CRYSTALLINE FORMS OF 1-[(3R,4S)-4-CYANOTETRAHYDROPYRAN-3-YL]-3-[(2-FLUORO-6-METHOXY-4-PYRIDYL)AMINO]PYRAZOLE-4-CARBOXAMIDE Russian patent published in 2024 - IPC C07D405/14 A61K31/4439 A61P17/00 A61P17/04 A61P19/02 A61P35/00 

Abstract RU 2828229 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a crystalline form (form 1) 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide, characterized by a powder X-ray diffraction pattern (X-ray diffraction pattern), containing at least five peaks in °2θ(±0.2), selected from a group consisting of 6.9, 13.9, 17.8, 19.6, 20.4, 20.9, 24.7, 25.0, 26.6 and 29.1. Method involves deposition of a crystalline form from solution 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide and solvent; where the solution is heated at boiling point and then cooled; wherein the solvent is selected from a group consisting of methanol, dimethylacetamide or a mixture thereof; and boiling point ranges from 60 to 70 °C, and the solution is cooled to a temperature lower than 25 °C.

EFFECT: thermodynamically stable crystalline form of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide.

1 cl, 3 tbl, 9 dwg, 2 ex

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RU 2 828 229 C2

Authors

Chassaing, Christophe, Pierre, Alain

Jin, Xiaoling

Petrova, Rositza, Iordanova

Varsolona, Richard, J

Codan, Lorenzo

Cleator, Edward

Goodyear, Adrian

Simmons, Jonathan

Schweisel, Tanja

Dates

2024-10-08Published

2019-12-12Filed