CRYSTAL OF COMPOUND POSSESSING JAK1 INHIBITORY ACTIVITY Russian patent published in 2019 - IPC C07D513/04 A61K31/506 A61P37/00 A61P35/00 A61P25/00 A61P11/00

Abstract RU 2705721 C1

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and pharmaceutics, specifically to methyl[1-({6-[(2S)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]thiazol-7-yl)pyrimidin-4-yl}carbonyl)piperidin-4-yl]carbamatosylate monohydrate, methyl[1-({6-[(2R)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]thiazol-7-yl)pyrimidin-4-yl}carbonyl)piperidin-4-yl]carbamatosylate monohydrate, methyl(1-{[6-{[(1S)-1-cyclopropyl-ethyl]amino}-2-(pyrazolo[5,1-b][1,3]thiazol-7-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)carbamatosylate monohydrate and their crystals. Invention also relates to crystal of ethyl(1-{[6-{[(1S)-1-cyclopropylethyl]amino}-2-(pyrazolo[5,1-b][1,3]thiazol-7-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)carbamate, crystal of N-(1-{[6-{[(1S)-1-cyclopropylethyl]amino}-2-(pyrazolo[5,1-b][1,3]thiazol-7-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)cyclopropanecarboxamide and crystal of N-(1-{[6-{[(2R)-3,3-dimethylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]thiazole-7-yl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)cyclopropanecarboxamide. There are also described pharmaceutical compositions possessing JAK1 inhibitory activity based on said compounds.

EFFECT: obtaining novel compounds and pharmaceutical compositions based thereon, which can be used in medicine in treating diseases such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, vasculitis, bronchial asthma, chronic obstructive pulmonary disease, eosinophilic maxillary sinusitis and nasal polyp.

15 cl, 1 tbl, 6 dwg, 6 ex

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RU 2 705 721 C1

Authors

Higuchi Fumi

Dates

2019-11-11—Published

2017-02-28—Filed