CORTICOTROPIN-RELEASING FACTOR (CRF) RECEPTOR ANTAGONISTS BICYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

The present invention relates to compounds of formula (I) wherein R 1 is aryl or heteroaryl, each of which may be substituted with 1 to 4 substituents selected from the group consisting of halogen, alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, halogen, alkoxy, -C (O) R5, nitro, -NR6R7, cyano and / or R8; R1 is hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkoxy, halogen, -NR 6 R 7 or cyano; R 2 is hydrogen, cycloalkyl or -R 9; R3 is cycloalkyl or -R9; or R2 and R3 together with the nitrogen atom form a 5-14 membered heterocyclic group which may be optionally substituted with 1-3 -R10; R4 is hydrogen, halogen, alkyl or haloalkyl; R5 is alkyl, -OR6 or -NR6R7; R6 and R7 are hydrogen or alkyl; R8 is a 5-6 membered heterocyclic group containing a saturated or 1-3 double bond, optionally substituted with one or more groups -R11; R9alkyl which may optionally carry one or more substituents selected from the group consisting of cycloalkyl, alkoxy, haloalkoxy, hydroxy and / or haloalkyl; R10-R8, cycloalkyl, alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, haloalkoxy, hydroxy, halogen, nitro, cyano, -C (O) NR6R7, or optionally 1 Phenyl substituted with -4-R11; R11 is cycloalkyl, alkyl, alkoxy, haloalkyl, alkenyl, alkynyl, haloalkoxy, hydroxy, halogen, nitro, cyano or -C (O) NR6R7; X is carbon or nitrogen; and n is 1 or 2 and relates to their stereoisomers, their prodrugs, and their pharmaceutically acceptable salts and solvates, as well as processes for the preparation of the compounds, pharmaceutical compositions containing the compounds and treating the compounds mediated by corticotropin releasing factor (CRF). HE