DERIVATIVES OF 4,5-DIHYDRO-1H-PYRAZOLE POSSESSING CB-ANTAGONISTIC ACTIVITY Russian patent published in 2006 - IPC C07D231/06 A61K31/415 A61K31/4439 A61P25/00 A61P1/00 A61P9/00

Abstract RU 2281941 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to an enantiomer in S-configuration at position 4 of its 4,5-dihydropyrazole ring, compound of the formula (I): wherein R and R₁ are similar or different and represent 3-pyridyl or 4-pyridyl, or phenyl that can be substituted with halogen atom or methoxy-group; R₂ and R₃ are similar or different and represent hydrogen atom, (C₁-C₃)-alkyl or dimethylamino-group; R₄ represents phenyl that can be substituted with 1, 2 or 3 substitutes chosen among group comprising halogen atoms, trifluoromethyl, methoxy-group and (C₁-C₃)-alkyl, and to its tautomers and salts also. Compounds possess antagonistic activity with respect to CB₁-cannabis. Also, invention relates to a pharmaceutical composition possessing the abovementioned activity, method for preparing the pharmaceutical composition, method for synthesis of compounds of the formula (I), method for antagonistic effect on CB₁-receptors and method for treatment of cardiovascular diseases.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

7 cl, 4 ex

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RU 2 281 941 C2

Authors

Lange Jozefus Kh. M.

Krjuse Kornelis G.

Tipker Jakobus

Khogendorn Jan

Dates

2006-08-20—Published

2002-03-18—Filed