CRYSTALLINE FORMS OF [(S)-1-CARBAMOYL-2-(PHENYLPYRIMIDIN-2-YLAMINO)ETHYL]AMIDE 2-(2-METHYLAMINOPYRIMIDIN-4-YL)-1H-INDOLE-5-CARBONIC ACID Russian patent published in 2017 - IPC C07D403/14 A61K31/506 A61P29/00 A61P19/02 

FIELD: chemistry.

SUBSTANCE: invention relates to the novel polymorph 1 ((S)-1-carbamoyl-2-(phenylpyrimidin-2-ylamino)ethyl]amide 2-(2-methylaminopyrimidin-4-yl)-1H-indole-5-carboxylic acid and method for its preparation. Polymorph 1 of the compound has the properties of IkB kinase inhibitors and can be used for the treatment of inflammatory, immunologically or metabolically mediated acute and chronic arthritis, arthropathies, rheumatoid arthritis, degenerative joint diseases, spondylosis, diabetes II type, inflammatory bowel disease, loss of cartilage following joint trauma or a relatively long period of joint immobilization after meniscus or patella injuries or torn ligaments, or diseases of the connective tissue, m algy or disorders of bone metabolism, and also for the treatment of pain, including acute pain and chronic pain. Polymorph 1 has characteristic reflections in a powder X-ray diffraction pattern using CuK-alpha1 radiation in the reflection mode at 2 theta angles (in degrees) of 14.9±0.2, 19.4±0.2, 19.7±0.2, 20.0±0.2, 22.3±0.2, 25.0±0.2. The method of producing polymorph 1 involves heating the polymorph 2 of mentioned compound in a mixture of acetone and water to a temperature of 50 to 60°C, cooling the mixture to a temperature of 20 to 25°C and precipitate precipitation. In this case polymorph 2 has a characteristic x-ray powder reflection using CuK-Alpha1 radiation reflection mode with 2 Theta angles (degrees): 5.8±0.2, 6.7±0.2, 9.3±0.2, 11.2±0.2, 16.5±0.2, 18.1±0.2, 19.4±0.2, 22.1±0.2, as well as indicators of DSC peaks 222.1±1; 248.1±1; 251±1 at heating rate 10°C/minute.

EFFECT: polymorphic form 1 is thermodynamically stable, has low hygroscopicity and stability.

8 cl, 2 tbl, 5 dwg