首页> 外国专利> N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS

N-(2-CYANO HETEROCYCLYL)PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS

机译:N-(2-氰基杂环基)吡唑并吡咯烷类抑制剂

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt or stereoisomer thereof, which have the properties of a Janus kinase inhibitor (JAK). In formula I A is selected from phenyl and heteroaryl; X is independently selected from CH2 and O, wherein at least one X is other than CH2; n is equal to 0; m is equal to 0, 1, 2, 3 or 4; p is equal to 2, 3, 4 or 5; R1 is selected from halogen, oxo (=O), C0-10alkyliminoC0-10alkyl, C1-10alkyl(oxy)0-1(carbonyl)0-1C0-10alkyl, heteroarylC0-10alkyl(oxy)0-1(carbonyl)0-1C0-10alkyl, (C3-12)heterocycloalkylC0-10alkyl(oxy)0-1(carbonyl)0-1C0-10alkyl, C0-10alkyl(oxy)0-1(carbonyl)0-1aminoC0-10alkyl, C3-12cycloalkylC0-10alkyl(oxy)0-1(carbonyl)0-1aminoC0-10alkyl, C0-10alkylamino(oxy)0-1(carbonyl)0-1C0-10alkyl, C3-12cycloalkylamino(hydroxy)0-1(carbonyl)0-1C0-10alkyl, C0-10alkylsulfonylC0-10alkyl, (C3-12)heterocycloalkylC0-10alkylsulfonylC0-10alkyl, (C0-10alkyl)1-2amino, -SO2NH2, -SO2NH(C1-10alkyl), -SO2N(C1-10alkyl)2, C1-10alkylsulfinylC0-10alkyl, thioC1-10alkyl, hydroxy, -(C1-10alkyl)OH, -C0-10alkylalkoxy, cyano, (C1-6alkyl)cyano and C1-6haloalkyl. Invention also relates to a pharmaceutical composition containing the above compounds. .;EFFECT: proposed N-(2-cyano heterocyclyl)pyrazolo pyridones as the Janus kinase inhibitors.;7 cl, 10 tbl, 113 ex
机译:发明领域本发明涉及具有Janus激酶抑制剂(JAK)特性的式I化合物或其药学上可接受的盐或立体异构体。式I中,A选自苯基和杂芳基; X独立地选自CH 2 和O,其中至少一个X不是CH 2 ; n等于0; m等于0、1、2、3或4; p等于2、3、4或5; R 1 选自卤素,氧代(= O),C 0-10 烷基亚氨基C 0-10 烷基,C 1- 10 烷基(氧基) 0-1 (羰基) 0-1 C 0-10 烷基,杂芳基C 0 -10 烷基(氧基) 0-1 (羰基) 0-1 C 0-10 烷基,(C 3-12 )杂环烷基C 0-10 烷基(氧基) 0-1 (羰基) 0-1 C 0-10 烷基,C 0-10 烷基(氧基) 0-1 (羰基) 0-1 氨基C < Sub> 0-10 烷基,C 3-12 环烷基C 0-10 烷基(氧基) 0-1 (羰基) 0-1 氨基C 0-10 烷基,C 0-10 烷基氨基(氧基) 0-1 (羰基) 0-1 C 0-10 烷基,C 3-12 环烷基氨基(羟基) 0-1 (羰基) 0-1 C 0-10 烷基,C 0-10 烷基磺酰基C 0-10 烷基,( C 3-12 )杂环烷基C 0-10 烷基磺酰基C 0-10 烷基,(C 0-10 烷基) 1-2 氨基,-SO 2 NH 2 ,-SO 2 NH(C 1-10 烷基),-SO 2 N( C 1-10 烷基) 2 ,C 1-10 烷基亚磺酰基C 0-10 烷基,硫代C 1-10 烷基,羟基,-(C 1-10 烷基)OH,-C 0-10 烷基烷氧基,氰基(C 1 -6 烷基)氰基和C 1-6 卤代烷基。本发明还涉及含有上述化合物的药物组合物。 。;效果:建议将N-(2-氰基杂环基)吡唑并吡啶酮用作Janus激酶抑制剂;; 7 cl,10 tbl,113 ex

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