DIPHENYLAZETIDINONE DERIVATIVES, METHODS FOR OBTAINING SAME, PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS OF SAID DERIVATIVES AND APPLICATION THEREOF IN CHOLESTEROL ABSORPTION INHIBITION Russian patent published in 2008 - IPC C07D205/08 C07D409/12 A61K31/397 A61P3/06 A61P9/10 

FIELD: chemistry.

SUBSTANCE: invention concerns a compound of the formula (I) , where A ring is selected out of phenyl or thienyl; X is selected out of -CR²R³-, -O- and -S(O)_a-; where a is 0-2; Y is selected out of -CR⁴R⁵-, -O- and -S(O)_a-; where a is 0-2; at least one -CR²R³- or -CR⁴R⁵- group is present; R¹ is independently selected out of halogeno, C_1-6alkyl and C_1-6ealkoxy; b is equal to 0-3; R² and R³, R⁴ and R⁵ are independently selected out of hydrogen, hydroxy, C_1-6alkyl and C_1-6alkoxy; or R² and R³, R⁴ and R⁵ together form oxogroup; R⁶ is independently selected out of halogeno, C_1-6alkyl and C_1-6alkoxy; c is 0-5; R⁷ is independently selected out of halogeno, trifluoromethyl, trifluoromethoxy, methyl, ethyl, methoxy and ethoxy; d is 0-4; R⁹ is hydrogen or C_1-4alkyl; R¹⁰ is hydrogen or C_1-4alkyl; R¹¹ and R¹² are independently selected out of hydrogen, C_1-4alkyl or carbocyclyl; where R¹¹ and R¹² can possibly be independently substituted for carbon atom with one or more substitute selected out of R²⁵; R¹³ is hydrogen, C_1-4alkyl or carbocyclyl; where R¹³ can possibly be substituted for carbon atom with one or more substitute selected out of R²⁷; R¹⁴ is hydrogen, hydroxy, amino, carbamoyl, mercapto, sulfamoyl, etc; or R¹⁴ is a group of the formula (IA) , where Z is -N(R³⁵)-; where R³⁵ is hydrogen or C_1-4alkyl; R¹⁵ is hydrogen or C_1-4alkyl; R¹⁶ and R¹⁷ are independently selected out of hydrogen, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C_1-6alkyl, C_1-6alkoxy, N-(C_1-6alkyl)-amino etc; R¹⁸ is selected out of hydroxy, amino, carbamoyl, mercapto, sulfamoyl, C_1-10alkyl, C_1-10alkoxy, N-(C_1-10alkyl)amino, N,N-(C_1-10alkyl)₂amino, etc; p is 1-3; q is 0-1; r is 0-3; m is 0-2; n is 1-2; where R¹, R⁶, R⁷, R¹⁶, R¹⁷, R¹³, R⁹ can be equal or different; R²⁵, R²⁷ and R³³ are independently selected out of hydroxy, amino, carbamoyl, mercapto, sulfamoyl, C_1-10alkyl, C_1-10alkoxy, C_1-10alkoxycarbonyl, N-(C_1-10alkyl)amino, etc; where carbocyclyl is a saturated, partially saturated or non-saturated monocyclic carbon ring including 3-6 atoms; or its pharmaceutically acceptable salt, solvate, or salt solvate. Compounds of the formula (I) or its pharmaceutically acceptable salts, solvates, or salt solvates are obtained by interaction of acid of the formula (IV) or its activated derivative with amine of the formula (V) . Compounds of the formula (I), where R¹⁴ is a group of the formula (IA), are obtained by interaction of compound of the formula (VI) , where R¹⁴ is carboxy, or its activated derivative, with amine of the formula (VI). Compounds of the formula (I), where X or Y is -S(O)_a-, and a is 1 or 2, is obtained by oxidation of compound of the formula (I), where X or Y is -S(O)_a-, and a is 0 (for compounds of the formula (I), where a is 1 or 2), or a is 1 (for compounds of the formula (I), where a is 2). The invention concerns pharmaceutical composition with inhibition effect on cholesterol absorption containing effective quantity of compound of the formula (I) combined with pharmaceutically acceptable dilutant or carrier, and combination of compound of the formula (I) and hydroxymethylglutaryl-coenzyme A (HMG Co-A) reductase inhibitor. Compounds of the formula (I) are applied to produce inhibition effect on cholesterol absorption or in hyperlipidemic state treatment of haematothermal animals.

EFFECT: obtaining diphenylazetidinone derivatives with inhibition effect on cholesterol absorption.

38 cl, 54 ex