DERIVATIVES OF PYRIMIDINE SULFONAMIDE AS MODULATORS OF CHEMOKINE RECEPTORS Russian patent published in 2011 - IPC C07D239/56 C07D403/12 C07D405/14 C07D417/14 C07D413/14 C07D413/12 C07D401/14 A61K31/506 A61K31/513 A61K31/5377 A61P35/00 A61P11/06 A61P19/02 A61P17/06 A61P27/14 A61P1/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to new compounds of formula (1) or its pharmaceutically acceptable salts, with properties of antagonist CXCR2 of human neutrophils receptor. In formula (1) R¹ represents a group selected from C_1-8alkyl; where this group is possibly substituted with 1 substituent, independently selected from phenyl or 5-6-unit heteroaryl, containing 1-2 heteroatoms selected from N, S; where phenyl and heteroaryl are possibly substituted by 1, 2 or 3 substitutors, independently selected from halogeno, cyano, -OR⁴, -COOR⁷, -SO₂R¹⁰, C_1-6alkyl; X represents -CH₂-, oxygen, sulfur; R² represents C_3-7carbocyclil, possibly substituted with 1, 2 or 3 substituents, independently selected from -OR⁴; or R² represents 5-unit ring, containing 2 heteroatoms, selected from O, -NR⁸, and where this ring is possibly substituted with 1 substituent, independently selected from C_1-3alkyl; or R² represents group, selected from C_1-8alkyla, where this group is substituted with 1, 2 or 3 substituents, independently selected from hydroxy, amino, C_1-6alkoxy, C_1-6alkylamino, di(C_1-6alkyl)amino, N-C_1-6alkylcarbamoyl, N,N-di(C_1-6alkyl)carbamoyl, carboxy, -NR⁸COR⁹ and -CONR⁵R⁶; R³ represents group -NR⁵R⁶, or R³ represents phenyl, possibly condensed with 6-unit heterocyclil, containing nitrogen, naphthyl, 4-8-unit monocyclic heterocyclil, containing 1-3 heteroatoms, selected from N, O, S, possibly condensed with benzole ring or 3-unit nitrogen-containing ring, where heteroring may be non-saturated, partially or fully saturated, and one or more than one circular atom of carbon may form carbonyl group, and where each phenyl or heterocyclil group is possibly substituted with 1, 2 or 3 substituents, independently selected from halogeno, cyano, phenyl, 5-6-unit heteroaryl, containing 1-2 atoms of nitrogen, -OR⁴, -NR⁵R⁶, -CONR⁵R⁶, -COR⁷, -COR²⁰, -COOR⁷, -NR⁸COR⁹, -SO₂R¹⁰, -SO₂NR⁵R⁶ or C_1-6alkyl [possibly additionally substituted with 1, 2 or 3 substituents, independently selected from halogeno, cyano, -OR²⁰, -COOR²⁰, -NR¹⁸R¹⁹, -CONR¹⁸R¹⁹, phenyl or 5-6-unit of monocyclic heteroaryl, containing 1-2 heteroatoms O, N, S, or 10-unit bicyclic heteroaryl, containing 1 heteroatom O, where heteroring may be partially or fully saturated, and where each phenyl or heteroaryl is group possibly substituted with 1 or 2 substituents, independently selected from halogeno, cyano, nitro, -OR²⁰, -NR⁵R⁶, -COOR⁷, -NR⁸COR⁹, 6-unit heterocyclil, containing two heteroatoms, selected from O and N, 5-unit heteroaryl, containing 3 heteroatoms N, C_1-6alkyl (possibly additionally substituted with 1 substituent, independently selected from halogeno, cyano, nitro, -OR²⁰, -COOR²⁰; or R³ represents group, selected from C_3-7carbocyclil, C_1-8alkyl, where this group is possibly substituted with 1, 2 or 3 substituents, independently selected from halogeno, -OR⁴, -NR⁵R⁶; R⁴ represents hydrogen; R⁵ and R⁶ independently represent hydrogen or group, selected from C_1-6alkyl and monocyclic 6-unit saturated heterocyclil containing 1 heteroatom N; where C_1-6alkyl is possibly substituted with 1 substituent, independently selected from -NR¹⁵R¹⁶; or R⁵ and R⁶ together with atom of nitrogen, to which they are linked, form 4-7-unit saturated heterocyclic circukar system, possibly containing additional heteroatom, selected from oxygen, -SO(_n)- (where n equals 0, 1 or 2) and atoms of nitrogen; R¹⁰ represents hydrogen or group, selected from C_1-6alkyl; and each of R⁷, R⁸, R⁹, R¹⁵, R¹⁶, R¹⁷ independently represents hydrogen, C_1-6alkyl; R¹⁸, R¹⁹ and R²⁰ represent hydrogen or group, selected from C_1-6alkyl, where this group is possibly substituted with 1 substituent, independently selected from -NR⁸R⁹, -CONR⁸R^9.

EFFECT: production of new compounds, which may find application in production of medicinal agent for use in treatment of diseases and disorders mediated with chemokines, such as asthma, allergic rhinitis, chronic obstructive pulmonary disease, inflammatory intestine disease, irritable colon syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis or psoriasis, and also for treatment of cancer.

12 cl, 155 ex