YM 60828 dihydrochloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: YM 60828 dihydrochloride
• 英文别名: 2-[(7-carbamimidoylnaphthalen-2-yl)methyl-[4-(1-ethanimidoylpiperidin-4-yl)oxyphenyl]sulfamoyl]acetic acid;dihydrochloride
• 化学式: C27H33Cl2N5O5S
• 分子量: 610.6
• InChiKey: GKELESGQQAPAAO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.23
• 重原子数：
  40
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  169
• 氢给体数：
  6
• 氢受体数：
  8

文献信息

• MEDICINAL COMPOSITION FOR PERCUTANEOUS ADMINISTRATION
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1043020A1

  公开（公告）日：2000-10-11

  A percutaneously absorbable medicinal composition comprising a percutaneous absorption enhancer and at least one member selected from the group consisting of aromatic amidine derivatives represented by formula (1): salts of the derivatives, solvates of the derivatives, and solvates of salts of the derivatives. The present invention provides a composition which exhibits high percutaneous absorbability, which can maintain an effective blood level for prolonged periods of time, which provides antithrombotic and anticoagulant effects.

  一种经皮吸收的药物组合物，包括经皮吸收增强剂以及选择自式（1）所表示的芳香族酰胺衍生物的至少一种成员：衍生物的盐，衍生物的溶剂，以及衍生物的盐的溶剂。本发明提供了一种组合物，具有高经皮吸收性，可以维持有效的血液水平长时间，具有抗血栓和抗凝血作用。
• NOVEL AMIDINONAPHTHYL DERIVATIVE OR SALT THEREOF
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0798295A1

  公开（公告）日：1997-10-01

  An amidinonaphthyl derivative represented by the following general formula (I) which has a platelet aggregation inhibiting action based on the activated blood coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. (symbols in the formula have the following meanings; R1: a hydrogen atom or a group represented by the formula -A-W-R4, A: a group represented by the formula a group represented by the formula or a group represented by the formula -SO2-, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula -NR5-, R4: a hydroxyl group, a lower alkoxy group, etc., not a hydroxyl group or a lower alkoxy group, R5: a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R2: a lower alkyl group, R3: a hydrogen atom, a halogen atom, a carboxyl group, B: a lower alkylene group or a carbonyl group, and n: 0 or 1).

  一种由下式通式（I）表示的脒基萘衍生物、其盐、中间体和包含该脒基萘衍生物的药物组合物，该脒基萘衍生物具有基于活化血液凝固因子 X 抑制作用的血小板聚集抑制作用，可用作抗血栓剂等。 由以下通式（I）代表的脒基萘衍生物或其药学上可接受的盐。 (式中符号含义如下； R1：氢原子或由式-A-W-R4 所代表的基团、 A：由式 式所代表的基团 或由式 -SO2- 代表的基团、 X：氧原子或硫原子，W：单键或由式-NR5-代表的基团，R4：羟基、低级烷氧基等，不是羟基或低级烷氧基，R5：氢原子、氨基甲酰基、低级烷氧基羰基等，R2：低级烷基，R3：氢原子、卤素原子、羧基，B：低级亚烷基或羰基，n：0 或 1）。
• PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP0953359A1

  公开（公告）日：1999-11-03

  The present invention is directed to a pharmaceutical composition for oral administration, comprising a basic drug, a lipophilic substance, and/or a cyclodextrin. The composition exhibits improved peroral absorption of a basic drug which is difficult to be absorbed by oral administration.

  本发明涉及一种口服药物组合物，其中包括一种碱性药物、一种亲脂性物质和/或一种环糊精。 该组合物改善了难以通过口服吸收的碱性药物的口腔吸收。
• LYOPHILIZATION PRODUCT
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1504755A1

  公开（公告）日：2005-02-09

  The present invention relates to an aqueous solution containing a physiologically active substance which may have a substituent and which has an amidino group, wherein the pH of the solution is higher than 2 and equal to or lower than 4. The invention also relates to a lyophilized product obtained by drying the solution, to an injection containing the aqueous solution or the lyophilized product, and to an injection kit.

  本发明涉及一种含有生理活性物质的水溶液，该生理活性物质可能具有一个取代基和一个脒基，其中溶液的pH值高于2，等于或低于4。本发明还涉及一种通过干燥该溶液而获得的冻干产品，一种含有该水溶液或冻干产品的注射剂，以及一种注射试剂盒。
• Lypohilization product
  申请人：Fuji Yoshimine

  公开号：US20050187249A1

  公开（公告）日：2005-08-25

  The present invention relates to an aqueous solution containing a physiologically active substance which may have a substituent and which has an amidino group, wherein the pH of the solution is higher than 2 and equal to or lower than 4. The invention also relates to a lyophilized product obtained by drying the solution, to an injection containing the aqueous solution or the lyophilized product, and to an injection kit.

  本发明涉及一种含有生理活性物质的水溶液，该生理活性物质可能具有一个取代基和一个脒基，其中溶液的pH值高于2，等于或低于4。本发明还涉及一种通过干燥该溶液而获得的冻干产品，一种含有该水溶液或冻干产品的注射剂，以及一种注射试剂盒。