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    Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
    8.
    发明授权
    Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation 失效
    吡啶并[2,3-D]嘧啶和4-氨基嘧啶作为细胞增殖抑制剂

    公开(公告)号：US06498163B1

    公开(公告)日：2002-12-24

    申请号：US09355681

    申请日：1999-08-02

    申请人： Diane Harris Boschelli ,  Annette Marian Doherty ,  Ali Fattaey ,  David William Fry ,  Susanne Andrea Trumpp-Kallmeyer ,  Zhipei Wu ,  Ellen Myra Dobrusin ,  Mark Robert Barvian

    发明人： Diane Harris Boschelli ,  Annette Marian Doherty ,  Ali Fattaey ,  David William Fry ,  Susanne Andrea Trumpp-Kallmeyer ,  Zhipei Wu ,  Ellen Myra Dobrusin ,  Mark Robert Barvian

    IPC分类号： A61K31519

    CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D471/04

    摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 2,4-diaminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula I: and Formula II: where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R8 and R9 include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula I or II together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.

    摘要翻译： 本发明提供可用于治疗细胞增殖性疾病如癌症和再狭窄的吡啶并嘧啶和4-氨基嘧啶。 我们现在已经发现了一组7,8-二氢-2-（氨基和硫代）吡啶并[2,3-d]嘧啶和2,4-二氨基嘧啶，其是细胞周期蛋白依赖性激酶（cdks）和生长因子的有效抑制剂 介导的激酶。 这些化合物很容易合成，并且可以通过多种途径施用，包括口服，并具有足够的生物利用度。 本发明提供式I化合物和式II化合物：其中W是NH，S，SO或SO 2，R 1包括苯基和取代的苯基，R 2包括烷基和环烷基，R 3包括烷基和氢，R 8和R 9包括氢和烷基， 并且Z是羧基。本发明还提供了包含式I或II化合物及其药学上可接受的载体，稀释剂或赋形剂的药物制剂。