| abstract |
Described are compounds of General formula, wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen, or R and R1 together may mean the group -CH = CH-CH = CH-; R2 and R2 'independently of one another denote hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R2 and R2 'together may mean a group -CH = CH-CH = CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; each R3 is hydrogen, lower alkyl or together form a cycloalkyl group; R4 is hydrogen, -N (R5) 2, -N (R5) (CH2) nOH, -N (R5) S (O) 2-lower alkyl, -N (R5) S (O) 2-phenyl, -N = CH-N (R5) 2, -N (R5) C (O) R5 or a cyclic tertiary amine - or, R5 independently of one another means hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, - (CH2) nCOO-lower alkyl, -N (R5) CO-lower alkyl, hydroxy-lower alkyl, cyano, - (CH2) nO (CH2) nOH, -CHO or 5- or a 6-membered heterocyclic group possibly linked through an alkylene group, X is -C (O) N (R5) -, - (CH2) mO-, - (CH2) mN (R5) -, -N (R5 ) C (O) - or -N (R5) (CH2) m-; n = 0-4; and m = 1 or 2, as well as their pharmaceutically acceptable salts with acids. The compounds of formula I show a high affinity for the NK-1 receptor. They can be used to treat diseases involving NK-1 receptor antagonists. |