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Use of Core 2 GlcNac-T inhibitors III for the treatment of inflammatory conditions

机译:核心2 GlcNac-T抑制剂III在治疗炎症中的用途

摘要

Treatments for conditions involving detrimental activity of the enzyme core 2 GlcNAc - T are provided using compounds of the formula I wherein R 1 is H, -OH, C 1-6 alkoxy, -NR 5 R 6 , or Sac 1; R 2 is H, -OH, C 1-6 alkoxy or Sac 2; R 3 is H, -OH, C 1-6 alkoxy or Sac 3; R 4 is H, C 1-6 alkyl, C 1-6 hydroxyalkyl or C 1-6 -alkoxy-C 1-6 -alkyl; R 5 is H, C 1-6 alkyl or C 1-6 acyl; R 6 is H, C 1-6 alkyl or C 1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof, wherein the condition to be treated is an inflammatory condition selected from ileitis, cholitis, cholecystitis, diverticulitis, gastritis, irritable bowel syndrome, inflammatory bowel disease, Lupus and ulcerative cholitis.
机译:使用式I化合物提供了涉及酶核心2 GlcNAc-T有害活性的疾病的治疗。其中R 1为H,-OH,C 1-6烷氧基,-NR 5 R 6或Sac 1;R 2为H,-OH,C 1-6烷氧基或Sac 2;R 3为H,-OH,C 1-6烷氧基或Sac 3;R 4为H,C 1-6烷基,C 1-6羟烷基或C 1-6-烷氧基-C 1-6-烷基;R 5是H,C 1-6烷基或C 1-6酰基;R 6为H,C 1-6烷基或C 1-6酰基;Sac 1 Sac 2和Sac 3是独立选择的糖部分;和Z是类固醇部分;或其药学上可接受的盐,醚或酯形式,其中要治疗的疾病是选自回肠炎,胆汁炎,胆囊炎,憩室炎,胃炎,肠易激综合症,炎症性肠病,狼疮和溃疡性胆管炎的炎性疾病。

著录项

  • 公开/公告号EP2382981B1

    专利类型

  • 公开/公告日2014-10-15

    原文格式PDF

  • 申请/专利权人 BTG INTERNATIONAL LIMITED;

    申请/专利号EP20110163564

  • 发明设计人 CHIBBER RAKESH;

    申请日2006-07-06

  • 分类号A61K31/704;A61K31/7048;A61K31/706;A61P1/04;A61P1/06;A61P1/16;A61P29;A61P37;

  • 国家 EP

  • 入库时间 2022-08-21 15:50:03

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