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    CRF antagonistic quino-and quinazolines
    1.
    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

    CRF antagonistic quino- and quinazolines
    2.
    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

    CRF receptor antagonists and methods relating thereto
    5.
    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 receptor antagonists and methods relating thereto
    6.
    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：US06723721B2

    公开(公告)日：2004-04-20

    申请号：US10027789

    申请日：2001-12-20

    申请人： Mustapha Haddach ,  Zhiqiang Guo ,  James R. McCarthy

    发明人： Mustapha Haddach ,  Zhiqiang Guo ,  James R. McCarthy

    IPC分类号： A61K31495

    CPC分类号： C07D471/16 ,  C07D487/16

    摘要： Compounds 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, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了可用于治疗多种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。 本发明的化合物具有以下结构：其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。

    CRF receptor antagonists and methods relating thereto
    7.
    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：US06348466B1

    公开(公告)日：2002-02-19

    申请号：US09439841

    申请日：1999-11-12

    申请人： Mustapha Haddach ,  Zhiqiang Guo ,  James R. McCarthy

    发明人： Mustapha Haddach ,  Zhiqiang Guo ,  James R. McCarthy

    IPC分类号： A61K31495

    CPC分类号： C07D471/16 ,  C07D487/16

    摘要： Compounds 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, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.

    摘要翻译： 公开了可用于治疗多种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。 本发明的化合物具有以下结构：其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。