ethyl [(Z)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-ethoxycarbonyloxypent-2-en-3-yl]sulfanylformate;hydron;chloride

• 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: ethyl [(Z)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-ethoxycarbonyloxypent-2-en-3-yl]sulfanylformate;hydron;chloride
• 化学式: C18H27ClN4O6S
• 分子量: 462.9
• InChiKey: LIOJHMDIELWKFZ-OBBOLZQKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.43
• 重原子数：
  30
• 可旋转键数：
  13
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  159
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• CRYSTALLINE CONDITION DISLOCATING METHOD
  申请人：NIPPON SHINYAKU COMPANY, LIMITED

  公开号：EP0665009A1

  公开（公告）日：1995-08-02

  An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition (△ is dislocated to another crystalline condition (○), i.e., when the dislocation of crystalline condition (△->○) is carried out.

  本发明的目的是提供一种简单、快速和均匀地将结晶药物的结晶状态变位的方法，而且是一次性大量变位。本发明针对的是一种使用挤压机将某种结晶状态（△）的结晶药物变位到另一种结晶状态（○）的方法，即结晶状态（△->○）变位的方法。
• SACCHARIDE-CONTAINING COMPOSITIONS
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP1008353A1

  公开（公告）日：2000-06-14

  Spray-dried powders containing calcium hydrogen phosphate and saccharides having excellent powder-fluidity and compression-moldability, being quickly disintegrated/dissolved when put into the oral cavity or water in the form of granules, tablets, etc., being useful as fillers, compression-moldability improvers, disintegration aids, administration-facilitating agents, solubilizers in the oral cavity, etc. and being applicable to drugs, foods, etc.

  含有磷酸氢钙和糖类的喷雾干燥粉末，具有极佳的粉末流动性和压模性，以颗粒、片剂等形式放入口腔或水中时可迅速崩解/溶解，可用作填充剂、压模性改进剂、崩解辅助剂、给药促进剂、口腔增溶剂等，适用于药物、食品等。
• PROCESS FOR PRODUCING HARD CAPSULE
  申请人：Shionogi Qualicaps Co., Ltd.

  公开号：EP1044682A1

  公开（公告）日：2000-10-18

  A method of manufacturing hard capsules is characterized by comprising the steps of dispersing a water-soluble cellulose derivative in hot water and cooling the dispersion to effect dissolution of the water-soluble cellulose derivative in the water, adding and dissolving a gelling agent in the water-soluble cellulose derivative solution to give a capsule-preparing solution, dipping a capsule-forming pin into the capsule-preparing solution at a predetermined temperature, then drawing out the pin and inducing gelation of the capsule-preparing solution adhering to the pin.

  一种制造硬胶囊的方法，其特征在于包括以下步骤：将水溶性纤维素衍生物分散在热水中，然后冷却分散液，使水溶性纤维素衍生物溶解在水中、在水溶性纤维素衍生物溶液中加入并溶解胶凝剂，得到胶囊制备溶液，在预定温度下将胶囊成型针浸入胶囊制备溶液中，然后拔出针，使粘附在针上的胶囊制备溶液凝胶化。
• Composition for rapid disintegrating tablet in oral cavity
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP1523974A1

  公开（公告）日：2005-04-20

  The present invention provides rapid disintegrating tablets in oral cavity having a shortened disintegration time in oral cavity as well as a sufficient hardness with compared to rapid disintegrating tablets of the prior art. The above objective is solved by a composition for rapid disintegrating tablets in oral cavity, wherein components (a) to (c) are contained in such manner that (a) saccharides consisting of a combination of mannitol and xylitol is 40 to 90 parts by weight; (b) the inorganic excipient is 1 to 30 parts by weight; and (c) the disintegrating agent is 5 to 40 parts by weight, provided that the total amount of (a), (b) and (c) is 100 parts by weight.

  本发明提供的口腔快速崩解片与现有技术的口腔快速崩解片相比，具有更短的口腔崩解时间和足够的硬度。 本发明通过一种口腔快速崩解片剂组合物来实现上述目标，其中组分（a）至（c）的含有方式为 (a) 糖类由甘露糖醇和木糖醇组合而成，按重量计占 40 至 90%； (b) 无机赋形剂按重量计为 1 至 30 份；以及 (c) 以重量計，崩解劑為 5 至 40 份、 条件是(a)、(b)和(c)的总用量以重量计为 100 份。
• TABLET QUICKLY DISINTEGRATING IN ORAL CAVITY
  申请人：FUJI CHEMICAL INDUSTRY CO., LTD.

  公开号：EP1674083A1

  公开（公告）日：2006-06-28

  The present invention provides rapid disintegrating tablets in oral cavity having a shortened disintegration time in oral cavity as well as a sufficient hardness compared to rapid disintegrating tablets of the prior art. The above objective is solved by a composition in which the inorganic excipient and the disintegrating agent are dispersed in the complex particles consisting of mannitol and other saccharide(s) in a specific ratio, and rapid disintegrating tablets in oral cavity obtained by direct compression of the composition.

  本发明提供的口腔快速崩解片与现有技术的口腔快速崩解片相比，具有更短的口腔崩解时间和足够的硬度。 解决上述问题的方法是将无机辅料和崩解剂按特定比例分散在由甘露醇和其他糖类组成的复合颗粒中，通过直接压缩该组合物获得口腔快速崩解片。