Benzeneacetic acid, alpha-(hydroxymethyl)-alpha-(2-((R)-methylsulfinyl)ethyl)-, (3R)-1-azabicyclo(2.2.2)oct-3-YL ester, hydrobromide, (alphaS)- | 262586-79-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 奎宁环
• 英文名称: Benzeneacetic acid, alpha-(hydroxymethyl)-alpha-(2-((R)-methylsulfinyl)ethyl)-, (3R)-1-azabicyclo(2.2.2)oct-3-YL ester, hydrobromide, (alphaS)-
• 英文别名: [(3R)-1-azabicyclo[2.2.2]octan-3-yl] (2S)-2-(hydroxymethyl)-4-[(R)-methylsulfinyl]-2-phenylbutanoate;hydrobromide
• CAS: 262586-79-8
• 化学式: C19H28BrNO4S
• 分子量: 446.4
• InChiKey: WUBKMAXEHQTPBW-XPTPVYCOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.63
• 拓扑面积：
  86
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• PREVENTIVE AND/OR REMEDY FOR HAND AND FOOT SYNDROME
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP2554184A1

  公开（公告）日：2013-02-06

  The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.

  可以提供由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂。由具有抗胆碱能活性的化合物组成的预防和/或治疗手足综合征的制剂可安全地用于手足综合征患者，并显示出对手足综合征具有卓越的预防和/或治疗效果。
• AMORPHOUS COMPOUND
  申请人：——

  公开号：US20030171301A1

  公开（公告）日：2003-09-11

  The present invention relates to a novel form of (S)-1-[N 2 -(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril for the treatment of hypertension and other cardiovascular diseases, pharmaceutical compositions containing it as well as processes for the preparation of the novel amorphous form of lisinopril.

  本发明涉及一种新形式的(S)-1-[N 2 -(1-羧基-3-苯基丙基]-L-赖氨酰]-L-脯氨酸的新形式，其通用名称为赖氨普利。此外，本发明还涉及新型无定形形式的赖辛普利在治疗高血压和其他心血管疾病中的用途、含赖辛普利的药物组合物以及新型无定形形式的赖辛普利的制备工艺。
• STABILIZED HME COMPOSITION WITH SMALL DRUG PARTICLES
  申请人：Board of Regents, The University of Texas System

  公开号：EP1817008B1

  公开（公告）日：2020-04-01
• Stabilized Hme Composition With Small Drug Particles
  申请人：Miller Dave A.

  公开号：US20080274194A1

  公开（公告）日：2008-11-06

  A hot-melt extruded composition having finely divided drug-containing particles dispersed within a polymeric and/or lipophyllic carrier matrix is provided. The carrier softens or melts during hot-melt extrusion but it does not dissolve the drug-containing particles during extrusion. As a result, a majority or at least 90% wt. of the drug-containing particles in the extrudate are deaggregated during extrusion into essentially primary crystalline and/or amorphous particles. PEO is a suitable carrier material for drugs insoluble in the solid state in this carrier. Various functional excipients can be included in the carrier system to stabilize the particle size and physical state of the drug substance in either a crystalline and/or amorphous state. The carrier system is comprised of at least one thermal binder, and may also contain various functional excipients, such as: super-disintegrants, antioxidants, surfactants, wetting agents, stabilizing agents, retardants, or similar functional excipients. A hydrophilic polymer, such as hydroxypropyl methylcellulose (HPMC E15), polyvinyl alcohol (PVA), or poloxamer, and/or a surfactant, such as sodium lauryl sulfate (SLS), can be included in the composition. A process for preparing the extrudate is conducted at a temperature approximating or above the softening or melting temperature of the matrix and below the point of solubilization of drug-containing particles in the carrier system, and below the recrystallization point in the case of amorphous fine drug particles.
• PREVENTIVE AND/OR THERAPEUTIC AGENT OF HAND-FOOT SYNDROME
  申请人：Ishizaka Kazuhiro

  公开号：US20130045956A1

  公开（公告）日：2013-02-21

  The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.