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 R1 is C¿1-6?alkyl, NR?6R7, OR6 or SR7; R2¿ is hydrogen, C¿1-6?alkyl, C1-6alkyloxy or C1-6alkylthio; R?3 is Ar1 or Het1; R4 and R5¿ are each independently selected from hydrogen, halo, C¿1-6?alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R?6¿ is hydrogen, C¿1-6?alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R?7¿ is hydrogen, C¿1-8?alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R?6¿ is C¿1-8?alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar?2CH¿2, 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 R7¿ taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C¿1-6?alkyl or C1-6alkyloxyC1-6alkyl; and Ar?1 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).