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    Pyrazolopyrimidines as CRF receptor antagonists
    1.
    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).

    Pyrazolopyrimidines as CRF receptor antagonists
    2.
    发明授权
    Pyrazolopyrimidines as CRF receptor antagonists 有权

    公开(公告)号：US07074797B2

    公开(公告)日：2006-07-11

    申请号：US10665740

    申请日：2003-09-19

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

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

    IPC分类号： A61K31/505 ,  C07D239/00 ,  C07D487/00

    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, A1CH2, 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).

    Pyrazolopyrimidines as CRF receptor antagonists
    3.
    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。

    CRF antagonistic quino-and quinazolines
    5.
    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

    Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
    8.
    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。

    CRF antagonistic quino- and quinazolines
    10.
    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