CRF ANTAGONISTIC QUINO- AND QUINAZOLINES

摘要

This invention concerns compounds of formula (I), including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R<1> is C1-6alkyl, NR<6>R<7>, OR<6> or SR<7>; R<2> is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R<3> is Ar<1> or Het<1>; R<4> and R<5> are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R<6> is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R<7> is hydrogen, C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R<6> is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar<2>CH2, 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 R<6> and R<7> 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 Ar<1> and Ar<2> are each optionally substituted phenyl; and Het<1> 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).