DERIVATIVES OF 4-PHENYLPYRIMIDINE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2004 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of 4-phenylpyrimidine and their pharmaceutically acceptable acid-additive salts that elicit properties of antagonist of neurokinin (NK-1) receptors. These compounds can be used in treatment of diseases mediated by NK-1 receptors, for example, headache, Alzheimer's diseases, cerebrospinal sclerosis, cardiovascular disorders, edema, chronic inflammatory diseases and so on. Proposed compounds correspond to the general formula (I):

wherein R¹ means hydrogen or halogen atom; R² means hydrogen, halogen atom, lower alkyl or lower alkoxy-group; R¹ and R² in common with two atoms of carbon cycle can mean the group -CH=CH-CH=CH-; R³ means halogen atom, trifluoromethyl, lower alkyl or lower alkoxy-group; R⁴/R^4' each means independently of one another hydrogen atom or lower alkyl; R⁵ means lower alkyl, lower alkoxy-group, amino-group, phenyl, hydroxy-(lower)-alkyl, cyano-(lower)-alkyl, carbamoyl-(lower)-alkyl, pyridyl, pyrimidyl, -(CH₂)_n-piperazinyl substituted optionally with one or two lower alkyl groups or hydroxy-(lower)-alkyl, -(CH₂)_n-morpholinyl, -(CH₂)_n-piperidinyl, -(CH₂)_n+1-imidazolyl, lower alkylsulfanyl, lower alkylsulfonyl, benzylamino-group, -NH-(CH₂)_n+1-N(R^4'')₂, -(CH₂)_n+1-N(R^4'')₂, -O-(CH₂)_n+1-morpholinyl, -O-(CH₂)_n+1-piperidinyl or -O-(CH₂)_n+1-N(R^4'')₂ wherein 4'' means hydrogen atom or lower alkyl; n = 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.

11 cl, 6 sch, 121 ex