6-[4-(2,4-difluoro-phenyl)-oxazol-5-yl]-3-(1-methyl-cyclopropyl)-[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: 6-[4-(2,4-difluoro-phenyl)-oxazol-5-yl]-3-(1-methyl-cyclopropyl)-[1,2,4]triazolo(4,3-a)pyridine
• 英文别名: Triazolopyridine oxazole inhibitor 61；4-(2,4-difluorophenyl)-5-[3-(1-methylcyclopropyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]-1,3-oxazole
• 化学式: C₁₉H₁₄F₂N₄O
• 分子量: 352.343
• InChiKey: ZBSUTYBJWPJEPR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  56.2
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS<br/>[FR] COMPOSES ANTI-INFLAMMATOIRES A BASE DE DI- ET TRIFLUORO-TRIAZOLO-PYRIDINES
  申请人：PFIZER PROD INC

  公开号：WO2004020440A1

  公开（公告）日：2004-03-11

  The present invention relates to novel triazolo-pyridines of the formula (I) wherein R1 is fluoro; s is an integer from two to three; R2 is (C3-C6)cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (Cl-C4)alkyl, hydroxy, (Cl-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; or R2 is (Cl-C6)alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C1-C6)alkyl, hydroxy, (C1-C6)alkoxy and (C1-C6)alkyl-(C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; 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.

  本发明涉及式(I)的新型三唑吡啶，其中R1为氟；s为2至3的整数；R2为（C3-C6）环烷基，可选地取代为从卤素，（Cl-C4）烷基，羟基，（Cl-C6）烷氧基和（C1-C6）烷基-（C=O）-0-中独立选择的一种或两种基团；或R2为（Cl-C6）烷基，可选地取代为从卤素，（C1-C6）烷基，羟基，（C1-C6）烷氧基和（C1-C6）烷基-（C=O）-0-中独立选择的一种或两种基团；但是，具有式(I)的化合物不能为6-[4-(2,4-二氟苯基)-噁唑-5-基]-3-异丙基-[1,2,4]三唑并[4,3-a]吡啶；或6-[4-(3,4-二氟苯基)-噁唑-5-基]-3-异丙基-[1,2,4]三唑并[4,3-a]吡啶；本发明还涉及其制备中间体、含有它们的制药组合物以及它们的医药用途。本发明的化合物是MAP激酶，特别是p38激酶的有效抑制剂。它们在炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病的再灌注或缺血，自身免疫性疾病和其他疾病的治疗中有用。
• Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
  申请人：Pfizer Inc

  公开号：US20040087615A1

  公开（公告）日：2004-05-06

  The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]triazolo-pyridines, 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, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

  本发明涉及新型环烷基-[4-(二氟苯基)-噁唑-5-基]三唑吡啶、其制备中间体、含有它们的药物组合物以及它们的药用。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、中风或心脏病发作的再灌注或缺血、自身免疫疾病和其他疾病方面有用。
• Di and trifluoro-triazolo-pyridines anti-inflammatory compounds
  申请人：Pfizer Inc.

  公开号：US20040053958A1

  公开（公告）日：2004-03-18

  The present invention relates to novel triazolo-pyridines of the formula I 1 wherein R 1 is fluoro; s is an integer from two to three; R 2 is (C 3 -C 6 )cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C 1 -C 4 )alkyl, hydroxy, (C 1 -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C═O)—O—; or R 2 is (C 1 -C 6 )alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, hydroxy, (C 1 -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C═O)—O—; with the proviso that said compound of formula I cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; 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.

  本发明涉及式I1的新型三唑啉-吡啶化合物，其中R1为氟；s为2至3的整数；R2为（C3-C6）环烷基，可选地被一或两个基团独立地选自卤素、（C1-C4）烷基、羟基、（C1-C6）烷氧基和（C1-C6）烷基-(C═O)-O-；或者R2为（C1-C6）烷基，可选地被一或两个基团独立地选自卤素、（C1-C6）烷基、羟基、（C1-C6）烷氧基和（C1-C6）烷基-(C═O)-O-；但式I化合物不能是6-[4-(2,4-二氟苯基)-噁唑-5-基]-3-异丙基-[1,2,4]三唑啉[4,3-a]吡啶；或6-[4-(3,4-二氟苯基)-噁唑-5-基]-3-异丙基-[1,2,4]三唑啉[4,3-a]吡啶；本发明化合物是MAP激酶的有效抑制剂，优选为p38激酶。它们可用于治疗炎症、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。本发明还涉及其制备的中间体、含有它们的制药组合物和它们的药用用途。
• EP1537108B1
  申请人：——

  公开号：EP1537108B1

  公开（公告）日：2008-11-19
• DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS
  申请人：Pfizer Products Inc.

  公开号：EP1537108A1

  公开（公告）日：2005-06-08