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    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
    1.
    发明申请
    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：US20060122204A1

    公开(公告)日：2006-06-08

    申请号：US11264702

    申请日：2005-11-01

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

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

    IPC分类号： 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以下结构：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。

    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
    6.
    发明申请
    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：US20050043338A1

    公开(公告)日：2005-02-24

    申请号：US10885511

    申请日：2004-07-06

    申请人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

    发明人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

    IPC分类号： A61P5/02 ,  C07D239/54 ,  C07D401/06 ,  A61K31/513 ,  C07D43/02

    CPC分类号： C07D239/54 ,  C07D401/06

    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 R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 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以下结构：其中R1a，R1b，R2a，R2b，R3，R4，R5，R6，R7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。

    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
    7.
    发明申请
    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：US20070015778A1

    公开(公告)日：2007-01-18

    申请号：US11446583

    申请日：2006-06-02

    申请人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

    发明人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

    IPC分类号： A61K31/513 ,  C07D239/52

    CPC分类号： C07D239/54 ,  C07D401/06

    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 R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 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以下结构：其中R 1a，R 1b，R 2a，R 2b， R 3，R 4，R 5，R 6，R 7和R 7， 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。

    CRF antagonistic quino-and quinazolines
    8.
    发明授权
    CRF antagonistic quino-and quinazolines 有权
    CRF对抗喹诺酮和喹唑啉

    公开(公告)号：US06610678B2

    公开(公告)日：2003-08-26

    申请号：US10266662

    申请日：2002-10-08

    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： A61K3133

    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(C3-6cyclo-alkyl)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 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; 通过施用有效的方法治疗与CRF分泌过高有关的疾病，如抑郁症，焦虑症，药物滥用

    Pyrazolopyrimidines as CRF receptor antagonists
    9.
    发明授权
    Pyrazolopyrimidines as CRF receptor antagonists 有权
    吡唑并嘧啶作为CRF受体拮抗剂

    公开(公告)号：US06664261B2

    公开(公告)日：2003-12-16

    申请号：US09117717

    申请日：1999-03-02

    申请人： Chen Chen ,  Thomas R. Webb ,  James R. McCarthy ,  Terence J. Moran ,  Keith M. Wilcoxen ,  Charles Huang

    发明人： Chen Chen ,  Thomas R. Webb ,  James R. McCarthy ,  Terence J. Moran ,  Keith M. Wilcoxen ,  Charles Huang

    IPC分类号： A61K31505

    CPC分类号： C07D487/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula —Alk—O—CO—Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; 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为NR 4 R 5或OR 5。 R 2是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基; R 3是氢，C 1-6烷基，C 1-6烷基磺酰基，C 1-6烷基磺酰基或C 1-6烷硫基; R 4是氢，C 1-6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 5为C 1-6烷基，单或二（C 3-6环烷基）甲基，Ar 1 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， 吗啉基，单或二（C 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，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar 1的基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; 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。

    Pyrazolopyrimidines as CRF receptor antagonists
    10.
    发明申请
    Pyrazolopyrimidines as CRF receptor antagonists 审中-公开

    公开(公告)号：US20060270659A1

    公开(公告)日：2006-11-30

    申请号：US11413610

    申请日：2006-04-28

    申请人： Chen Chen ,  Thomas Webb ,  James McCarthy ,  Terence Moran ,  Keith Wilcoxen ,  Charles Huang

    发明人： Chen Chen ,  Thomas Webb ,  James McCarthy ,  Terence Moran ,  Keith Wilcoxen ,  Charles Huang

    IPC分类号： A61K31/55 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -Alk-O—CO—Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; 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).