美托咪酯 | 5377-20-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 美托咪酯
• 中文别名: 苄咪唑甲酯
• 英文名称: etomidate
• 英文别名: DL-1-<1-Phenyl-aethyl>-imidazol-5-carbonsaeure-methylester；Metomidate；Hypnodil；3-(1-phenyl-ethyl)-3H-imidazole-4-carboxylic acid methyl ester；(+/-)-methyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate；methyl 3-(1-phenylethyl)imidazole-4-carboxylate
• CAS: 5377-20-8
• 化学式: C₁₃H₁₄N₂O₂
• 分子量: 230.266
• InChiKey: FHFZEKYDSVTYLL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  44.1
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  美托咪酯 在 cellulose tris(3,5-dichlorophenylcarbamate) 作用下， 生成 依托咪酯EP杂质B 、 (S)-Metomidate
  参考文献：
  名称：

  HPLC Enantioseparation with Cellulose Tris(3,5-dichlorophenylcarbamate) in Aqueous Methanol as a Mobile Phase

  摘要：

  适当的移动相和固定相组合设计允许将纤维素三（3,5-二氯苯基氨基甲酸酯）(CDCPC)作为高效液相色谱（HPLC）中的手性固定相（CSP）使用。结合在正己烷/异丙醇作为移动相中获得的先前数据，本研究表明CDCPC具有非常高的手性分离能力。

  DOI：

  10.1246/cl.2000.352

文献信息

• D-AMINO ACID OXIDASE INHIBITORS AND THERAPEUTIC USES THEREOF
  申请人：Tsai Guochuan Emil

  公开号：US20190112289A1

  公开（公告）日：2019-04-18

  The present invention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: each of A, B, C, D, and E, independently, is C, N, N—H, O, S, or absent is a single bond or a double bond; each of X, Y, and Z, independently, is aryl, heteroaryl, aralkyl, H, or absent; each of L 1 and L 2 , independently, is a moiety selected from O, CH 2 , C═O, C 2-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, —((CH 2 ) n —W)—, wherein n=0, 1, 2, 3, 4, or 5, and W is O or S, or absent; and when L 2 is absent, Z is aryl or heteroaryl fused with B C. Also provided in the present invention is a method for inhibiting, treating and/or reducing the risk of a neuropsychiatric disorder, comprising administering a subject in need a composition comprising a compound of Formula (I).

  本发明涉及以下式（I）的化合物： 或其药学上可接受的盐，其中：A、B、C、D 和 E 中的每一个独立地是 C、N、N—H、O、S 或不存在 是单键或双键；X、Y 和 Z 中的每一个独立地是芳基、杂环芳基、芳基烷基、H 或不存在；L 1 和 L 2 中的每一个独立地是从 O、CH 2 、C═O、C 2-10 烷基、C 2-10 烯基、C 2-10 炔基、—((CH 2 ) n —W)— 中选择的基团，其中 n=0、1、2、3、4 或 5，W 是 O 或 S，或不存在；当 L 2 不存在时，Z 是与 B 相融合的芳基或杂环芳基。本发明还提供了一种用于抑制、治疗和/或减少神经精神障碍风险的方法，包括向需要的受试者施用包含式（I）化合物的组合物。
• SUBSTITUTED IMIDAZOLECARBOXYLATE DERIVATIVES AND THE USE THEREOF
  申请人：CHENGDU MFS PHARMA. CO., LTD.

  公开号：US20200369621A1

  公开（公告）日：2020-11-26

  A compound is shown in formula (I). The derivatives of the compound include a stereoisomer, a pharmaceutically acceptable salt, a solvate, a prodrug, a metabolite, a deuterated derivative. The compound is a structurally novel substituted imidazole formate derivative. Substituted imidazole formate derivatives are used in preparing a drug with sedative, hypnotic and/or anesthetic effects, as well as a drug that can control the state of epilepsy. The compound has a good inhibitory effect on the central nervous system, and provides a new option for clinical screening of and/or preparation of a drug with sedative, hypnotic and/or anesthetic effects and controlling the state of epilepsy.

  化合物在式（I）中显示。该化合物的衍生物包括立体异构体、药用可接受的盐、溶剂合物、前药、代谢物、氘代衍生物。该化合物是一种结构新颖的取代咪唑甲酸酯衍生物。取代咪唑甲酸酯衍生物用于制备具有镇静、催眠和/或麻醉作用的药物，以及可以控制癫痫状态的药物。该化合物对中枢神经系统具有良好的抑制作用，并为临床筛选和/或制备具有镇静、催眠和/或麻醉作用以及控制癫痫状态的药物提供了新选择。
• Composition for the treatment of damaged tissue
  申请人：Pfizer Inc.

  公开号：US20030199440A1

  公开（公告）日：2003-10-23

  A pharmaceutical for use in damaged tissue, such as wound, treatment (e.g. healing) is described. The pharmaceutical comprising a composition which comprises: (a) a growth factor; and (b) an inhibitor agent; and optionally (c) a pharmaceutically acceptable carrier, diluent or excipient; wherein the inhibitor agent can inhibit the action of at least one specific adverse protein (e.g. a specific protease) that is upregulated in a damaged tissue, such as a wound, environment.

  描述了一种用于受损组织，如伤口治疗（例如愈合）的药物。该药物包括包含以下成分的组合物：（a）生长因子；和（b）抑制剂；以及可选的（c）药用载体、稀释剂或赋形剂；其中抑制剂可以抑制至少一种在受损组织，如伤口环境中上调的特定不良蛋白质（例如特定蛋白酶）的作用。
• Radiolabelled phenylethyl imidazole caboxylic acid ester derivatives
  申请人：Zolle Ilse

  公开号：US20050033060A1

  公开（公告）日：2005-02-10

  Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

  苯乙基咪唑的卤代羧酸酯衍生物及其制备方法已被披露。这些化合物的放射性卤代形式非常适合于肾上腺的正电子成像，因为已知这些化合物在肾上腺中表现出选择性和高速的积累率。制备这些衍生物的方法通过将具有三烷基锡离去基团的稳定的非放射性中间体转化而来。这些中间体通过用卤素或放射性卤素替换三烷基锡基团而高效地转化为相应的卤代形式。
• [EN] ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE<br/>[FR] COMPOSÉS ANESTHÉSIQUES ET PROCÉDÉS D'UTILISATION AFFÉRENTS
  申请人：GEN HOSPITAL CORP

  公开号：WO2013106717A1

  公开（公告）日：2013-07-18

  Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.

  本文提供了符合以下式(I)的化合物。本文还提供了一种包含符合式(I)的化合物和药用可接受载体的药物组合物，以及通过给予受试者这种药物组合物来提供麻醉的方法。