DIPEPTIDYL PEPTIDASE-IV INHIBITORS Russian patent published in 2016 - IPC C07D207/10 C07D207/12 C07D211/46 C07D213/12 C07D401/12 C07D403/12 C07D413/12 C07D413/14 C07D417/12 A61K31/40 A61K31/4025 A61K31/4196 A61K31/4245 A61K31/4439 A61K31/46 A61K31/497 A61K31/5377 A61K31/541 A61P1/00 A61P25/00 A61P25/28 A61P3/04 A61P3/06 A61P3/10 A61P9/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula

,

its stereoisomers or pharmaceutically acceptable salts, wherein Y means -CH₂-, -CHF- or -CF₂-; m = 1, n = 1 or 2, and p represents integers optionally specified in 0, 1 or 2; X means a bond, C₁-C₅-alkylene or -C(=O)-; R¹ means hydrogen, groups specified in alkyl, -S(O)_PR¹⁰, -NR¹⁰S(O)_pR¹¹, -CN, -NR¹⁰R¹¹, -NR¹⁰COR¹¹ or 5-6-merous heterocyclic rings with 1-4 heteroatoms specified in N, O and S, which is optionally substituted by alkoxy, hydroxy, hydroxyalkyl, halogenalkyl, cycloalkyl, aryl, arylalkyl, 6-merous heteroaryl cycle with 1-2 nitrogen atoms or one or more oxo, alkyl, halogen; the substitutes are optionally additionally substituted by one or more halogen atoms; R², R³ and R⁴ independently mean hydrogen or alkyl; R² and R⁴ may be combined to form an optionally substituted 6-7-merous cycle with 1 heteroatom specified in N and O, wherein the substitutes are specified in one or more oxo or alkyl; R⁵ means hydrogen or alkyl group; R⁶ means hydrogen or alkyl; R⁷ means hydrogen or alkyl; R⁸ means -CN; R¹⁰ and R¹¹ independently mean hydrogen or optionally substituted groups specified in alkyl, cycoalkyl, cycloalkylalkyl, aryl, arylalkyl and 6-merous heterocyclyl with one nitrogen atom; when groups R¹⁰ and R¹¹ are substituted with the substitutes representing one or more substitutes specified in halogens, cyano, oxo (=O), thioxo (=S), thioalkyl, amino, alkyl, halogenalkyl and -SO₂R^a; wherein R^a means alkyl; the above groups represent C₁-C₆ alkyl groups; the above cycloalkyl groups represent C₃-C₁₀ cycloalkly groups; the above aryl groups represent C₆-C₁₀ aryl groups; the above halogens are specified in fluorine, chlorine bromine and iodine. The compounds of formula (I) are produced by binding the compound of formula , which is presented in the free, saline or protected form, with the compound of formula , wherein L means leaving groups specified in chlorine, bromine, iodine, tosylates, mesylates, triflates; PG means hydrogen or protective groups containing acetyl, trifluoracetyl, arylsulphonyl, nosyl, tosyl, -Boc or -CBz. The invention also refers to intermediate compounds of formula (II). The compounds of formula (I) aim at treating diseases controlled or normalised by DPP-IV inhibition.

EFFECT: dipeptidyl peptidase (DPP-IV) inhibitors effective for treating conditions controlled or normalised by DPP-IV inhibition, particularly type II diabetes mellitus.

19 cl, 2 tbl, 83 ex