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    Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors
    31.
    发明申请
    Thieno[3,2-b]pyridine-6-carbonitriles and thieno[2,3-b]pyridine-5-carbonitriles as protein kinase inhibitors 失效
    噻吩并[3,2-b]吡啶-6-羰腈和噻吩并[2,3-b]吡啶-5-腈作为蛋白激酶抑制剂

    公开(公告)号：US20040242883A1

    公开(公告)日：2004-12-02

    申请号：US10845710

    申请日：2004-05-14

    申请人： Wyeth

    发明人： Diane Harris Boschelli ,  Nan Zhang ,  Ana Carolina Barrios Sosa ,  Haris Durutlic ,  Biqi Wu

    IPC分类号： C07D498/02 ,  A61K031/4743

    CPC分类号： C07D495/04 ,  A61K31/44 ,  A61K31/497 ,  A61K31/535

    摘要： This invention provides compounds of Formula (1a)-(1f), II 1 wherein: X, m, n, q, R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, Q, Z, Znull, Znullnull, Znull and J are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, myocardial infarction, neuropathic pain, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant rejection and process for producing said compounds.

    摘要翻译： 本发明提供式（1a） - （1f），II的化合物，其中：X，m，n，q，R 1，R 2，R 3，R 4，R 5， R 6，R 7，R 8，R 9，Y，Q，Z，Z'，Z“'，Z”和J如上文在本说明书中所定义， 癌症，中风，心肌梗死，神经性疼痛，骨质疏松症，多囊肾病，自身免疫性疾病，类风湿性关节炎和移植排斥的治疗以及用于制备所述化合物的方法。

    Therapeutic compounds
    32.
    发明申请
    Therapeutic compounds 审中-公开
    治疗化合物

    公开(公告)号：US20040214815A1

    公开(公告)日：2004-10-28

    申请号：US10842044

    申请日：2004-05-07

    申请人： Pharmacia & Upjohn Company

    发明人： William W. McWhorter JR. ,  Valentina Badescu

    IPC分类号： A61K031/55 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/4743 ,  C07D498/02

    CPC分类号： C07D491/04

    摘要： The present invention provides compounds of formula (I): 1 wherein: R1, R2, R3 R4, R5, R6, X, - - - , m, and n have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts thereof. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I). The compounds are useful as 5-HT ligands.

    摘要翻译： 本发明提供式（I）化合物：其中：R1，R2，R3R4，R5，R6，X， - - ，m和n具有说​​明书中定义的任何值，以及包含 化合物或其盐。 本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。 该化合物可用作5-HT配体。

    Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents
    33.
    发明申请
    Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents 失效
    用作抗癌剂的双环嘧啶和嘧啶衍生物

    公开(公告)号：US20040171590A1

    公开(公告)日：2004-09-02

    申请号：US10479655

    申请日：2003-12-01

    发明人： Christopher Autry ,  Michael J Luzzio ,  Matthew A Marx

    IPC分类号： C07D498/02 ,  A61K031/519 ,  A61K031/4743

    CPC分类号： C07D495/04

    摘要： The invention relates to compounds of the formulas 1 and 2 and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R1 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.

    摘要翻译： 本发明涉及式1和2的化合物及其前药，所述化合物或所述前药的药学上可接受的盐或溶剂合物，其中X，R 1和R 11如本文所定义。 本发明还涉及含有式1和式2化合物的药物组合物以及通过施用式1和式2化合物来治疗哺乳动物中过度增殖性疾病的方法。

    Method of preventing or treating atherosclerosis or restenosis
    36.
    发明申请
    Method of preventing or treating atherosclerosis or restenosis 审中-公开
    预防或治疗动脉粥样硬化或再狭窄的方法

    公开(公告)号：US20040102473A1

    公开(公告)日：2004-05-27

    申请号：US10651216

    申请日：2003-08-28

    发明人： Michael W. Wathen ,  Lynne K. Wathen

    IPC分类号： A61K031/4743

    CPC分类号： A61K31/4743 ,  A61K31/435 ,  A61K31/4745

    摘要： The present invention provides a method of treating atherosclerosis or restenosis in a mammal which comprises administering to said mammal an effective amount of a compound selected from the group consisting of structures of Formulae I, Inull and II, 1 wherein the substituents on the Formulae are as defined herein.

    摘要翻译： 本发明提供治疗哺乳动物的动脉粥样硬化或再狭窄的方法，其包括向所述哺乳动物施用有效量的选自式I，I'和II结构的化合物，其中式中的取代基为 本文定义。

    Stabilized L-Arginine platelet aggregation inhibitory compositions and processes for making same
    37.
    发明申请
    Stabilized L-Arginine platelet aggregation inhibitory compositions and processes for making same 审中-公开
    稳定的L-精氨酸血小板聚集抑制组合物及其制备方法

    公开(公告)号：US20040092592A1

    公开(公告)日：2004-05-13

    申请号：US10291283

    申请日：2002-11-08

    发明人： Leonard L. Kaplan

    IPC分类号： A61K031/60 ,  A61K031/50 ,  A61K031/4743 ,  A61K031/198

    CPC分类号： A61K45/06 ,  A61K9/2009 ,  A61K33/06 ,  A61K2300/00

    摘要： Linking Magnesium ions to Nitric Oxide precursor L-Arginine, chemically 2-amino-5-guanidino valeric acid, with a platelet aggregation inhibitor compound such as, but not limited to acetylsalicylic acid or clopidogrel bisulfate, unexpectedly results in a pharmaceutically stabilized compositions with extended shelf life to be taken orally to provide gradual release vasodilatory and anti-platelet aggregation pharmacological activity with reduced potential for producing gastrointestinal lesions. L-Arginine releases ADNO (Arginine derived Nitric Oxide) in the coronary artery epithelium as EDRF (endothelium dependent relaxing factor) to dilate the arteries to promote blood flow to the myocardium, and the platelet aggregation inhibitor such acetylsalicylic acid or clopidogrel and others of this class of drugs inhibits or antagonizes the aggregation adhesion of platelets in the blood stream. Aggregated or clumped blood platelets contribute to arterial stenosis due to formation of atherosclerotic plaques that occlude coronary and other circulatory arteries. In addition to coronary arteries, atherosclerotic plaques can occlude and stenose carotid arteries and femoral arteries due to aggregated or clumped blood platelets, and the subject of this patent discovery will also be of cardiovascular health benefit respectively in preventing carotid cerebrovascular accidents and femoral artery leg circulation disease.

    摘要翻译： 将镁离子连接到一氧化氮前体L-精氨酸，化学式2-氨基-5-胍基丁酸与血小板聚集抑制剂化合物，例如但不限于乙酰水杨酸或硫酸氢氯吡格雷，意外地导致具有延长的药学上稳定的组合物 保质期要口服，提供逐渐释放血管扩张和抗血小板聚集的药理活性，降低产生胃肠道损伤的潜力。 L-精氨酸在冠状动脉上皮中释放ADNO（精氨酸衍生的一氧化氮），作为EDRF（内皮依赖性松弛因子），以扩张动脉以促进血液流向心肌，血小板聚集抑制剂如乙酰水杨酸或氯吡格雷等 药物类别抑制或拮抗血液中血小板的聚集粘附。 聚集或聚集的血小板由于形成阻塞冠状动脉和其他循环动脉的动脉粥样硬化斑块而导致动脉狭窄。 除了冠状动脉之外，动脉粥样硬化斑可以由于聚集或聚集的血小板而阻塞和狭窄颈动脉和股动脉，并且本专利发现的主题也将分别用于预防颈动脉脑血管意外和股动脉腿循环中的心血管健康益处 疾病。