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41 条记录 (耗时 0.042 秒)

    Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
    31.
    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。

    N-oxides of amino containing pyrido �2,3-D! pyrimidines
    35.
    发明授权
    N-oxides of amino containing pyrido �2,3-D! pyrimidines 失效
    含有吡啶并[2,3-D]嘧啶的氨基氧化物

    公开(公告)号：US5945422A

    公开(公告)日：1999-08-31

    申请号：US15739

    申请日：1998-01-29

    申请人： Annette Marian Doherty ,  Hussein Osman Hallak ,  James Marino Hamby

    发明人： Annette Marian Doherty ,  Hussein Osman Hallak ,  James Marino Hamby

    IPC分类号： C07D471/04 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： N-oxides of amino containing 6-aryl pyrido�2,3-d!-pyrimidine 7-imines, 7-ones, and 7-thiones have the formula ##STR1## where A and B are linkers, Ar is aryl, R.sub.2 is aklyl, X is O, S, or NH, or NAcyl, and R.sub.5 and R.sub.6 are alkyl. The compounds are inhibitors of protein tyrosine kinases and cyclin-dependent kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

    摘要翻译： 含有6-芳基吡啶并[2,3-d] - 嘧啶-7-亚胺，7-酮和7-硫代氨基的氨基氧化物具有下式，其中A和B为连接基，Ar为芳基，R 2为甲酰基，X 是O，S或NH，或NAcyl，R5和R6是烷基。 这些化合物是蛋白酪氨酸激酶和细胞周期蛋白依赖性激酶的抑制剂，因此可用于治疗由此介导的细胞增殖。 该化合物特别可用于治疗癌症，动脉粥样硬化，再狭窄和牛皮癣。

    Endothelin antagonists
    40.
    发明授权
    Endothelin antagonists 失效
    内皮素拮抗剂

    公开(公告)号：US5922681A

    公开(公告)日：1999-07-13

    申请号：US945316

    申请日：1992-09-14

    申请人： Annette Marian Doherty ,  David Charles Rees

    发明人： Annette Marian Doherty ,  David Charles Rees

    IPC分类号： A61K38/00 ,  C07K5/065 ,  C07K5/078 ,  C07K5/06

    CPC分类号： C07K5/06078 ,  C07K5/06156 ,  A61K38/00

    摘要： Antagonists of endothelin are described, as well as methods of using them and pharmaceutical compositions containing them. These compounds are useful in controlling hypertension, myocardial infarction, pulmonary hypertension, angina, metabolic, endocrinological, and neurological disorders, congestive heart failure, septic or endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, acute and chronic renal failure, preeclampsia, and diabetes.

    摘要翻译： 描述了内皮素的拮抗剂，以及使用它们的方法和含有它们的药物组合物。 这些化合物可用于控制高血压，心肌梗塞，肺动脉高压，心绞痛，代谢，内分泌和神经障碍，充血性心力衰竭，脓毒性或内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，急性和慢性肾衰竭，先兆子痫和糖尿病 。