司替氨酯 | 94-35-9

• 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: 司替氨酯
• 英文名称: styramate
• 英文别名: Styramat；(2-hydroxy-2-phenylethyl) carbamate
• CAS: 94-35-9
• 化学式: C₉H₁₁NO₃
• mdl: MFCD00867701
• 分子量: 181.191
• InChiKey: OCSOHUROTFFTFO-UHFFFAOYSA-N

物化性质

• 熔点：
  111-112°
• 沸点：
  314.29°C (rough estimate)
• 密度：
  1.2375 (rough estimate)
• 保留指数：
  1667

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  72.6
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2924299090

反应信息

• 作为反应物：
  描述：

  司替氨酯 在 chromium(VI) oxide 作用下， 以 甲醇 、 溶剂黄146 为溶剂， 生成 N-Benzyl-carbamidsaeure-phenacylester
  参考文献：
  名称：

  Da Settimo,A. et al., Gazzetta Chimica Italiana, 1965, vol. 95, p. 624 - 635

  摘要：

  DOI：

文献信息

• [EN] TRIAZOLOBENZAZEPINES AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] TRIAZOLOBENZAZÉPINES UTILISÉES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116324A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及一般式(I)的5,6-二氢-4H-[1,2,4]三唑并[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其非对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶形式，这些化合物是中枢和/或外周作用的V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是制备这些化合物的过程以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的用途。
• Identification and Differentiation of Organic Medicinal Agents II
  作者：Lynn A. Doan、Leslie G. Ghatten

  DOI：10.1002/jps.2600541110

  日期：1965.11

  The reactions of some skeletal muscle relaxants (containing an alcohol or carbamate or both functional groups) with phenyl and 1-naphthyl isocyanate, 3,5-dinitrobenzoyl chloride, 3-nitrophthalic anhydride, 2,4-dinitrobenzenesulfenyl chloride, xanthydrol, benzhydrol, and acetic anhydride have been studied. By the use of the melting point data of these derivatives, supplemented with their infrared spectra

  某些骨骼肌松弛剂（包含醇或氨基甲酸酯或两个官能团）与苯基和异氰酸1-萘酯，3,5-二硝基苯甲酰氯，3-硝基邻苯二甲酸酐，2,4-二硝基苯硫基氯，黄嘌呤，苯甲酚和已经研究了乙酸酐。通过使用这些衍生物的熔点数据以及红外光谱的补充，可以区分美芬新，美索巴莫，DEP，硬脂酸酯，苯乙酰胺，丙氨甲酸酯和卡立普洛。
• [EN] TRICYCLIC COMPOUNDS AS VASOPRESSIN V1A RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS TRICYCLIQUES UTILISÉS EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE V1A
  申请人：RICHTER GEDEON NYRT

  公开号：WO2019116325A1

  公开（公告）日：2019-06-20

  The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

  本发明涉及通式（I）的5,6-二氢-4H-[1,2,4]三唑[4,3-a][1]苯并蒽啉衍生物和/或其盐和/或其几何异构体和/或其立体异构体和/或其对映异构体和/或其消旋体和/或其二对映异构体和/或其生物活性代谢物和/或其前药和/或其溶剂化合物和/或其水合物和/或其多晶型，这些化合物是中枢和/或外周作用V1a受体调节剂，特别是V1a受体拮抗剂。本发明的另一个主题是化合物的制备方法以及制备过程的中间体。该发明还涉及含有这些化合物或与一个或多个其他活性物质一起的药物组合物，以及在治疗和/或预防与V1a受体功能相关的疾病或症状中的使用。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Compositions and methods to effect the release profile in the transdermal administration of active agents
  申请人：——

  公开号：US20020004065A1

  公开（公告）日：2002-01-10

  Compositions and methods for the transdermal delivery of active agents up to a period of seven days or more at substantially a zero-order release rate comprising a pharmaceutically acceptable adhesive matrix and a polymeric plastic material that provides a release rate regulating effect on the active agents.

  本发明涉及一种用于经皮递送活性药剂的组合物和方法，该组合物和方法能够在持续时间为七天或更长时间内以几乎零阶释放速率递送活性药剂，包括一种药学上可接受的粘合基质和一种聚合物塑料材料，该聚合物塑料材料对活性药剂具有释放速率调节作用。

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