ANTAGONISTS OF TRPV1, CONTAINING DIHYDROXY GROUP AS SUBSTITUTE, AND THEIR USE Russian patent published in 2017 - IPC C07D417/14 A61K31/496 A61P29/00 A61P19/02 A61P13/00 A61P1/04 A61P25/04 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, in which R₁ represents -halo or -CF₃; R₄ represents -H or -CH₃; each of R₈ and R₉ independently represents -H, -halo, -CH₃ or -OCH₃, each halo independently represents -F, -Cl, -Br or -I; and m means an integer of 0 or 1; (1) provided that if R₄ represents -H, the m means 1; and (2) provided that if R₄ represents -H and the carbon atom in the position a of the a-b bond is in (S)-configuration, the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group, a (S)-3-methyl group or a (R)-3-methyl group; (3) provided that if R₄ represents -H, the carbon atom in position a of the a-b bond is in (S)-configuration, R₈ represents -H and R₉ represents -halo, then the methyl group connected to piperazinonyl ring represents a (R)-3-methyl group; (4) provided that if R₄ represents -H, the carbon atom in position a of the a-b bond is in (S) configuration, R₈ represents -F and R₉ represents -F, then the methyl group connected to piperazinonyl ring represents a (S)-2-methyl group or a (S)-3-methyl group; and (5) provided that if R₄ represents -CH₃, each of the carbon atoms in positions a and c and the a-b bond and the c-d bond is in (S) configuration,R₈ represents -H, R₉ represents -halo, and m means 1, the methyl group connected to piperazinonyl ring is a (S)-3-methyl group or a (R)-3-methyl group. Invention also relates to a compound of formula (II) or a pharmaceutically acceptable salt thereof, a specific compound of formula (Ia) or a pharmaceutically acceptable salt thereof and / or a co-crystal of fumaric acid. Invention also relates to specific compounds of formula (Ib) or a pharmaceutically acceptable salt thereof. The compounds as per invention are intended to inhibit the function of TRPV1 in a cell and to treat pain, pain associated with osteoarthritis, osteoarthritis, urinary incontinence (UI), ulcer, inflammatory bowel disease (IBD) or irritable bowel syndrome (IBS) in an animal.

EFFECT: compounds having an affinity for the receptor TRPV1.

38 cl, 11 tbl, 3 dwg, 16 ex