DIPHENYLAZETIDINONE DERIVATIVES HAVING INHIBITORY ACTIVITY TOWARDS CHOLESTEROL ABSORPTION Russian patent published in 2010 - IPC C07D205/08 A61K31/397 A61P3/06 

FIELD: chemistry.

SUBSTANCE: compounds of formula (I): , where: R¹ is H, C_1-6alkyl, C_3-6cycloalkyl, phenyl, naphthyl; where the said C_1-6alkyl can possibly be substituted with one or two substitutes selected from OH, NH₂, guanidine, carbamoyl, COOH, C_1-6alkoxy, N-(C_1-6alkyl)amino, N,N-(C_1-6alkyl)₂amino, C₁-C₆alkylcarbonylamino, C_1-6alkylS(O)_a, where a equals 0-2, C_3-6cycloalkyl, phenyl or indolyl; and where any of the said phenyl, indolyl can possibly be substituted with one or two substitutes selected from halogen, OH, C_1-6alkyl, C_1-6alkoxy; R², R⁵ independently represents H, branched or straight C_1-6alkyl, C_3-6cycloalkyl, phenyl or naphthyl; where the said C_1-6alkyl can possibly be substituted with one or more OH, NH₂, guanidine, CN, carbamoyl, COOH, C_1-6alkoxy, phenylC_1-6alkoxy, naphthylC_1-6alkoxy, indolyl, imidazolyl, naphthyl, (C₁-C₄)₃Si, N-(C_1-6alkyl)amino, N,N-(C_1-6alkyl)₂amino, C_1-6alkylS(O)_a, C_3-6cycloalkyl, phenyl, phenyl-C_1-6alkylS(O)_a, naphthyl-C_1-6alkylS(O)_a, where a equals 0-2; where any of phenyl, naphthyl, indolyl, imidazolyl can possibly be substituted with one or two substitutes selected from halogen, OH, C_1-6alkyl, C_1-6alkoxy; R³ is H, C_1-6alkyl, halogen, C_1-6alkoxy or C_1-6alkylS-; R⁴ is H, C_1-6alkyl, halogen, C_1-6alkoxy; R⁶ is H, C_1-6alkyl, phenylC_1-6alkyl, naphthylC_1-6alkyl; where R⁵, R² can form a cyclopropane, cyclopentane ring, where R⁶, R² can form a pyrrole ring; or its pharmaceutically acceptable salt; given the condition that the said compound is not 3-(R)-4-(R)-1-(phenyl)-3-[2-(4-fluorophenyl)-2-hydroxyethylsulphanyl]-4-[4-(N-{N-[(R)-1-(carboxy)-2-hydroxy)ethyl]carbamoylmethyl}carbamoylmethoxy)phenyl]-azetidin -2-one or 3-(R)-4-(R)-1-(phenyl)-3-[2-(4-flurophenyl)-2-hydroxyethylsulphanyl]-4-{4-N-((R)-α-{N-[(S)-1-(carboxy)-2-(hydroxy)ethyl]-carbamoyl}benzyl)carbamoylmethoxy]phenyl}azetidin-2-one.

EFFECT: obtaining compounds which are useful as cholesterol absorption inhibitors, enabling their use in pharmaceutical compositions.

18 cl, 136 ex