Patent ID: 6441018
Filing Date: 2002-08-27
Classification: C07D

Abstract:
A composition for the treatment of (a) illnesses induced or facilitated by corticotropin releasing factor or (b) stress-induced illnesses, which comprises a compound of the formula whereinA and R1 together with the carbons to which they are attached form 5-pyridyl which is optionally substituted by R5 which is hydrogen, C1-C6 alkyl, fluoro, chloro, bromo, hydroxy, amino, O(C1-C6 alkyl), NH(C1-C6 alkyl), N(C1-C6 alkyl)(C1-C6 alkyl), SH, S(O)n(C1-C6 alkyl) wherein n=0, 1 or 2, WHEREIN said C1-C6 alkyl optionally contains from one to two double or triple bonds and is optionally substituted by from 1 to 3 substituents R6 which is hydroxy, amino, C1-C3 alkoxy, dimethylamino, diethylamino, methylamino, ethylamino, NH(C&boxH;O)CH3, fluoro, chloro, bromo or C1-C3 thioalkyl; R2 is hydrogen, C1-C6 alkyl, hydroxy, amino, O(C1-C6 alkyl), NH(C1-C6 alkyl), N(C1-C6 alkyl)(C1-C6 alkyl), SH, S(O)n(C1-C6 alkyl) wherein n=0, 1, or 2, cyano, hydroxy, carboxy, or amido, wherein said alkyls are optionally substituted by one to three of hydroxy, amino, carboxy, amido, NH(C&boxH;O)(C1-C6 alkyl), N(C1-C6 alkyl)C1-C6 alkyl), (C&boxH;O)O(C1-C6 alkyl), C1-C3 alkoxy, C1-C3 thioalkyl, fluoro, bromo, chloro, iodo, cyano or nitro; R3 is phenyl, naphthyl, 3 to 8-membered cycloalkyl or 9 to 12 membered bicycloalkyl, wherein each one of the above groups is optionally substituted independently by from one to three of fluoro, chloro, bromo, trifluoromethyl, C1-C6 alkyl or C1-C6 alkoxy, or one of cyano, nitro, amino, NH(C1-C6 alkyl) N(C1-C4 alkyl)(C1-C2 alkyl), COO(C1-C4 alkyl), CO(C1-C4 alkyl), SO2NH(C1-C4 alkyl), SO2N(C1-C4 alkyl)(C1-C2 alkyl), SO2NH2, NHSO2(C1-C4 alkyl), S(C1-C6 alkyl), SO2(C1-C6 alkyl), wherein said C1-C4 alkyl and C1-C6 alkyl are optionally substituted by one or two of fluoro, chloro, hydroxy, amino, methylamino, dimethylamino or acetyl; and R4 is phenyl, naphthyl, 3 to 8-membered cycloalkyl or 9 to 12-membered bicycloalkyl, wherein each of the above groups is optionally substituted independently by from one to three of fluoro, chloro, bromo, trifluoromethyl, C1-C6 alkyl or C1-C6 alkoxy, or one of cyano, nitro, amino NH(C1-C6 alkyl), NC1-C4 alkyl)(C1-C2 alkyl), COO(C1-C4 alkyl), CO(C1-C4 alkyl), SO2NH(C1-C4 alkyl), SO2N(C1-C4 alkyl)(C1-C2 alkyl), SO2NH2, NH2SO2(C1-C4 alkyl), S(C1-C6 alkyl) or SO2(C1-C6 alkyl), wherein said C1-C4 alkyl and C1-C6 alkyl are optionally substituted by one or two of fluoro, chloro, hydroxy, amino, methylamino, dimethylamino or acetyl; provided that R4 is not unsubstituted phenyl.