DERIVATIVES OF DIPHENYL AND MEDICINAL AGENT Russian patent published in 2004 - IPC

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to new compounds of the general formula (I):

that elicit properties of antagonists of neurokinin-1 (NK-1) receptor. In the general formula (I) R means hydrogen atom, (C₁-C₇)-alkyl, (C₁-C₇)-alkoxy-group, halogen atom, amino-group, -N(R⁶)₂ or trifluoromethyl; R¹ means hydrogen atom, (C₁-C)-alkoxy-group or halogen atom; or R and R¹ can form in common -CH=CH-CH=CH-; R² means halogen atom, (C₁-C₇)-alkyl or trifluoromethyl; R³ means hydrogen atom or (C₁-C₇)-alkyl; R⁴ means hydrogen atom or saturated cyclic tertiary amine comprising 5-6 atoms in cycle possibly substituted with (C₁-C₇)-alkyl; R⁵ means hydrogen atom, nitro-group, amino-group or -N(R⁶)₂; R⁶ means hydrogen atom or (C₁-C₇)-alkyl; X means -C(O)N(R⁶)-, -(CH₂)_nO-, -(CH₂)_nN(R⁶)-, -N(R⁶)C(O)- or -N(R⁶)(CH₂)_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.

EFFECT: valuable medicinal properties of compounds.

9 cl, 7 sch, 32 ex