DERIVATIVES OF 4,5-DIHYDRO-1H-PYRAZOLE ELICITING CB1-ANTAGONISTIC ACTIVITY Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a group of new derivatives of 4,5-dihydro-1H-pyrazole of the general formula (I):

wherein R means phenyl, thienyl or pyridyl and these indicated groups can be substituted with (C₁-C₃)-alkoxy-group or halogen atom; R₁ means phenyl that can be substituted with (C₁-C₃)-alkoxy-group or pyridyl group; R₂ means hydrogen atom or hydroxy-group; Aa means one group among the following groups: (i) , (ii) , (iii) , (iv) or (v) ; R₄ and R₅ mean independently from one another hydrogen atom or (C₁-C₈)-branched or unbranched alkyl; or R₄ means acetamido- or dimethylamino-group or 2,2,2-trifluoroethyl, or phenyl, or pyridyl under condition that R₅ means hydrogen atom; R₆ means hydrogen atom at (C₁-C₃)-unbranched alkyl; Bb means sulfonyl or carbonyl; R₃ means benzyl, phenyl or pyridyl that can be substituted with 1, 2 or 3 substitutes Y that can be similar or different and taken among the group including (C₁-C₃)-alkyl or (C₁-C₃)-alkoxy-group, halogen atom, trifluoromethyl; or R₃ means naphthyl, and its racemates, mixtures of diastereomers and individual stereoisomers and as well as E-isomers, Z-isomers and mixture of E/Z-compounds of the formula (I) wherein A has values (i) or (ii), and its salt. These compounds are power antagonists of Cannbis-1 (CB₁) receptor and can be used for treatment of psychiatric and neurological diseases. Except for, invention relates to a pharmaceutical composition used for treatment of some diseases mediated by CB₁-receptor, to a method for preparing this composition, a method for preparing representatives of compounds of the formula (I) wherein Aa means group of the formulae (i) or (ii), intermediate compounds used for preparing compounds of the formula (I) and to a method for treatment of some diseases mediated by CB₁-receptor.

EFFECT: valuable medicinal properties of compounds.

16 cl, 9 ex