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    Pyrazolopyrimidines as CRF receptor antagonists
    10.
    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).