3-Cyclopropyl-6-[4-(4-fluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo[4,3-a]pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-Cyclopropyl-6-[4-(4-fluoro-phenyl)-oxazol-5-yl]-[1,2,4]triazolo[4,3-a]pyridine
• 英文别名: Triazolopyridine oxazole inhibitor 46；5-(3-cyclopropyl-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-4-(4-fluorophenyl)-1,3-oxazole
• 化学式: C₁₈H₁₃FN₄O
• 分子量: 320.326
• InChiKey: HTRYISKMFSYGKQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  56.2
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Novel triazolo-pyridines anti-inflammatory compounds
  申请人：Pfizer Inc.

  公开号：US20030096838A1

  公开（公告）日：2003-05-22

  The present invention relates to novel triazolo-pyridines of the formula I 1 wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R 2 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; R 3 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

  本发明涉及公式I1的新型三唑并[3,4-d]吡啶化合物，其中Het是一个含有1-2个异原子（氮、硫和氧）的可选取代的5-元杂环，其中至少一个异原子必须是氮；R2选自氢，（C1-C6）烷基或其他适当的取代基；R3选自氢，（C1-C6）烷基或其他适当的取代基；s是0-5的整数；本发明还涉及其制备中间体、含有它们的制药组合物及其医药用途。本发明的化合物是MAP激酶，特别是p38激酶的有效抑制剂。它们在治疗炎症、骨关节炎、类风湿性关节炎、癌症、脑卒中或心脏病的再灌注或缺血、自身免疫性疾病和其他疾病中有用。
• TRIAZOLOPYRIDINES AS ANTI-INFLAMMATORY AGENTS
  申请人：Pfizer Products Inc.

  公开号：EP1370559A1

  公开（公告）日：2003-12-17
• US6696464B2
  申请人：——

  公开号：US6696464B2

  公开（公告）日：2004-02-24
• [EN] TRIAZOLOPYRIDINES AS ANTI-INFLAMMATORY AGENTS<br/>[FR] TRIAZOLOPYRIDINES, AGENTS ANTI-INFLAMMATOIRES
  申请人：PFIZER PROD INC

  公开号：WO2002072579A1

  公开（公告）日：2002-09-19

  The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C¿1?-C6) alkyl or other suitable substituents; R?3¿ is selected from the group consisting of hydrogen, (C¿1?-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.