SUBSTITUTED DERIVATIVES OF 4-AMINOCYCLOHEXANOL, METHOD FOR THEIR PREPARING AND THEIR USING, MEDICINAL AGENT POSSESSING BINDING PROPERTY WITH ORL1-RECEPTOR Russian patent published in 2008 - IPC C07C215/44 C07D295/96 C07D209/14 C07D333/58 C07D307/81 A61K31/133 A61P29/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel substituted derivatives of 4-aminocyclohexanol of the general formula (I) being optionally as their physiologically acceptable salts and first of all physiologically compatible acids. In compound of the general formula (I) R¹ and R² mean independently of one another hydrogen atom (H) or (C₁-C₈)-alkyl that can be saturated or unsaturated but both R¹ and R² can't mean simultaneously H, or residues R¹ and R form a ring in common and mean (CH₂)_3-6; R² means unsubstituted phenyl or phenyl substituted with halogen atom that is added through saturated or unsaturated, branched or linear (C₁-C₄)-alkyl group; R⁴ means heteroaryl chosen from 5-membered heteroaryl wherein heteroatoms are chosen from nitrogen, oxygen or sulfur atoms and each of these atoms is condensed with benzene ring and means unsubstituted or monosubstituted (C₁-C₈)-alkyl; -CHR⁶R⁷, -CHR⁶-CH₂R⁷, -CHR⁶-CH₂-CH₂R⁷, -CHR⁶-CH₂-CH₂-CH₂R⁷ wherein R⁶ represents H; R⁷ represents phenyl that can be unsubstituted or mono- either multi-substituted with halogen atoms. Also, invention relates to a method for synthesis of compounds of the formula (I) and a medicinal agent based on thereof. Synthesized compounds can be sued for preparing a medicinal agent designated for treatment of pain being first of all acute, visceral, neuropathic or chronic pain, and to a medicinal agent designated for treatment of diseases mediated by function of ORL1-receptor, for example, such as fear state, epilepsy, cardiovascular diseases.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and drug.

10 cl, 1 tbl, 21 ex