INCRETIN SECRETAGOGUES, METHODS FOR PREPARING AND APPLYING THEM Russian patent published in 2012 - IPC C07D471/02 C07D267/20 C07D498/04 A61K31/553 A61K31/519 A61K31/4985 A61P25/28 A61P9/00 A61P3/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of general formula 1, or their pharmaceutically acceptable salts showing the properties of incretin secretagogues, preferentially the properties of a bile acid receptor TGR5 agonist. The compounds are applicable for treating metabolic diseases associated with glucose metabolism, such as diabetes, obesity, metabolic syndrome, etc. In formula 1 R1, R2 and R3 independently represent a cyclic system substitute specified in: hydrogen, C₁-C₃alkyl, halogen, a trifluoromethyl group, C₁-C₃alkoxy, a cyano group, a trifluoromethoxy group; an amino group substituted by C₁-C₃alkyl; or two radicals R3, found at carbon neighbours in a benzene ring, together with the benzene ring bound therewith form 3,4-methylene dioxyphenyl; R4 represents hydrogen, C₁-C₅alkyl, a carboxyl group, C₁-C₃alkoxycarbonyl or an amide group CONHR5; R5 is an optionally substituted by C₁-C₃alkyl, C₅-C₆cycloalkyl optionally substituted by phenyl, benzyl, pyridyl; X and Y represent two hydrogen atoms or an oxygen atom, provided Y=O, then X=2H, provided Y=2H, then X=O or X=Y=2H; the sign (N) shows the possibility of bioisosteric substitution of the benzene ring by the pyridine, pyrimidine, pyridazine, triazine or pyrazine ones.

EFFECT: preparing the pharmaceutical composition and the combined drugs with the use of the compounds of formula 1 or the based pharmaceutical composition and a protein kinase DPP-IV inhibitor specified in Vildagliptin or Sitagliptin, and/or an endogenous bile acid or mied bile acid secretagogues.

53 cl, 7 dwg, 8 ex