| abstract |
The present invention relates to compounds of the general formula: (CF DRAWING IN BOPI) in which R is a hydrogen atom, a lower alkyl group, lower alkoxy, a halogen atom or a trifluoromethyl group; R1 is an atom. hydrogen or halogen; or R and R1 may together be -CH = CH-CH = CH; R2 and R2 are independently of each other a hydrogen atom, a halogen atom, a trifluoromethyl group, a lower alkoxy or cyano group; orR2 and R2 'can be, taken together, -CH = CH-CH = CH-, optionally substituted by one or more substituents selected from lower alkyl or lower alkoxy groups; R3 is a hydrogen atom, a lower alkyl group or forms a cycloalkyl group; R4 is a hydrogen atom, -N (R5) 2, -N (R5) (CH2) - N (R5) S (O) 2 - (lower alkyl), -N (R5) S (O) 2 -phenyl, -N = CHN (R5) 2, -N (R5) C (O) R5 or a cyclic tertiary amine from the group. (CF DRAWING IN BOPI) or of the group (CF DRAWING IN BOPI) R5 are, independently of each other, a hydrogen atom, a C3 to C6 cycloalkyl, benzyl or lower alkyl group; R6 is a hydrogen atom, a hydroxy group, lower alkyl, (CH2) n COO- (lower alkyl), -N (R5) CO- (lower alkyl), hydroxy- (lower alkyl), cyano, - (CH2) n O (CH2) n OH , -CHO or a 5 or 6 membered heterocyclic group, optionally linked through an alkylene group, X is -C (O) N (R5) -, - (CH2) m O-, - (CH2) m N (R5) -, -N (R5) C (O) -, or -N (R5) (CH2) m; n is 0 to 4; andm is 1 or 2; and their pharmaceutically acceptable addition salts. The compounds of formula I show a high affinity towards the NK-1 receptor. They can be used for the treatment of diseases which are related to NK-1 receptor antagonists. |