NOVEL INDAZOLE PEPTIDOMIMETICS AS THROMBIN RECEPTOR ANTAGONISTS
    23.
    发明申请
    NOVEL INDAZOLE PEPTIDOMIMETICS AS THROMBIN RECEPTOR ANTAGONISTS 审中-公开
    新型吲哚美辛作为硫蛋白受体拮抗剂

    公开(公告)号:WO0100656A3

    公开(公告)日:2001-05-25

    申请号:PCT/US0017718

    申请日:2000-06-28

    CPC classification number: C07K5/06078 A61K31/416 A61K38/00

    Abstract: 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.

    Abstract translation: 本发明涉及新颖的吲唑拟肽化合物,其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,缺血性病症,血管发生相关疾病,癌症相关的疾病的凝血酶受体拮抗剂 ,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。

    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    26.
    发明申请
    PHARMACEUTICAL PYRAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
    用作蛋白激酶抑制剂的药用吡唑组合物

    公开(公告)号:WO9614843A3

    公开(公告)日:1996-05-23

    申请号:PCT/US9514723

    申请日:1995-11-09

    CPC classification number: A61K31/455 A61K31/415 A61K31/4155 A61K31/4439

    Abstract: A method for selectively inhibiting a kinase is disclosed, which comprises contacting a composition containing a kinase with a compound of formula (I), wherein: R1 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, polyaromatic, polyaromatic carbonyl, polyheteroaromatic or polyheteroaromatic carbonyl; R2 is lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, lower hydrocarboyl, 5- or 6-membered heterocyclic aromatic carbonyl, polyaromatic or polyheteroaromatic; R3 is H or lower alkyl; R5 is H, lower alkyl, lower hydrocarbyl, aryl lower alkyl, heteroaryl lower alkyl, 5- or 6-membered heterocyclic aromatic, halogen, or cyano; and R6 is H or lower hydrocarboyl. 00000

    Abstract translation: 公开了选择性抑制激酶的方法,其包括将含有激酶的组合物与式(I)化合物接触,其中:R 1是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6- 多芳基,多芳基羰基,多杂芳基或多杂芳基羰基; R 2是低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,低级烃基,5-或6-元杂环芳族羰基,多芳族或多杂芳族; R3是H或低级烷基; R5是H,低级烷基,低级烃基,芳基低级烷基,杂芳基低级烷基,5-或6-元杂环芳族,卤素或氰基; R6为H或低级烃基。 00000

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