Pyrazolopyrimidines as CRF receptor antagonists

    公开(公告)号:US07074797B2

    公开(公告)日:2006-07-11

    申请号:US10665740

    申请日:2003-09-19

    CPC classification number: C07D487/04

    Abstract: 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).

    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:US06352990B1

    公开(公告)日:2002-03-05

    申请号:US09415503

    申请日:1999-10-08

    CPC classification number: C07D471/04 C07D235/08 C07D473/00 C07D487/04

    Abstract: 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.

    Abstract translation: 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。

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