CRYSTALLINE FORM OF BISULPHATE JAK-KINASE INHIBITOR AND A METHOD FOR PRODUCTION THEREOF Russian patent published in 2020 - IPC C07D487/04 A61K31/519 A61P19/02 A61P29/00 

Abstract RU 2716260 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a crystalline form of a bisulfate JAK-kinase inhibitor. Crystalline form II of bisulphate (3aR,5s,6aS)-N-(3-methoxyl-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydro-cyclopenta[c]pyrrol-2(1H)-formamide has X-ray powder diffraction spectrum, which is obtained by using Cu-Kα radiation and is represented by angle 2θ and interplanar distance, where characteristic peaks are given at approximately 8.96 (9.87); 11.80 (7.50); 13.12 (6.74); 13.53 (6.54); 13.89 (6.37); 14.42 (6.14); 14.98 (5.91); 16.52 (5.36); 18.20 (4.87); 18.75 (4.73); 19.15 (4.63); 19.72 (4.50); 20.82 (4.26); 22.05 (4.03); 22.52 (3.95); 22.92 (3.88); 23.58 (3.77) and 27.04 (3.30). Crystalline form II is intended for preparing a pharmaceutical composition for preparing a drug for treating a JAK-related disease, which is rheumatic and rheumatoid arthritis.

EFFECT: invention discloses a crystalline form of a bisulfate JAK-kinase inhibitor and a method for production thereof.

5 cl, 4 dwg, 2 tbl, 14 ex

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RU 2 716 260 C2

Authors

Sun Pyaoyan

U Guajli

Chzhan Tsyuanlyan

Chen Yuntszyan

Shen Lintszya

Dates

2020-03-11Published

2015-10-09Filed