PYRAZOLOTHIAZOLE COMPOUND AND DRUG CONTAINING THEREOF Russian patent published in 2019 - IPC C07D513/04 A61K31/506 A61P11/06 A61P13/12 A61P17/00 A61P17/14 A61P29/00 A61P35/00 A61P37/00 A61P37/08 A61P43/00 

FIELD: chemistry.

SUBSTANCE: invention relates to pyrazolothiazole compound represented by formula [I], where R¹ is hydrogen, C1-6alkyl or C1-6alkoxy; Z is -OR³ or -NR⁴R⁵; where R³ is C1-6alkyl, C1-6alkyl substituted with C3-6cycloalkyl, C3-6cycloalkyl, phenyl or pyridyl; R⁴ is hydrogen or C1-6alkyl; R⁵ is C1-6alkyl, C3-6cycloalkyl or a saturated heterocyclic group selected from oxane, piperidine, pyrrolidine, oxetane, said C1-6alkyl in R⁵ is optionally substituted with one or two groups selected from the group consisting of following (1)–(5): (1) hydroxy, (2) C1-6alkoxy and difluoro C1-6alkoxy, (3) C3-6cycloalkyl, C3-6cycloalkyl, substituted (difluoro C1-6alkoxy) C1-6alkyl, and C3-6 cycloalkyl substituted with C1-6alkoxyC1-6alkyl, (4) a saturated heterocyclic group selected from tetrahydropyran, optionally substituted (difluoro C1-6alkoxy)C1-6alkyl, and (5) phenyl, substituted with fluorine, and phenyl, substituted C1-6alkoxy, said C3-6cycloalkyl in R⁵ optionally substituted with one or two groups selected from a group consisting of (1)–(3): hydroxy, (2) C1-6alkoxy and difluoro C1-6alkoxy, and (3) nitrile, and said oxane, piperidine, pyrrolidine, oxetane in R⁵ are optionally substituted with one group selected from the group consisting of following (1)–(3): (1) C1-6alkyl, (2) C1-6alkylcarbonyl, and (3) C1-6alkoxycarbonyl; R² is hydroxy or -NHR⁸, where R⁸ is heteroaryl (pyrimidine, thiazole), heteroaryl (pyridine), optionally substituted with fluorine or C1-6alkyl, 1,2-oxazole, optionally substituted with C1-6alkyl, or -COL¹, -COOL² or -SO₂L³, said L¹ represents a group selected from a group consisting of following (1)–(5): (1) C1-6alkyl, difluoro C1-6alkyl and C1-6alkyl, substituted C1-6alkoxy, (2) C3-6cycloalkyl, (3) phenyl, (4) pyridine and thienyl, and (5) C1-6 dialkylamino and C3-6cycloalkylamino, said L² represents a group selected from a group consisting of following (1)–(3): (1) C1-6alkyl, monohalogen C1-6alkyl, dihaloC1-6alkyl, trihaloC1-6alkyl, and C1-6alkyl, substituted C1-6alkoxy, (2) C3-6cycloalkyl, and (3) C1-6 dialkylamino C1-6alkyl, and said L³ represents C1-6alkyl or C3-6cycloalkyl, or its pharmaceutically acceptable salt or its hydrate.

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EFFECT: compound of the present invention has inhibitory activity on JAK1.

10 cl, 7 tbl, 264 ex