5-MEMBERED N-HETEROCYCLIC COMPOUNDS WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY Russian patent published in 2005 - IPC

FIELD: pharmaceutical industry, medicine.

SUBSTANCE: invention relates to 5-membered N-heterocyclic compounds and salts thereof having hypoglycemic and hypolipidemic activity of general formula I , wherein R¹ is optionally substituted C₁-C₈-alkyl, optionally substituted C₆-C₁₄-aryl or optionally substituted 5-7-membered heterocyclic group, containing in ring 1-4 heteroatoms selected from oxygen, sulfur and nitrogen; or condensed heterocyclic group obtained by condensation of 5-7-membered monoheterocyclic group with 6-membered ring containing 1-2 nitrogen atoms, benzene ring, or 5-membered ring containing one sulfur atom; { is direct bond or -NR⁶-, wherein R⁶ is hydrogen atom or C₁-C₆-alkyl; m = 0-3, integer; Y is oxygen, -SO-, -SO₂- or -NHCO-; A ring is benzene ring, condensed C₉-C₁₄-aromatic hydrocarbon ring or 5-6-membered aromatic heterocyclic ring containing 1-3 heteroatoms selected from oxygen and nitrogen, each is optionally substituted with 1-3 substituents selected from C₇-C₁₀-aralkyloxy; hydroxyl and C₁-C₄-alkoxy; n = 1-8, integer; B ring is nitrogen-containing 5-membered heterocycle optionally substituted with C₁-C₄-alkyl; X¹ is bond, oxygen or -O-SO₂-; R² is hydrogen atom, C₁-C₈-alkyl, C₇-C₁₃-aralkyl or C₆-C₁₄-aryl or 5-6-membered heterocyclic group containing in ring 1-3 heteroatoms selected from oxygen, sulfur and nitrogen, optionally substituted with 1-3 substituents; W is bond, C₁-C₂₀-alkylene or C₁-C₂₀-alkenylene; R³ is -OR⁸ (R⁸ is hydrogen or C₁-C₄-alkyl) or -NR⁹R¹⁰ (R⁹ and R¹⁰ are independently hydrogen or C₁-C₄-alkyl). Compounds of present invention are useful in treatment of diabetes mellitus, hyperlipidemia, reduced glucose tolerance, and controlling of retinoid-associated receptor.

EFFECT: new medicines for treatment of diabetes mellitus, hyperlipidemia, etc.

26 cl, 518 ex, 3 tbl