HYDROCHLORIDE FORM OF INHIBITOR OF DIPEPTIDYLPEPTIDASE IV AND METHOD OF PRODUCING SALT FORM Russian patent published in 2020 - IPC C07D495/04 A61K31/519 A61P3/10 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidin-6-carboxylic acid of formula (1)

,

which is selected from a group consisting of hydrochloride, maleate, phosphate and glycolate, and a method of producing a salt form, wherein the powder X-ray diffraction pattern of the hydrochloride crystal includes following values 2θ: 7.43±0.2°; 11.06±0.2°; 11.70±0.2°; 13.46±0.2°; 15.03±0.2°; 15.34±0.2°; 18.32±0.2°; 21.96±0.2°; 24.01±0.2°; 27.20±0.2°; 29.32±0.2°; 30.26±0.2°; pattern of powder x-ray diffraction of a maleate crystal includes following values 2θ: 7.55±0.2°; 12.41±0.2°; 15.45±0.2°; 17.50±0.2°; 20.89±0.2°; 26.59±0.2°; 26.93±0.2°; pattern of powder X-ray diffraction of a phosphate crystal includes following values 2θ: 11.99±0.2°; 12.20±0.2°; 14.80±0.2°; 20.11±0.2°; 20.46±0.2°; 24.18±0.2°; 24.68±0.2°; pattern of powder X-ray diffraction of a glycolate crystal includes following values 2θ: 8.92±0.2°; 10.20±0.2°; 13.35±0.2°; 16.89±0.2°; 19.37±0.2°. Also disclosed is a pharmaceutical composition of a salt form of the compound of formula I.

EFFECT: according to the present invention, the salt form has a high degree of hypoglycemic activity in vivo and is a novel pharmaceutically active compound, intended for treating or preventing type 2 diabetes mellitus and/or complications caused by type 2 diabetes mellitus.

9 cl, 4 ex, 24 dwg