DERIVATIVES OF 5-PHENYLPYRIMIDINE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of 5-phenylpyrimidine or their pharmaceutically acceptable acid-additive salts that elicit properties of antagonists of neuropeptide receptor neurokinin-1 (NK-1). This allows their applying for treatment of such diseases as Alzheimer's disease, cerebrospinal sclerosis, attenuating syndrome in morphine withdrawal, cardiovascular alterations and so on. Compounds of invention correspond to the general formula (I):

wherein R¹ means hydrogen or halogen; R² means hydrogen, halogen atom, (lower)-alkyl or (lower)-alkoxy-group; R³ means halogen atom, trifluoromethyl group, (lower)-alkoxy-group or (lower)-alkyl; R⁴/R^4' mean independently hydrogen atom or (lower)-alkyl; R⁵ means (lower)-alkyl, (lower)-alkoxy-group, amino-group, hydroxyl group, hydroxy-(lower)-alkyl, -(CH₂)_n-piperazinyl substituted optionally with lower alkyl, -(CH)_n-morpholinyl, -(CH₂)_n+1-imidazolyl, -O-(CH₂)_n+1-morpholinyl, -O-(CH₂)_n+1-piperidinyl, (lower)-alkylsulfanyl, (lower)-alkylsulfonyl, benzylamino-group, -NH-(CH₂)_n+1N(R^4'')₂, -(CH₂)_n-NH-(CH₂)_n+1N(R^4'')₂, -(CH₂)_n+1N(R^4'')₂ or -O-(CH₂)_n+1N(R^4'')₂ wherein R^4'' means hydrogen atom or (lower)-alkyl; R⁶ means hydrogen atom; R² and R⁶ or R¹ and R⁶ in common with two ring carbon atoms can represent -CH=CH-CH=CH- under condition that n for R¹ is 1; n means independently 0-2; X means -C(O)N(R^4'')- or -N(R^4'')C(O)-. Also, invention relates to a pharmaceutical composition.

EFFECT: valuable medicinal properties of compounds.

15 cl, 4 sch, 86 ex