NOVEL CRYSTALLINE FORM OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(5,6-DIHYDRO-4H-[1,2,4]TRIAZIN-1-YL)PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)THIOPHENE-2-CARBOXAMIDE METHANESULPHONATE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME Russian patent published in 2018 - IPC C07D413/14 C07D417/10 A61K31/53 A61P9/10 A61P29/00 

Abstract RU 2663617 C1

FIELD: chemistry.

SUBSTANCE: invention relates to the crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulphonate (GCC-4401C), characterised by an X-ray powder diffraction spectrum using Cu-Kα-radiation, having peaks at a diffraction angle 2θ, equal to 12.022, 15.721, 15.971, 18.125, 18.928, 19.979, 20.311, 20.726, 21.66, 22.805, 23.18, 23.985, 25.857, 27.25, 27.829, 28, 28.189 and 29.753. Invention also relates to a pharmaceutical composition having the properties of a blood coagulation factor inhibitor Xa, containing anhydrous crystalline 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulphonate according to the invention, as the active ingredient.

EFFECT: crystalline form of the compound of the invention has excellent stability and can be effectively used to prevent or treat diseases such as thrombosis, heart attack, arteriosclerosis, inflammation, stroke, stenocardia, recurrent stricture after angioplasty and thromboembolism.

5 cl, 8 dwg, 8 tbl, 4 ex

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RU 2 663 617 C1

Authors

Choj Soongiu

Choj Dzungsub

Joon So-Khiun

Kim Joo Khoon

Kim Dzae Jeon

Li Suk Kho

Cho Joung Lag

Song Kho Joung

Li Dae Jon

Baek Sung Joon

Chae Sang Eun

Park Tae Kio

Voo Sung Kho

Kim Jong Zu

Dates

2018-08-07Published

2014-07-18Filed