DERIVATIVES OF 3-OXO-1-CYCLOBUTENE AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2007 - IPC C07D213/81 C07D417/04 C07D213/89 C07D401/12 C07C229/36 A61K31/4375 A61K31/4412 A61P7/00 A61P9/00 

FIELD: organic chemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of 3-oxo-1-cyclobutene of the general formula (I): and their salts, solvates, hydrates and N-oxides wherein R¹ represents group of the formula: Ar¹L²Ar²Alk wherein Ar¹ represents aromatic or heteroaromatic group; L² represents a covalent bond or -O-, -NH- or -CONH-; Ar² represents arylene or heteroarylene group; Alk represents chain -CH₂CH(R) or -CH(CH₂R)- wherein R represents -CO₂H or -COOAlk⁷ wherein Alk⁷ represents (C₁-C₈)-alkyl, (C₃-C₈)-cycloalkyl, (C₃-C₈)-heterocycloalkyl group and others; X represents group -N(R²)- wherein R² represents hydrogen atom or (C₁-C₆)-alkyl group; V represents oxygen atom; R^x, R^y and R^z represent atom or group -L¹(Alk¹)_n(R³)_v wherein L¹ represents covalent bond or -O-, -S-, -Se-, -S(O)-, -NH- or -N(CH₃)-; Alk¹ represents aliphatic group; R³ represents hydrogen, halogen atom, group -OR^3a, -SR^3a and others wherein R^3a represents hydrogen atom, (C₁-C₆)-alkyl and others; n = 0 or 1; v = 1, 2 or 3 under condition that if n = 0 and L¹ represents covalent bond then v = 1; or R^z represents atom or group given above, and R^x and R^y taken together form spiro-bound cycloaliphatic or heterocycloaliphatic group. Compounds of the formula (I) possess inhibitory activity with respect to α₄-integrin and can be used in medicine.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

26 cl, 216 ex