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Heterocycle substituted purine derivatives as potent antiproliferative agents

机译:杂环取代的嘌呤衍生物作为有效的抗增殖剂

摘要

The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of human cellular proliferation. As such, the compounds of the present invention constitute pharmaceutical compositions with a pharmaceutically acceptable carrier. Such compounds are useful in treating a disorder mediated by elevated levels of cell proliferation in a mammal compared to a healthy mammal by administering to such mammal an effective amount of the compound. Examples of the compounds of the present invention are represented by the following chemical structures: embedded image;wherein:;V;NH;;O;;S; or;CH2;;R7 is a heterocycle selected from the group consisting of:;thiophene;;furan;;pyrrole;;thiazole;;pyrazole;;imidazole;;isoxazole;;isothiazole; and;1,3,4-thiadiazole;;and Y, A, R1, R2, R3, R4, and n1 are defined herein.
机译:本发明的化合物是2,6,9-三取代的嘌呤衍生物,它们是细胞周期蛋白/ cdk复合物的抑制剂。本发明的化合物也是人细胞增殖的有效抑制剂。这样,本发明的化合物与药学上可接受的载体一起构成药物组合物。与健康哺乳动物相比,通过向此类哺乳动物施用有效量的化合物,此类化合物可用于治疗哺乳动物细胞增殖水平升高所介导的疾病。本发明化合物的实例由以下化学结构表示:<化学ID =“ CHEM-US-00001”> <图像alt =“嵌入式图像” file =“ US06812232-20041102-C00001.GIF” he =“ 244.34865“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 127.4616“ /> ;其中:; V; NH ;; O ;; S;或; CH 2 ;; R 7 是选自以下的杂环:噻吩;呋喃;吡咯;噻唑;吡唑;咪唑;或;异恶唑;;异噻唑;和; 1,3,4-噻二唑;和Y,A,R 1 ,R 2 ,R 3 ,R 这里定义4 和n 1

著录项

  • 公开/公告号US6812232B2

    专利类型

  • 公开/公告日2004-11-02

    原文格式PDF

  • 申请/专利权人 AMR TECHNOLOGY INC.;

    申请/专利号US20020237530

  • 发明设计人 MICHAEL PETER TROVA;

    申请日2002-09-06

  • 分类号C07D4731/60;C07D4732/40;C07D4733/40;C07D4731/80;A61K315/20;

  • 国家 US

  • 入库时间 2022-08-21 23:18:29

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