DERIVATIVES OF PYRIMIDINE AND PHARMACEUTICAL COMPOSITION Russian patent published in 2006 - IPC C07D239/56 C07D239/46 C07D239/52 C07D403/04 C07D403/12 A61K31/505 A61K31/506 A61P25/00 A61P19/02 A61P25/06 A61P25/28 

FIELD: organic chemistry of heterocyclic compounds, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of pyrimidine of the general formula (I) and their pharmaceutically acceptable acid-additive salts possessing properties of neurokinin-1 (NK) receptors antagonists. In the general formula (I): R¹ means lower alkyl, lower alkoxyl, pyridinyl, pyrimidinyl, phenyl, -S-lower alkyl, -S(O₂)-lower alkyl, -N(R)-(CH₂)_n-N(R)₂, -O-(CH)_n-N(R)₂, -N(R)₂ or cyclic tertiary amine as a group of the formula: R¹ means lower alkyl, lower alkoxyl, pyridinyl, pyrimidinyl, phenyl, -S-lower alkyl, -S(O₂)-lower alkyl, -N(R)-(CH₂)_n-N(R)₂, -O-(CH)-N(R)₂, -N(R)₂ or cyclic tertiary amine of the formula: that can comprise additional heteroatom chosen from atoms N, O or S, and wherein this group can be bound with pyrimidine ring by bridge -O-(CH₂)_n-; R² means hydrogen atom, lower alkyl, lower alkoxyl, halogen atom or trifluoromethyl group; R³/R^3' mean independently of one another hydrogen atom or lower alkyl; R⁴ means independently of one another halogen atom, trifluoromethyl group or lower alkoxyl; R means hydrogen atom or lower alkyl; R means independently of one another hydrogen atom or lower alkyl; X means -C(OH)N(R)- or -N(R)C(O)-; Y means -O-; n = 1, 2, 3 or 4; m means 0, 1 or 2. Also, invention relates to a pharmaceutical composition comprising one or some compounds by any claim among claims 1-19 and pharmaceutically acceptable excipients. Proposed compounds can be used in treatment, for example, inflammatory diseases, rheumatic arthritis, asthma, benign prostate hyperplasia, Alzheimer's diseases and others.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

21 cl, 1 tbl, 76 ex