首页> 外国专利> 2-PHENYL-OXAZOLE-4-CARBOXAMIDE DERIVATIVES, MODULATING ACTIVITY OF JAK AND TYK2 KINASE

2-PHENYL-OXAZOLE-4-CARBOXAMIDE DERIVATIVES, MODULATING ACTIVITY OF JAK AND TYK2 KINASE

机译:2-苯基-恶唑-4-羧酰胺衍生物,调节JAK和TYK2激酶的活性

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to organic chemistry, specifically to novel oxazole derivatives of general formula (2) or a pharmaceutically acceptable salt or stereoisomer thereof; where R7 is chlorine; R6 is selected from chlorine and fluorine; R3, R4 and R5 are hydrogen; n is 0 or 1; Q1 is selected from C(=O) and SO2; A is absent or is NR2; R1 is selected from: – hydrogen; – C1-3 alkyl group optionally substituted with one or more substituents selected from hydroxy, amino and methylamino; and 5-6 membered heterocyclic rings selected from pyrrolidine and piperidine, wherein the heterocyclic rings are optionally substituted with a methyl group; R2, if present, is selected from hydrogen and methyl; or NR1R2 forms a 5-6 membered heterocyclic ring selected from pyrrolidine and morpholine, wherein the heterocyclic ring is optionally substituted with hydroxymethyl. Invention also relates to a pharmaceutical composition based on a compound of formula (2) and use thereof. ; .;EFFECT: obtaining novel compounds that modulate the activity of JAK and TYK2 kinases and are useful in the treatment of inflammatory or autoimmune diseases.;11 cl, 8 tbl, 35 ex
机译:技术领域本发明涉及有机化学,特别是涉及通式(2)的新型恶唑衍生物或其药学上可接受的盐或立体异构体。其中R 7 是氯; R 6 选自氯和氟; R 3 ,R 4 和R 5 是氢; n为0或1;从C(= O)和SO 2 中选择Q 1 ; A不存在或为NR 2 ; R 1 选自:–氢; –任选被一个或多个选自羟基,氨基和甲基氨基的取代基取代的C 1-3 烷基;选自吡咯烷和哌啶的5-6元杂环,其中杂环任选地被甲基取代;如果存在,则R 2 选自氢和甲基;或NR 1 R 2 形成选自吡咯烷和吗啉的5-6元杂环,其中杂环任选地被羟甲基取代。本发明还涉及基于式(2)的化合物的药物组合物及其用途。 ; 。;效果:获得可调节JAK和TYK2激酶活性的新型化合物,非常有用; 11 cl,8 tbl,35 ex

著录项

  • 公开/公告号RU2652795C2

    专利类型

  • 公开/公告日2018-05-03

    原文格式PDF

  • 申请/专利权人 SAREUM LIMITED;

    申请/专利号RU20160111522

  • 发明设计人 RIDER DZHON CHARLZ (GB);

    申请日2013-09-03

  • 分类号C07D263/48;C07D403/12;C07D413/12;A61K31/421;A61K31/422;A61K31/4523;A61P25;A61P29;A61P37;

  • 国家 RU

  • 入库时间 2022-08-21 12:35:39

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