6-[(2-aminopyrrolidin-1-yl)methyl]-5-chloro-1H-pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-[(2-aminopyrrolidin-1-yl)methyl]-5-chloro-1H-pyrimidine-2,4-dione
• 化学式: C₉H₁₃ClN₄O₂
• 分子量: 244.68
• InChiKey: ZHQANGNACINMKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  87.5
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE
  申请人：Taiho Pharmaceutical Co., Ltd.

  公开号：EP2005962B1

  公开（公告）日：2012-04-25
• POTENTIATOR OF RADIATION THERAPY
  申请人：FUKUSHIMA Masakazu

  公开号：US20120010165A1

  公开（公告）日：2012-01-12

  To provide a radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects. The invention provides a radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented by formula (1) (wherein R 1 represents a halogen atom or a cyano group; and R 2 represents a 4- to 8-membered heterocyclic group having 1 to 3 nitrogen atoms and optionally having as a substituent a lower alkyl group, an imino group, a hydroxyl group, a hydroxymethyl group, a methanesulfonyloxy group, or an amino group; an amidinothio group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group; a guanidino group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group or a cyano group; a lower alkylamidino group; or a 1-pyrrolidinylmethyl group) or a pharmaceutically acceptable salt thereof.
• US8440675B2
  申请人：——

  公开号：US8440675B2

  公开（公告）日：2013-05-14
• [EN] THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE<br/>[FR] AGENT THÉRAPEUTIQUE POUR AFFECTION ABDOMINALE INFLAMMATOIRE
  申请人：TAIHO PHARMACEUTICAL CO LTD

  公开号：WO2007122812A1

  公开（公告）日：2007-11-01

  [EN] Disclosed is a therapeutic agent for inflammatory bowel disease comprising 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl- 2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof as an active ingredient. An effective and safe therapeutic agent for inflammatory bowel disease including ulcerative colitis and Crohn's disease can be provided. The balance between the therapeutic effect on a chronic inflammation such as inflammatory bowel disease and the adverse side effect of the compound is superior to those of an aminosalicylic acid preparation and a corticosteroid preparation. The compound shows an unexpected effect beyond a mere antidiarrheal effect.
  [FR] La présente invention divulgue un agent thérapeutique pour affection abdominale inflammatoire comprenant 5-chloro-6-(2-aminopyrrolidine-1-yl)méthyle- 2,4(1H,3H)-pyrimidinedione ou un sel pharmaceutiquement acceptable de celui-ci en tant que principe actif. Un agent thérapeutique efficace et inoffensif pour les affections abdominales inflammatoires comprenant la rectocolite hémorragique et la maladie de Crohn peut être proposé. L'équilibre entre l'effet thérapeutique sur une inflammation chronique telle qu'une affection abdominale inflammatoire et l'effet indésirable du composé est supérieur à ceux d'une préparation d'acide para-aminosalicylique et d'une préparation de corticostéroïde. Le composé présente un effet inattendu au-delà d'un simple effet antidiarrhéique.