QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
    33.
    发明申请
    QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS 失效
    喹诺酮衍生物作为激酶抑制剂

    公开(公告)号:US20100113468A1

    公开(公告)日:2010-05-06

    申请号:US12471280

    申请日:2009-05-22

    IPC分类号: A61K31/497

    摘要: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

    摘要翻译: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面,本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐,以及预防或治疗细胞增殖性疾病如动脉硬化,血管 重建,癌症和肾小球硬化症。

    Compositions and methods for inhibiting TGF-β
    35.
    发明授权
    Compositions and methods for inhibiting TGF-β 失效
    用于抑制TGF-β的组合物和方法

    公开(公告)号:US07189733B2

    公开(公告)日:2007-03-13

    申请号:US10795538

    申请日:2004-03-08

    CPC分类号: C07D471/04

    摘要: This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH═CH, CH═N, or N═CH; Z is N or C—F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.

    摘要翻译: 本发明提供可用于治疗患有TGF-β介导的疾病,特别是ALK5介导的疾病的患者的化合物。 化合物由式I表示:其中:ab是CH 2 CH 2 CH 2,CH 2 CH 2 CH 2 CH 2,CH-CH,CH-N或N-CH; Z是N或C-F; 和G为C 1-6脂族基或苯基,萘基或5-6元杂芳基环。

    Indazole peptidomimetics as thrombin receptor antagonists
    36.
    发明授权
    Indazole peptidomimetics as thrombin receptor antagonists 有权
    吲唑类似物作为凝血酶受体拮抗剂

    公开(公告)号:US07049297B2

    公开(公告)日:2006-05-23

    申请号:US10403218

    申请日:2003-03-31

    摘要: The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indazole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

    摘要翻译: 本发明涉及可用作治疗与血栓形成,再狭窄,高血压,心力衰竭,心律失常,炎症,心绞痛,中风,动脉粥样硬化,缺血性疾病,血管发生相关疾病,癌症相关的疾病的凝血酶受体拮抗剂的新型吲唑拟肽化合物 ,和神经变性疾病。 还公开了包含本发明的取代的吲唑肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。

    NITROGENOUS HETEROCYCLIC COMPOUNDS AND PROCESS FOR MAKING NITROGENOUS HETEROCYCLIC COMPOUNDS AND INTERMEDIATES THEREOF
    38.
    发明申请
    NITROGENOUS HETEROCYCLIC COMPOUNDS AND PROCESS FOR MAKING NITROGENOUS HETEROCYCLIC COMPOUNDS AND INTERMEDIATES THEREOF 失效
    氮杂环化合物和制备氮杂环化合物的方法及其中间体

    公开(公告)号:US20100240893A1

    公开(公告)日:2010-09-23

    申请号:US12622411

    申请日:2009-11-19

    IPC分类号: C07D295/215

    CPC分类号: C07D239/94

    摘要: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

    摘要翻译: 本发明提供含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 本发明还提供了可用于该方法的中间体化合物,以及通过该方法生产的最终产物及其盐或前药。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法,包括向有需要的患者施用有效量的本发明化合物。