4-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyrazolo[1,5-a]pyridin-3-yl]-benzenesulfonamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyrazolo[1,5-a]pyridin-3-yl]-benzenesulfonamide
• 英文别名: 4-[2-(4-Fluoro-phenyl)-6-trifluoromethyl-pyrazolo[1,5-a]pyridin-3-yl]benzenesulphonamide；4-[2-(4-fluorophenyl)-6-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]benzenesulfonamide
• 化学式: C₂₀H₁₃F₄N₃O₂S
• 分子量: 435.402
• InChiKey: WYRNBKPPAUKLBU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  85.8
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  4-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyrazolo[1,5-a]pyridin-3-yl]-benzenesulfonamide 、 乙酸酐 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 氯仿 为溶剂， 反应 4.0h， 以31%的产率得到N-acetyl-4-[2-(4-fluorophenyl)-6-(trifluoromethyt)pyrazolo[1,5-a]pyridin-3-yl]benzenesulfonamide
  参考文献：
  名称：

  PYRAZOLOPYRIDINE DERIVATIVES AS SELECTIVE COX-2 INHIBITORS

  摘要：

  公开号：

  EP1127058B1

文献信息

• Amide-type triazole compounds
  申请人：SANKYO COMPANY, LIMITED

  公开号：US20030176480A1

  公开（公告）日：2003-09-18

  A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: 1 wherein Ar 1 represents a phenyl group or the like; Ar 2 represents a phenylene group or the like. X represents a sulfur atom or a methylene group. R 1 represents a hydrogen atom or a C 1-3 alkyl group; R 2 represents a hydrogen atom or a C 1-3 alkyl group; and R 3 represents an optionally substituted C 6-10 aryl group or the like. Fungal infections may be prevented and/or treated by administering said compound (I) or said prodrug or salt thereof.

  一种具有出色抗真菌活性的化合物，其化学式为（I）或其药理学上可接受的前药或盐：其中Ar1代表苯基或类似物；Ar2代表苯基或类似物。X代表硫原子或亚甲基基团。R1代表氢原子或C1-3烷基基团；R2代表氢原子或C1-3烷基基团；R3代表可选择取代的C6-10芳基基团或类似物。通过给予该化合物（I）或其前药或盐可预防和/或治疗真菌感染。
• Pyrazolopyridine derivatives as selective cox-2 inhibitors
  申请人：SmithKline Beecham Corporation

  公开号：US07223772B1

  公开（公告）日：2007-05-29

  The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R0 and R1 are independently selected from the group consisting of H, halogen, C1-6alkyl, C1-6alkoxy, and C1-6alkoxy substituted by one or more fluorine atoms; R2 is selected from the group consisting of H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, and C1-6alkoxy substituted by one or more fluorine atoms; and R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

  本发明提供了公式（I）的化合物及其药学上可接受的衍生物，其中：R0和R1独立地选自H，卤素，C1-6烷基，C1-6烷氧基和一个或多个氟原子取代的C1-6烷氧基；R2选自H，C1-6烷基，一个或多个氟原子取代的C1-6烷基，C1-6烷氧基，C1-6羟基烷基，SC1-6烷基，C（O）H，C（O）C1-6烷基，C1-6烷基磺酰基和一个或多个氟原子取代的C1-6烷氧基；R3为C1-6烷基或NH2。公式（I）的化合物是COX-2的有效和选择性抑制剂，并可用于治疗各种疾病的疼痛，发热和炎症。
• TRIAZOLE COMPOUNDS HAVING AMIDE LINKAGE
  申请人：Sankyo Company, Limited

  公开号：EP1284267A1

  公开（公告）日：2003-02-19

  The present invention provides a compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: [wherein Ar1 represents a phenyl group or the like; Ar2 represents a phenylene group or the like; X represents a sulfur atom or a methylene group; R1 represents a hydrogen atom or a C1-3 alkyl group; R2 represents a hydrogen atom or a C1-3 alkyl group; and R3 represents an optionally substituted C6-10 aryl group or the like].

  本发明提供了一种具有优异抗真菌活性的式(I)化合物或其药理学上可接受的原药或盐： [其中 Ar1 代表苯基或类似物；Ar2 代表亚苯基或类似物；X 代表硫原子或亚甲基；R1 代表氢原子或 C1-3 烷基；R2 代表氢原子或 C1-3 烷基；R3 代表任选取代的 C6-10 芳基或类似物]。
• US6653330B2
  申请人：——

  公开号：US6653330B2

  公开（公告）日：2003-11-25
• US7223772B1
  申请人：——

  公开号：US7223772B1

  公开（公告）日：2007-05-29