7-[(1S)-1-(4-chlorophenoxy)ethyl]-[1,2,4]triazolo[1,5-a]pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并嘧啶类
• 英文名称: 7-[(1S)-1-(4-chlorophenoxy)ethyl]-[1,2,4]triazolo[1,5-a]pyrimidine
• 化学式: C₁₃H₁₁ClN₄O
• 分子量: 274.7
• InChiKey: FCEPUTGEUCVRRI-VIFPVBQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  52.3
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• USE OF 1,2,4-TRIAZOLO[1,5-A]PYRIMIDINE DERIVATIVES FOR TREATING MIGRAINE
  申请人：Knoll GmbH

  公开号：EP1161244A2

  公开（公告）日：2001-12-12
• PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE DERIVATIVE AND CYCLODEXTRIN
  申请人：Knoll GmbH

  公开号：EP1161243A2

  公开（公告）日：2001-12-12
• NEW USE OF 1,2,4-TRIAZOLO[1,5-A]PYRIMIDINES
  申请人：KNOLL AKTIENGESELLSCHAFT

  公开号：EP1218008A2

  公开（公告）日：2002-07-03
• [EN] COMPOUNDS FOR USE IN THERAPY<br/>[FR] COMPOSES A USAGE THERAPEUTIQUE
  申请人：KNOLL AG

  公开号：WO2000056292A2

  公开（公告）日：2000-09-28

  A method of treating migraine comprising the administration of a therapeutically effective amount of a compound of formula (I) including pharmaceutically acceptable salts, solvates, racemates, enantiomers, diastereoisomers and mixtures thereof in which: R1 represents H or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C1-6alkyl, C1-6alkoxy or C1-6alkanoyl; R2 and R3 independently represent H or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C1-6alkyl, C1-6alkoxy, C1-6alkanoyl, C1-6alkylthio, C1-6alkylsulphinyl, C1-6alkylsulphonyl or hydroxy; R4 and R5 independently represent H, C1-6alkyl or R4 and R5 combined together with the carbon atom to which they are attached represent C3-6cycloalkylidene (each alkyl or cycloalkylidene being optionally substituted with one or more of halo, cyano, hydroxy, amino or C1-6alkyl); and R6, R7 and R8 independently represent H, halo, hydroxy, mercapto, nitro, cyano or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino; and any nitrogen atom being optionally substituted with one or more C1-6alkyl): C1-6alkyl, C1-6alkanoyl, C1-6alkoxy, C2-6alkoxycarbonyl, carboxy, C1-6alkanoyloxy, C1-6alkylthio, C1-6alkylsulphinyl, C1-6alkylsulphonyl, C1-6alkylsulphonylamino, sulphamoyl, carbamoyl, C2-6alkylcarbamoyl or C1-6alkanoylamino; to a mammal in need thereof.
• [EN] PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE DERIVATIVE AND CYCLODEXTRIN<br/>[FR] COMPOSITIONS PHARMACEUTIQUES CONTENANT UN DERIVE DE PYRIMIDINE ET DE LA CYCLODEXTRINE
  申请人：KNOLL AG

  公开号：WO2000056336A2

  公开（公告）日：2000-09-28

  A pharmaceutical composition comprising a) a 1,2,4-triazolo(1,5-a)pyrimidine derivative of formula (I) including pharmaceutically acceptable salts, racemates, enantiomers, diastereoisomers and mixtures thereof, b) a cyclodextrin. These compositions are useful in the treatment of migraine, seizures and/or neurological disorders such as epilepsy and/or as neuroprotective agents to protect against conditions such as stroke, brain trauma, head injuries and haemorrhage in animals including human beings.