| abstract |
FIELD: organic chemistry, pharmacy. n SUBSTANCE: invention relates to new compounds of the general formula (I): n n n n that elicit properties of antagonists of neurokinin-1 (NK-1) receptor. In the general formula (I) R means hydrogen atom, (C 1 -C 7 )-alkyl, (C 1 -C 7 )-alkoxy-group, halogen atom, amino-group, -N(R 6 ) 2 or trifluoromethyl; R 1 means hydrogen atom, (C 1 -C)-alkoxy-group or halogen atom; or R and R 1 can form in common -CH=CH-CH=CH-; R 2 means halogen atom, (C 1 -C 7 )-alkyl or trifluoromethyl; R 3 means hydrogen atom or (C 1 -C 7 )-alkyl; R 4 means hydrogen atom or saturated cyclic tertiary amine comprising 5-6 atoms in cycle possibly substituted with (C 1 -C 7 )-alkyl; R 5 means hydrogen atom, nitro-group, amino-group or -N(R 6 ) 2 ; R 6 means hydrogen atom or (C 1 -C 7 )-alkyl; X means -C(O)N(R 6 )-, -(CH 2 ) n O-, -(CH 2 ) n N(R 6 )-, -N(R 6 )C(O)- or -N(R 6 )(CH 2 ) n -; n means 1 or 2; and their pharmaceutically acceptable acid-additive salts with exception for (1,1'-diphenyl)-2-methaneamine N-[(4-methylphenyl)methyl]hydrochloride and (1,1'-diphenyl)-2-methaneamine N-{[4-(1,1-dimethylethyl)phenyl}-N-methylhydrochloride. Invention relates also to a medicinal agent based on claimed compounds. n EFFECT: valuable medicinal properties of compounds. n 9 cl, 7 sch, 32 ex |