盐酸利马扎封 | 85815-37-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 盐酸利马扎封
• 英文名称: 2',5-dichloro-2-(3-dimethylcarbamoyl-5-glycylaminomethyl-1H-1,2,4-triazol-1-yl)benzophenone hydrochloride
• 英文别名: rilmazafone hydrochloride；5-[[(2-aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide;hydrochloride
• CAS: 85815-37-8
• 化学式: C₂₁H₂₀Cl₂N₆O₃*ClH
• 分子量: 511.795
• InChiKey: KHINGHZNENOVFD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  123
• 氢给体数：
  3
• 氢受体数：
  6

安全信息

• 储存条件：
  -20°C，密闭保存，置于干燥处

制备方法与用途

450191S是一种新型的睡眠诱导剂。

反应信息

• 作为产物：
  描述：

  2',5-dichloro-2-(3-dimethylcarbamoyl-5-phthalylglycylaminomethyl-1H-1,2,4-triazol-1-yl)benzophenone 、 肼 以83%的产率得到
  参考文献：
  名称：

  HIRAI, KENTARO;SUGIMOTO, HIROHIKO;ISBIBA, TERUYUKI;FUJISHITA, TOSHIO;TSUK+, J. HETEROCYCL. CHEM., 1982, 19, N 6, 1363-1369

  摘要：

  DOI：

文献信息

• NOVEL PYRAZOLE DERIVATIVE
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：US20140378447A1

  公开（公告）日：2014-12-25

  It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.

  已经有人希望开发一种药物组合物，用于预防和/或治疗与PDE10相关的各种疾病（例如精神障碍和神经退行性疾病）。本发明提供：具有PDE10抑制作用的化合物，特别是具有以下式（I）所代表的4-杂环芳基吡唑-5-羧酰胺结构的化合物，或其药学上可接受的盐，或其溶剂化物；包含作为活性成分的化合物，或其药学上可接受的盐，或其溶剂化物的药物组合物；以及化合物的医学用途，或其药学上可接受的盐，或其溶剂化物。
• 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。
• 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。
• ADHESIVE PREPARATIONS
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP1074251A1

  公开（公告）日：2001-02-07

  Adhesive preparations with improved percutaneous absorption of physiologically active substances, in particular, matrix adhesive preparations containing a base drug salt and an organic acid salt having an mean diameter of from 0.1 to 100 µm are provided.

  提供了可改善生理活性物质经皮吸收的粘合剂制剂，特别是含有平均直径为 0.1 至 100 微米的碱基药物盐和有机酸盐的基质粘合剂制剂。
• PATCHES FOR EXTERNAL USE
  申请人：HISAMITSU PHARMACEUTICAL CO. INC.

  公开号：EP1201232A1

  公开（公告）日：2002-05-02

  A patch formulation for external use where a basic drug, an organic acid and an organic acid salt are combined as essential components is disclosed. The basic drug is preferably in the form of its acid addition salt. The organic acid is preferably a carboxylic acid having carbon atoms of 2 to 7, and more preferably at least one acid selected from the group consisting of acetic, lactic, tartaric, citric, malic, benzoic and salicylic acids. The organic acid salt is preferably a metal salt of a carboxylic acid, and more preferably sodium acetate.

  本发明公开了一种外用贴剂配方，其中的基本成分是一种碱性药物、一种有机酸和一种有机酸盐。碱性药物最好以其酸加成盐的形式存在。有机酸最好是碳原子数为 2-7 的羧酸，更优选至少一种选自乙酸、乳酸、酒石酸、柠檬酸、苹果酸、苯甲酸和水杨酸的酸。有机酸盐最好是羧酸的金属盐，更优选醋酸钠。