BORATE DERIVATIVE OF AZETIDINE Russian patent published in 2023 - IPC C07F5/04 A61K31/69 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a borate compound of an azetidine derivative, in particular to a compound of formula (I), a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof or a geometric isomer thereof. In the formula (I): ring A is selected from a group consisting of phenyl and 5-10 membered heteroaryl, where the heteroaryl contains at least one ring atom selected from the group consisting of N, O and S; each R¹ is independently selected from the group consisting of halogen, CN, OH, NH₂ and C_1-6alkyl, where C_1-6alkyl is optionally substituted with one or more groups selected from the group consisting of halogen, OH and NH₂; n is selected from the group consisting of 0, 1, 2, 3, 4 and 5; each of R² and R³ is independently selected from the group consisting of H; R⁴ is selected from C_1-6alkyl; R⁵ is selected from the group consisting of H; ring D is selected from a 5-10 membered heterocyclyl wherein the 5-10 membered heterocyclyl is substituted with at least one =O, and wherein the heteroatoms in the ring atoms of the 5-10 membered heterocyclyl include only boron and oxygen atoms; each R⁶ is independently selected from the group consisting of C_1-6alkyl, where C_1-6alkyl is optionally substituted with one or more COOH groups; and m is selected from the group consisting of 0, 1, 2, 3, 4 and 5. Also a crystal of compound I-1, a pharmaceutical composition containing the above compound or crystal, a method of treating multiple myeloma, and the use of the above compound, crystal or pharmaceutical composition are provided.

EFFECT: proposed compound can be used to prevent or treat multiple myeloma.

37 cl, 2 dwg, 9 tbl, 8 ex