NOVEL TETRAHYDROISOQUINOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION BASED THEREON, USE THEREOF AND METHOD OF TREATING AND/OR PREVENTING DISEASE Russian patent published in 2013 - IPC C07D217/06 C07D401/12 C07D413/12 C07D417/12 C07D403/12 A61K31/472 A61K31/4725 A61P1/16 A61P3/04 A61P3/06 A61P3/10 A61P9/10 A61P15/08 A61P27/12 A61P29/00 A61P43/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel tetrahydroisoquinoline derivatives of general formula (I) or pharmacologically acceptable salts thereof, where R¹ is a phenyl aminocarbonyl group which can be substituted with 1-3 groups independently selected from a substituting group A, a heteroaryl aminocarbonyl group, where the heteroaryl is pyridine, pyrazine, thiazole, pyrazole or isoxazole, which can be substituted with 1 group selected from a substituting group A, benzoxazol-2-yl group, which can be substituted with 1 group selected from a substituting group A, benzothiazol-2-yl group, (C₁-C₆ alkyl which can be monosubstituted with a C₃-C₆ cycloalkyl group), aminocarbonyl group, (C₃-C₆ cycloalkyl)aminocarbonyl group or adamantyl aminocarbonyl group; R² independently represents a C₁-C₆ alkyl group; R³ is a heterocyclic group, where the heterocycle is oxazole, oxadiazole, pyrazole, isoxazole or tetrazole, which can be substituted with 1 group selected from a substituting group A, a group of formula -C(=O)-O-R⁴, or a group of formula -C(=O)-N(R⁵)R⁶; R⁴ is a hydrogen atom, a C₁-C₆ alkyl group which can be substituted with 1-2 groups independently selected from a substituting group B; R⁵ is a hydrogen atom, a C₁-C₆ alkyl group which can be substituted with 1 group selected from a substituting group B, a C₃-C₆ cycloalkyl group which is monosubstituted with a carboxyl group, or a heterocyclic group, where the heterocycle is tetrazole, which can be substituted with 1 group selected from a substituting group A; R⁶ is a hydrogen atom or a C₁-C₆ alkyl group; in those cases when both R⁵ and R⁶ represent a C₁-C₆ alkyl group, which can be substituted with 1 group selected from a substituting group B, their carbon atoms can be bonded to each other to form a 5-member saturated ring; X is an oxygen atom, a methylene group, a group of formula -NH-, a methylene group which is monosubstituted with a C₁-C₆ alkyl group, or a group of formula -N(R⁷)-; R⁷ is a C₁-C₆ alkyl group; L is a single bond, a methylene group, a 1,1-dimethylmethylene group, an ethylene group, a group of formula - CH=, or a methylene group which is monosubstituted with a C₁-C₆ alkyl group; … denotes a single bond or a double bond (however, … denotes a single bond when L is a group of formula -CH=); m equals 1 or 2; n equals 0 or 1; substituting group A is a group of substitutes selected from a halogen atom, a C₁-C₆ alkyl group, a C₁-C₆ halogenated alkyl group, a C₁-C₆ alkoxy group, a C₁-C₆ halogenated alkoxy group, a C₁-C₆ alkylthio group, a carboxyl group, a di-(C₁-C₆ alkyl)amino group, a cyano group, a hydroxy group, a C₁-C₆ alkylthionyl group and an oxo group; and substituting group B is a group of substitutes selected from a carboxyl group and a hydroxy group. The invention also relates to a pharmaceutical composition based on the compound of formula (I), use of the compound of formula (I) and a method of treating and/or preventing a disease.

EFFECT: obtaining novel tetrahydroisoquinoline derivatives, having excellent inhibiting action on acyl-coenzyme A: diacylglycerol-acyltransferase and excellent food intake suppression.

31 cl, 113 ex