CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS

FIELD: organic chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a compound of formula I or a pharmaceutically acceptable salt thereof (I),where A is selected from phenyl, isoindolinyl, quinolinyl, pyridinyl,,2,3-dihydro-1-indenyl, benzothazolyl and 1,2,3,4-tetrahydroisoqu...

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Hauptverfasser: BRUBEJKER Dzhejson, LYU Yujmej, TORRES Luis, KUN Norman, CHAJLDERS Mettyu Llojd, SKOTT Mark E, CHZHAN Khuntszyun, GERIN Devid, VAN Chungan, TSZEN Khunbo, BAJ Yunfyn, PU Tsinlin, FULLER Piter, TOMPSON Kristofer F, FOLKON Deniell, DINSMOR Kristofer, DU Syaosin, TSAJ Tszyatsyan, CHZHEN Chzhisyan, KATTS Dzhejson Devid
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry.SUBSTANCE: invention relates to organic chemistry, specifically to a compound of formula I or a pharmaceutically acceptable salt thereof (I),where A is selected from phenyl, isoindolinyl, quinolinyl, pyridinyl,,2,3-dihydro-1-indenyl, benzothazolyl and 1,2,3,4-tetrahydroisoquinolinyl; n is 0, 1, 2, or 3; m is 0, 1, 2, or 3; p is 2, 3, or 4; Ris selected from: halogen, oxo(=O), Calkyl(oxy)(carbonyl)Calkyl, CcycloalkylCalkyl, heteroaryl (carbonyl)Calkyl, where heteroaryl is a 5-6 membered ring containing 1-3 heteroatoms selected from nitrogen, nitrogen and oxygen, and nitrogen and sulphur, (C)heterocycloalkyl(carbonyl)Calkyl, where the 3-12 membered heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen, oxygen, nitrogen, sulphur, nitrogen and oxygen, and oxygen and sulphur, Calkyl(oxy)(carbonyl)aminoCalkyl, heteroaryl(carbonyl)aminoCalkyl, where heteroaryl is a 5-6 membered ring containing 1-2 heteroatoms selected from nitrogen and oxygen, Calkylamino(carbonyl)Calkyl, heteroarylamino(carbonyl)Calkyl, wherein heteroaryl is a 5-membered ring containing 1-2 heteroatoms selected from nitrogen, Calkylsulfonyl, (C)cycloheteroalkylsulfonylCalkyl, where cycloheteroalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, Calkylsulfonimidoyl, CalkylthioCalkyl, -COH, -SONH, -SONH(Calkyl), -SON(Calkyl), -(Calkyl)OH, -Calkylalkoxy, cyano, and Chaloalkyl; and where two Rmay optionally bind to ring atoms to which they are attached to form a 3 to 6-membered ring; Ris selected from: halogen, Calkyl, (C)heterocycloalkyl, where heterocycloalkyl contains 1 nitrogen heteroatom, CcycloalkylCalkylamino, (Calkyl)amino, and hydroxy, where two Rmay optionally be bound to a ring atom to which each is attached to form a 3-6 membered saturated ring; and where Rand Reach is optionally substituted with 1, 2, 3 or 4 substituents R; Ris independently selected from: halogen, Calkyl, phenyl, Ccycloalkyl, piperidinyl, -CO(Calkyl), -COH, amino, (Calkyl)amino, hydroxy, (Calkyl) OH, CalkoxyCalkyl, (Calkyl) cyano, CalkylsulfinylCalkyl, -O(C=O)Calkyl, oxo and Chaloalkyl. Invention also relates to a pharmaceutical composition capable of inhibiting the activity of Janus kinases JAK1 and JAK2, and methods of treatment based on said compounds.EFFECT: technical result: novel compounds are obtained, that can be used in medicine for treatment of arthritis, asthma and obstructive airways diseases, autoimmune diseases or disorders and cancer.14 cl, 22 ex, 50 tbl И