SUBSTITUTED HETEROARYLPIPERIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS Russian patent published in 2012 - IPC C07D401/04 C07D401/14 C07D417/14 C07D453/02 A61K31/44 A61P3/04 A61P3/10 A61P15/00 A61P35/00 A61P25/00 A61P25/22 A61P25/24 

FIELD: chemistry.

SUBSTANCE: invention relates to substituted heteroarylpiperidine derivatives of formula (I) and enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof, where R¹ denotes -N(R¹⁰)-(C(R⁶)₂)_m-T, (C(R⁶)₂)₁-T or -O-(C(R⁶)₂)_m-T; R⁶ is independently selected from H, OCH₃, C_1-6-alkyl, possibly substituted with 1-3 substitutes which are halogen, and C_3-6-cycloalkyl, possibly substituted with 1-3 substitutes which are halogen, T denotes NR⁷R⁸, , , , or ; R⁷ and R⁸ are independently selected from H, C_1-6-alkyl; R⁹ is independently selected from OH, C_1-6-alkyl, O-C_1-6-alkyl, or NR¹²R¹³; R¹⁰ denotes H or C_1-6-alkyl; R¹² and R¹³ are independently selected from C_1-6-alkyl, possibly substituted with OH, C_2-6-alkylene-O-C_1-6-alkyl and W denotes CH, O or NR¹⁰; B denotes CR² or N; G denotes CR² or N; D denotes CR² or N; E denotes CR² or N; provided that one or more of variables B, G, D and E must be N; R² is independently selected from H, F, Cl, CH₃, OCH₃ and CF₃; R³ denotes: H, CI, F or CH₃; R⁴ denotes Cl, F or CH₃, R⁵ denotes , morpholine, possibly substituted with 1-3 identical or different substitutes R¹⁴, a 4-7-member saturated or partially unsaturated heterocycle containing one nitrogen atom in the ring and possibly an additional heteroatom selected from O, N and S, where the heterocycle is possibly substituted with 1-4 identical or different substitutes R¹¹, or NR¹²R¹³; R¹¹ is indendently selected from halogen, OH, C_1-6-alkyl, possibly substituted with 1-3 substitutes which are halogen, C_2-6-alkynyl, -C_0-6-alkyl-C_3-6-cycloalkyl, -OC(O)C_1-6-alkyl, -NH₂, -NH(C1-6-alkyl) and -N(C_1-6-alkyl)₂; A denotes a 3-7-member saturated ring; R¹² and R¹³ are independently selected from C_1-6-alkyl, possibly substituted with OH, C_2-6-alkylene-O-C_1-6-alkyl; R¹⁴ denotes C_1-6-alkyl; 1 equals 0, 1, 2, 3 or 4; m equals 0, 1, 2, 3 or 4; o equals 0, 1 or 2; p equals 0, 1, 2, 3 or 4; r equals 0, 1, 2, 3 or 4; s equals 1 or 2 and t equals 0 or 1. The invention also relates to use the compound of formula I to produce a drug for treating or preventing disorders, diseases or conditions responsible for inactivation or activation of the melanocortin-4 receptor in mammals, and to a pharmaceutical composition based on said compounds.

EFFECT: novel compounds which can be used as melanocortin-4 receptor modulators are obtained and described.

10 cl, 134 ex, 16 tbl