利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

16 条记录 (耗时 0.036 秒)

    CRF receptor antagonists and methods relating thereto
    3.
    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 pyrazolo[4,3-b]pyridines
    4.
    发明授权
    CRF antagonistic pyrazolo[4,3-b]pyridines 有权
    CRF拮抗性吡唑并[4,3-b]吡啶

    公开(公告)号：US06613777B1

    公开(公告)日：2003-09-02

    申请号：US09623634

    申请日：2001-02-20

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

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

    IPC分类号： A61K3144

    CPC分类号： C07D471/04

    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, NR5R6, OR6 or SR6; R2 is C1-6alkyl, C1-6alkyloxy, or C1-6alkylthio; R3 is Ar1 or Het1; R4 is hydrogen or C1-6alkyl; R5 is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, mono- or di(C1-6alkyl)amino-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar2C1-6alkyl, Ar2oxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, tetrahydrofuranylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, or C1-6alkylcarbonylC1-6alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl, morpholinyl, or thiomorpholinyl group, optionally substituted with 1 or 2 substituents each independently selected from C1-6alkyl or C1-6alkyloxyC1-6alkyl; and 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： 本发明涉及包括其立​​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 5 R 6，OR 6或SR 6; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R4是氢或C1-6烷基; R5是氢，C1-8烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基，单或二（C1-6烷基）氨基C1- 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 C 1-6烷基，Ar 2氧基C 1-6烷基，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，四氢呋喃基甲基，C 1-6烷硫基C 1-6烷基 ，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基或C 1-6烷基羰基C 1-6烷基; 或者R 5和R 6与它们所连接的氮原子一起形成吡咯烷基，哌啶基，高哌啶基，吗啉基或硫代吗啉基，任选地被1或2个独立地选自C 1-6烷基或C 1-6烷氧基C 1-6烷基的取代基取代 ; 并且Ar 1和Ar 2各自为任选取代的苯基; 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; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
    9.
    发明授权
    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 有权
    促性腺激素释放激素受体拮抗剂及其相关方法

    公开(公告)号：US07229995B2

    公开(公告)日：2007-06-12

    申请号：US11264702

    申请日：2005-11-01

    申请人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

    发明人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

    IPC分类号： C07D239/54 ,  A61K31/513

    CPC分类号： C07D239/54 ,  C07D403/12

    摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

    摘要翻译： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有如下结构：其中n，R 1a，R 1b，R 1c，R 2a， R 2，R 3，R 3，R 4，R 5，R 6， >和X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。