Invention Grant
US07659294B2 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists 失效
作为S1P受体激动剂的2-(芳基)氮杂环甲基甲基羧酸盐,磺酸盐,膦酸盐,次膦酸盐和杂环

  • Patent Title: 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists
  • Patent Title (中): 作为S1P受体激动剂的2-(芳基)氮杂环甲基甲基羧酸盐,磺酸盐,膦酸盐,次膦酸盐和杂环
  • Application No.: US11665046
    Application Date: 2005-10-18
  • Publication No.: US07659294B2
    Publication Date: 2010-02-09
  • Inventor: Jeffrey John HaleLin Yan
  • Applicant: Jeffrey John HaleLin Yan
  • Applicant Address: US NJ Rahway
  • Assignee: Merck & Co., Inc.
  • Current Assignee: Merck & Co., Inc.
  • Current Assignee Address: US NJ Rahway
  • Agent Yong Zhao; Valerie J. Camara
  • International Application: PCT/US2005/037652 WO 20051018
  • International Announcement: WO2006/047195 WO 20060504
  • Main IPC: A61K31/4245
  • IPC: A61K31/4245 C07D271/10 C07D413/10
2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists
Abstract:
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
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