申请人:——
公开号:US20040198766A1
公开(公告)日:2004-10-07
The present invention is related to aza-oxindole derivatives formula (I), wherein X is N and Z is CH
i
o; X is CH and Z is N
i
, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
1
本发明涉及aza-oxindole衍生物的公式(I),其中X为N且Z为CHio; X为CH且Z为Ni,包含相同的组合物,以及使用和制造相同的方法。这些化合物通常在药理学上有用,作为那些通过改变一般的有丝分裂原活化信号通路或者特别是抑制或拮抗蛋白激酶所涉及的病理性细胞增殖而缓解的疾病状态的药剂。这些疾病状态包括肿瘤生长、再狭窄、动脉粥样硬化、疼痛和血栓形成。特别地,本发明涉及一系列取代的oxindole化合物,这些化合物表现出Trk家族蛋白酪氨酸激酶抑制作用,对癌症治疗和慢性疼痛指标有用。