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    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY
    13.
    发明专利
    QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING CORTICOTROPIN RELEASING FACTOR (CRF) ANTAGONIST ACTIVITY 未知

    公开(公告)号：CA2270777C

    公开(公告)日：2008-04-22

    申请号：CA2270777

    申请日：1998-09-07

    Applicant: DUPHAR INT RES

    Inventor： REINDERS JAN H ,  RONKEN ERIC ,  TULP MARTINUS T M ,  JANSEN JOHANNES W C M ,  VISSER GERBEN M ,  TOOROP GERRIT P ,  DEN HARTOG JACOBUS A J

    IPC: C07D239/94 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D215/42 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

    Abstract: The invention relates to novel quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity. It has been found that compounds having formula (I) wherein A is CH or N, ri ng Q is phenyl, pyridyl, pyrimidinyl or pyridazinyl, optionally substituted with one or two groups R4; ring Y is phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 and R2 are optionally branched C1-6-alkyl, C3-6-alkenyl, C3-46-alkynyl, C3-6-cycloalkyl - C1-4-alkyl, phenyl-C1-4-alkyl, 5- or 6-membered saturated or unsaturated heterocyclyl-C1-4-alkyl, which groups R1 and R2 can be substituted with OH, C1-3-alkoxy, C1-3-alkoxycarbonyl, optionally mono- or di-(C1-3-alkyl)substituted amino, halogen or cyano; R3 is H, C1-3- alkyl optionally substituted with one or more fluorine atoms, or R3 is halogen, methoxy or ethoxy; R4 is C1-3-alkyl optionally substituted with one or more fluorine atoms, or R4 is halogen, methoxy, ethoxy, amino, mono- or di-substituted amino, or cyano; R5 is halogen, optionally branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, C3-6-cycloalkyl-C1-4-alkyl, O-(C1-6-alkyl), S-(C1-6-alkyl), SO 2- (C1-6-alkyl), hydroxy, cyano, nitro, trifluoromethyl, SO2NH2, SO2N(mono- or di-C1-4-alkyl), formyl, CO-(C1-6-alkyl), COOH, COO-(C1 -6- alkyl), CONH2, CON(mono- or di-C1-4-alkyl),amino, N(mono or di-C1-4-alkyl), NHCO(C1-46-alkyl), NHSO2-(C1-6-alkyl), which groups R5 can be identical or different; and n has the value 0 to 4; with the proviso that the group NR1R2 is not diethylamino, ethyl,n-propylamino or ethyl,n-butylamino, if A is CH, Q is unsubstituted phenyl, R3 is methyl, and substituent Y with the group(s) R 5 is 2,4,6-trimethylphenyl, and salts thereof have good CRF antagonist activity.

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