SUBSTITUTED OXAZOLE DERIVATIVES WITH ANALGETIC ACTION Russian patent published in 2011 - IPC C07D263/48 C07D413/04 C07D413/06 C07D413/14 A61K31/421 A61K31/422 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to substituted oxazole derivatives of general formula I. The disclosed compounds have affinity to the µ-opioid receptor. In general formula I

, n equals 0, 1 or 2, R¹ denotes a phenyl residue bonded through a C₁-C₃alkyl chain, R² denotes phenyl or thienyl, each of which is unsubstituted or mono-substituted with F or Cl, R³ and R⁴ independently denote a saturated, branched or straight C₁-C₆alkyl, phenyl or a phenyl residue bonded through a C₁-C₃akyl chain, or R³ and R⁴ together form an unsubstituted five-, six- or seven-member saturated ring which can optionally contain an extra heteroatom selected from a group comprising O or NR⁹, where R⁹ denotes phenyl or a phenyl residue bonded through a C₁-C₃alkyl chain, any of which is unsubstituted or mono-substituted with a substitute selected from a group comprising F, Cl, Br, I and O-C₁-C₆alkyl, where the ring can be optionally condensed with a phenyl ring, R⁵ and R⁶ independently denote a saturated, branched or straight C₁-C₆alkyl, R⁷ and R⁸ independently denote a saturated, branched or straight unsubstituted C₁-C₆alkyl or a phenyl residue bonded through a C₁-C₃alkyl chain, or R⁷ and R⁸ together form an unsubstituted or mono- or disubstituted five-, six- or seven-member saturated ring, where the substitutes are selected from a group comprising C₁-C₆alkyl or a phenyl residue bonded through a C₁-C₃alkyl chain, where the ring can optionally contain an extra heteroatom selected from a group comprising S, O and NR¹⁰, where R¹⁰ denotes a phenyl or a phenyl residue bonded through a C₁-C₃alkyl chain, any of which can be unsubstituted or mono-substituted with O-C₁-C₆alkyl. The invention also relates to methods of producing the disclosed compounds, a medicinal agent containing at least one substituted oxazole derivative of formula I, use of the compounds to prepare a medicinal agent.

EFFECT: improved properties.

13 cl, 1 tbl, 150 ex