DERIVATIVES OF AMINOFLUORPIPERIDINE AS A KINASE INHIBITOR Russian patent published in 2021 - IPC C07D487/04 A61K31/519 A61P35/00 A61P37/00 

Abstract RU 2762637 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to compounds or to their pharmaceutically acceptable salts selected from: 1) 1-((3S,4R)-3-(5-chloro-2-(1-ethyl-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 2) 1-((3S,4R)-3-(5-chloro-2-(1-(2, 2-difluoroethyl)-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 3) 1-((3S,4R)-3-(5-chloro-2-(1-cyclopropyl-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 4) 1-((3S,4R)-3-(5-chloro-2-(isoxazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 5) 1-((3S,4R)-3-(5-chloro-2-(isothiazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 6) 4-((3S,4R)-1-acryloyl-4-fluoropiperidin-3-ylamino)-2-(1-ethyl-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile, 7) 4-((3S,4R)-1-acryloyl-4-fluoropiperidin-3-ylamino)-2-(1-(2,2-difluoroethyl)-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile, 8) 4-((3S,4R)-1-acryloyl-4-fluoropiperidin-3-ylamino)-2-(1-cyclopropyl-1H-pyrazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile, 9) 4-((3S,4R)-1-acryloyl-4-fluoropiperidin-3-ylamino)-2-(isoxazole-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile, 10) 1-((3S,4R)-3-(2-(1-ethyl-1H-pyrazol-4-ylamino)-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one, 11) 1-((3S,4R)-4-fluoro-3-(2-(isoxazol-4-ylamino)-5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)prop-2-ene-1-one, and 12) 1-((3S,4S)-3-(5-chloro-2-(1-ethyl-1H-pyrazol-4-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-fluoropiperidin-1-yl)prop-2-ene-1-one. The invention also relates to a pharmaceutical composition for inhibiting the activity of JAK3 and/or BTK, containing the above compounds or pharmaceutically acceptable salts thereof.

EFFECT: production of new compounds and a pharmaceutical composition based thereon, potentially applicable in medicine for treating inflammatory and proliferative diseases.

2 cl, 2 tbl, 12 ex

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RU 2 762 637 C1

Authors

Kim, In Woo

Jeong, Seung Hwarn

Kim, Nam Youn

Lee, Jun Hee

Dates

2021-12-21Published

2018-12-28Filed