CRYSTALLINE SOLID FORM OF A BENZENE SULPHONIC ACID SALT AND 2-[(4S)-6-(4-CHLOROPHENYL)-1-METHYL-8-(METHYLOXY)-4H-[1,2,4]TRIAZOLO[4,3-A][1,4]BENZODIAZEPIN-4-YL]-N-ETHYLACETAMIDE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF Russian patent published in 2019 - IPC C07D487/04 A61K31/5517 A61P29/00 A61P35/00 A61P37/02 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a benzenesulphonic acid salt and 2-[(4S)-6-(4-chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide in crystalline solid form, characterized by powder X-ray powder diffraction (XRPD) pattern, containing at least three diffraction angles, expressed in degrees 2θ, selected from a group consisting of approximately 5.5, 7.4, 9.1, 10.0, 10.4, 13.3, 13.6, 14.9, 18.7, 20.4, 20.9, 22.8 and 23.1° (±0.1°); and/or ¹³C solid-state nuclear magnetic resonance (NMR) spectrum comprising at least ten peaks expressed in terms of chemical shifts in ppm^-1, selected from a group consisting of peaks at approximately 169.6, 167.5, 165.6, 160.1, 159.4, 157.1, 155.9, 154.3, 152.4, 146.9, 145.8, 140.0, 137.9, 135.9, 133.4, 132.0, 130.6, 129.9, 128.3, 127.1, 125.6, 123.5, 120.6, 119.1, 114.1, 113.7, 58.0, 53.6, 53.1, 40.7, 37.0, 34.9, 15.8, 14.7 and 12.0 (±0.2 mln^-1). Invention also relates to a pharmaceutical composition and a method of producing a salt.

EFFECT: technical result is obtaining a new stable crystalline solid form of benzene sulphonic acid salt and 2-[(4S)-6-(4-chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide, which provides suitable properties for the development of a pharmaceutical product.

8 cl, 2 dwg, 2 tbl, 5 ex