BENZO-DERIVATIVES WITH SIX-MEMBERED RING AS DPP-4 INHIBITOR AND USE THEREOF Russian patent published in 2019 - IPC C07D311/92 C07D405/04 C07D417/04 C07D221/10 C07D335/04 A61K31/352 A61K31/5377 A61P3/00 A61P3/10 A61P7/10 A61P29/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a compound of general formula I, a pharmaceutically acceptable salt thereof or an optically active isomer thereof:

(I).

In formula (I), X is selected from O, S or NH; A is a benzene ring with 1–5 substituents, where each substitute is independently selected from halogen or cyano; R is H or hydroxy, n is 1–2; ring B is selected from an aromatic benzene ring, an aromatic heterocycle, a saturated or unsaturated 5-member or 6-member ring, an oxygen-containing five- or six-member saturated or unsaturated heterocycle, where R₁ is independently selected from a group consisting of halogen, cyano, hydroxy, C_1-6 alkyl, C_1-6 alkoxy, C_1-3 alkoxymethoxy, COOH, C_1-6 alkoxycarbonyl, NR²R³, C_1-6 alkylsulphonamido, C_1-5 alkylsulphonyl, C_3-5 cycloalkylsulphonyl or C_1-5 alkylsulphinyl, m is 1-4; R² and R³ together form a substituted or unsubstituted 5- or 6-membered cycloalkyl or a substituted or unsubstituted heterocyclic group containing N, O. Also disclosed are a pharmaceutical composition, use of the compound of formula (I) for preparing a drug and a method of producing the compound.

EFFECT: invention provides a compound of formula (I) as a DPP-4 inhibitor and use thereof for preventing or treating diseases associated with DPP-4.

13 cl, 1 tbl, 31 ex