利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

38 条记录 (耗时 0.067 秒)

    CRF receptor antagonists and methods relating thereto
    21.
    发明授权
    CRF receptor antagonists and methods relating thereto 失效
    CRF受体拮抗剂及其相关方法

    公开(公告)号：US06541469B2

    公开(公告)日：2003-04-01

    申请号：US09861472

    申请日：2001-05-18

    申请人： Mustapha Haddach

    发明人： Mustapha Haddach

    IPC分类号： A61K31542

    CPC分类号： C07D487/16 ,  C07D498/16

    摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein X is nitrogen or CR3; A is O, S, or NR4, and R, R1, R2are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

    摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：包括立体异构体及其药学上可接受的盐，其中X为氮或CR 3; A是O，S或NR4，R，R1，R2如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

    Pyrazolopyrimidines and related heterocycles as kinase inhibitors
    25.
    发明授权
    Pyrazolopyrimidines and related heterocycles as kinase inhibitors 有权
    吡唑并嘧啶和相关杂环作为激酶抑制剂

    公开(公告)号：US08367681B2

    公开(公告)日：2013-02-05

    申请号：US12784271

    申请日：2010-05-20

    申请人： Mustapha Haddach ,  Joe Tran

    发明人： Mustapha Haddach ,  Joe Tran

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.

    摘要翻译： 本发明提供抑制选择的激酶（Pim和/或CK2激酶）的通式（I）化合物和含有这些化合物的组合物。 这些化合物和组合物可用于治疗增殖性疾病如癌症，以及其它激酶相关病症，包括炎症，疼痛以及某些感染和免疫学疾病。

    COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS
    27.
    发明申请
    COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS 审中-公开
    包含5-LIPOXYGENASE激活蛋白抑制剂和硝酸氧化物调节剂的组合物和治疗

    公开(公告)号：US20100068301A1

    公开(公告)日：2010-03-18

    申请号：US12517166

    申请日：2007-11-30

    申请人： John H. Hutchinson ,  Mustapha Haddach ,  Mark Moran ,  Jillian Evans ,  Nicholas Simon Stock ,  Jeffrey Roger Roppe

    发明人： John H. Hutchinson ,  Mustapha Haddach ,  Mark Moran ,  Jillian Evans ,  Nicholas Simon Stock ,  Jeffrey Roger Roppe

    IPC分类号： A61K31/4709 ,  A61K31/404 ,  C07D401/12 ,  A61K33/26 ,  A61K31/04 ,  A61K31/34 ,  A61K31/195 ,  A61K31/7076 ,  A61K38/08 ,  A61P9/12

    CPC分类号： A61K45/06 ,  A61K31/195 ,  A61K31/404 ,  A61K31/47 ,  A61K2300/00

    摘要： Disclosed herein are compositions and compounds that combine an inhibitor of 5-lipoxygenase activating protein (FLAP) and a modulator of NO levels in a mammal. The NO modulator can be an agent that induces the production of NO in a mammal, or can be an agent that itself produces NO in the mammal. Further disclosed herein are strategies for synthesizing such compounds, and methods for testing whether the combination compounds and compositions provide a desired benefit. Also disclosed herein are pharmaceutical compositions and formulations that combine a FLAP inhibitor and an NO modulator. Further described herein are methods for using such compositions and compounds for the treatment of diseases, conditions, and disorders in a mammal, including a human. Such treatment methods include the separate administration of a FLAP inhibitor and a NO modulator to the mammal, and the simultaneous administration of a FLAP inhibitor and a NO modulator to the mammal.

    摘要翻译： 本文公开了在哺乳动物中组合5-脂氧合酶活化蛋白（FLAP）抑制剂和NO水平调节剂的组合物和化合物。 NO调节剂可以是诱导哺乳动物产生NO的药剂，或者可以是本身在哺乳动物中产生NO的药剂。 本文进一步公开的是合成这些化合物的策略，以及用于测试组合化合物和组合物是否提供期望益处的方法。 本文还公开了组合FLAP抑制剂和NO调节剂的药物组合物和制剂。 本文进一步描述的是使用这些组合物和化合物治疗哺乳动物，包括人类的疾病，病症和障碍的方法。 这样的治疗方法包括向哺乳动物分开施用FLAP抑制剂和NO调节剂，以及向哺乳动物同时施用FLAP抑制剂和NO调节剂。

    CRF receptor antagonists and methods relating thereto
    29.
    发明授权
    CRF receptor antagonists and methods relating thereto 有权
    CRF受体拮抗剂及其相关方法

    公开(公告)号：US06531475B1

    公开(公告)日：2003-03-11

    申请号：US09574751

    申请日：2000-05-18

    申请人： Mustapha Haddach ,  Brian P. Dyck ,  Charles Q. Huang ,  Jodie Nelson ,  Zhiqiang Guo ,  James R. McCarthy

    发明人： Mustapha Haddach ,  Brian P. Dyck ,  Charles Q. Huang ,  Jodie Nelson ,  Zhiqiang Guo ,  James R. McCarthy

    IPC分类号： C07D47114

    CPC分类号： C07D471/16 ,  C07D487/16

    摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same

    摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：包括立体异构体及其药学上可接受的盐，其中n，m，A，B，C，R，R 1，R 2和Ar如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法

    CRF antagonistic quino- and quinazolines
    30.
    发明授权
    CRF antagonistic quino- and quinazolines 失效
    CRF拮抗喹诺酮和喹唑啉

    公开(公告)号：US06482836B1

    公开(公告)日：2002-11-19

    申请号：US09403393

    申请日：1999-10-19

    申请人： Charles Huang ,  Keith M. Wilcoxen ,  Chen Chen ,  Mustapha Haddach ,  James R. McCarthy

    发明人： Charles Huang ,  Keith M. Wilcoxen ,  Chen Chen ,  Mustapha Haddach ,  James R. McCarthy

    IPC分类号： A61K314706

    CPC分类号： C07D215/233 ,  C07D215/12 ,  C07D215/36 ,  C07D215/42 ,  C07D239/94 ,  C07D401/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中R 1是C 1-6烷基，NR 6 R 7，OR 6或SR 7; R2是氢，C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R 4和R 5各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，氰基，硝基，氨基和单或二（C 1-6烷基）氨基; R6是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R 7是氢，C 1-8烷基，一或二（C 3-6环烷基）甲基，C 3-6环烷基，C 3-6烯基，羟基C 1-6烷基，C 1-6烷基羰氧基-C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基，单或二（C 3-6环烷基） - 甲基，Ar 2 CH 2，C 1-6烷氧基C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，单或二 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基; 或R6和R7与它们所连接的氮原子一起可以形成任选被C 1-6烷基或C 1-6烷氧基C 1-6烷基取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar 1和Ar 2各自为任意取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效的治疗来治疗与CRF过度分泌有关的疾病的方法，例如抑郁，焦虑，药物滥用