487/04

    摘要: Compounds according to formula (I) wherein the radicals R1, R2 and R3 are as herein defined, and wherein Ar represents an aryl group or heteroaryl group, preferably phenyl, n is 1 or 2, and the radical X represents a group selected from —C(Ra)(Rb)—, —C(Ra)(Rb)—C(Ra)(Rb)—, —C(Ra)═C(Ra)—, OC(Ra)(Rb)— or SC(Ra)(Rb)—. These compounds and their pharmaceutical acceptable salts are used in pharmaceutical compositions as prostaglandine D2 receptor antagonists useful in the treatment of CRTH2-mediated diseases such as respiratory, inflammatory or allergic conditions among others.

    摘要翻译: 根据式(I)的化合物,其中基团R 1,R 2和R 3如本文所定义,并且其中Ar表示芳基或杂芳基,优选苯基,n为1或2,基团X表示选自 - C(Ra)(Rb) - ,-C(Ra)(Rb)-C(Ra)(Rb) - ,-C(Ra)= C(Ra) - ,OC Ra)(Rb) - 。 这些化合物及其药学上可接受的盐在药物组合物中用作可用于治疗CRTH2介导的疾病如呼吸道,炎性或过敏性疾病等的前列腺素D2受体拮抗剂。

    Nitric oxide releasing prodrugs of diaryl-2-(5H)-furanones as cyclooxygenase-2 inhibitors
    46.
    发明授权
    Nitric oxide releasing prodrugs of diaryl-2-(5H)-furanones as cyclooxygenase-2 inhibitors 失效
    二芳基-2-(5H) - 呋喃酮作为环加氧酶-2抑制剂的一氧化氮释放前药

    公开(公告)号:US07169809B2

    公开(公告)日:2007-01-30

    申请号:US10790288

    申请日:2004-03-01

    IPC分类号: A61K31/21

    CPC分类号: C07C317/46

    摘要: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.

    摘要翻译: 本发明包括式I的新化合物,其是可用于治疗环氧合酶-2介导的疾病的二芳基-2-(5H)呋喃酮的一氧化氮释放前药。 本发明还包括用于治疗环加氧酶-2介导的疾病的某些药物组合物和方法,其包括使用式I化合物。上述化合物可用作与低剂量阿司匹林联合治疗以治疗慢性环氧合酶-2介导的疾病或病症 同时也降低血栓性心血管事件的风险。