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11 条记录 (耗时 0.035 秒)

    7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives useful as antagonists of gonadotropin releasing hormone
    2.
    发明授权
    7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives useful as antagonists of gonadotropin releasing hormone 有权
    7-杂环喹啉和噻吩并[2,3-b]吡啶衍生物，可用作促性腺激素释放激素的拮抗剂

    公开(公告)号：US06765011B2

    公开(公告)日：2004-07-20

    申请号：US10406393

    申请日：2003-04-03

    申请人： Zhihua Sui ,  Mark Macielag ,  James C. Lanter

    发明人： Zhihua Sui ,  Mark Macielag ,  James C. Lanter

    IPC分类号： A61K314365

    CPC分类号： C07D405/04 ,  C07D409/04 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

    摘要： The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.

    摘要翻译： 本发明涉及通式（I）或（II）的新型7-杂环基喹啉和噻吩并[2,3-b]吡啶衍生物，其中所有变量如本文所定义，含有它们的药物组合物及其在 治疗与促性腺激素释放激素（GnRH）相关的疾病和病症。 本发明的化合物是GnRH的拮抗剂，可用于治疗不育症，前列腺癌，良性前列腺增生症（BPH）和避孕药。

    Thienopyridine derivatives, their production and use
    3.
    发明授权
    Thienopyridine derivatives, their production and use 失效
    噻吩并吡啶衍生物，其生产和使用

    公开(公告)号：US06653476B2

    公开(公告)日：2003-11-25

    申请号：US10204593

    申请日：2002-08-22

    申请人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    发明人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    IPC分类号： A61K314365

    CPC分类号： C07D495/04 ,  C07D495/14

    摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.

    摘要翻译： 本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。 噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

    IL-8 receptor antagonists
    4.
    发明授权
    IL-8 receptor antagonists 失效
    IL-8受体拮抗剂

    公开(公告)号：US06440993B1

    公开(公告)日：2002-08-27

    申请号：US09806119

    申请日：2001-03-29

    申请人： Katherine L. Widdowson

    发明人： Katherine L. Widdowson

    IPC分类号： A61K314365

    CPC分类号： C07D513/04

    摘要： A compound of the formula: wherein R1 and R1 and m are as defined in the specification.

    摘要翻译： 下式的化合物：其中R1和R1和m如说明书中所定义

    Allosteric adenosine receptor modulators
    5.
    发明授权
    Allosteric adenosine receptor modulators 失效
    变构腺苷受体调节剂

    公开(公告)号：US06177444B1

    公开(公告)日：2001-01-23

    申请号：US09307225

    申请日：1999-05-07

    申请人： Pier Giovanni Baraldi

    发明人： Pier Giovanni Baraldi

    IPC分类号： A61K314365

    CPC分类号： C07D495/04 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4365 ,  C07D333/36 ,  C07D333/66 ,  C07D333/78

    摘要： The present invention relates to compounds of formulas (IA), (IB), and (IC): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

    摘要翻译： 本发明涉及式（IA），（IB）和（IC）的化合物：其制备方法，其药物组合物及其在药物中的用途，其用作包括保护免受缺氧和缺血诱导的损伤的变应性腺苷受体调节剂， 治疗腺苷敏感性心律失常。

    Substituted 2,4-dihydro-pyrrolo[3,4-b]quinolin-9-one derivatives useful as phosphodiesterase inhibitors
    6.
    发明授权
    Substituted 2,4-dihydro-pyrrolo[3,4-b]quinolin-9-one derivatives useful as phosphodiesterase inhibitors 有权
    用作磷酸二酯酶抑制剂的取代的2,4-二氢 - 吡咯并[3,4-b]喹啉-9-酮衍生物

    公开(公告)号：US06800625B2

    公开(公告)日：2004-10-05

    申请号：US10463941

    申请日：2003-06-17

    申请人： Weiqin Jiang ,  Zhihua Sui

    发明人： Weiqin Jiang ,  Zhihua Sui

    IPC分类号： A61K314365

    CPC分类号： C07D471/04

    摘要： The invention relates to novel 2,4-dihydro-pyrrolo[3,4-b]quinolin-9-one derivatives of the formula (I) and (IV): wherein all variables are as herein defined, pharmaceutical compositions containing the compounds and their use for the treatment of sexual dysfunction.

    摘要翻译： 本发明涉及式（I）和（IV）的新型2,4-二氢 - 吡咯并[3,4-b]喹啉-9-酮衍生物：其中所有变量如本文所定义，含有化合物的药物组合物和 它们用于治疗性功能障碍。

    Acid addition salts of hydropyridine derivatives
    7.
    发明授权
    Acid addition salts of hydropyridine derivatives 失效
    氢化吡啶衍生物的酸加成盐

    公开(公告)号：US06693115B2

    公开(公告)日：2004-02-17

    申请号：US10329629

    申请日：2002-12-26

    申请人： Fumitoshi Asai ,  Taketoshi Ogawa ,  Hideo Naganuma ,  Naotoshi Yamamura ,  Teruhiko Inoue ,  Kazuyoshi Nakamura

    发明人： Fumitoshi Asai ,  Taketoshi Ogawa ,  Hideo Naganuma ,  Naotoshi Yamamura ,  Teruhiko Inoue ,  Kazuyoshi Nakamura

    IPC分类号： A61K314365

    CPC分类号： C07D495/04

    摘要： Acid addition salts of 2-acetoxy-5-(&agr;-cyclopropyl-carbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]-pyridine. The acid addition salts of tetrahydrothienopyridine derivatives of the present invention exhibit excellent oral absorption, metabolization into the active compound, and platelet aggregation-inhibiting effects, low toxicity, and excellent storage and handling stabilities, and are useful as medicaments, preferably preventive or therapeutic agents (particularly therapeutic agents) for diseases caused by a thrombus or an embolus, still more preferably preventive or therapeutic agents (particularly therapeutic agents) for thrombosis or embolism.

    摘要翻译： 2-乙酰氧基-5-（α-环丙基 - 羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c] - 吡啶的酸加成盐。 本发明的四氢噻吩并吡啶衍生物的酸加成盐表现出优异的口服吸收，代谢成活性化合物，抑制血小板聚集作用，毒性低，储存和处理稳定性优异，可用作药物，优选预防或治疗剂 （特别是治疗剂），还优选用于血栓形成或栓塞的预防或治疗剂（特别是治疗剂）。