3-(2-dimethylaminomethyl-1-hydroxy-cyclohexyl)phenyl 2-(6-methoxy-naphthalen-2-yl)-propionate | 269079-67-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 3-(2-dimethylaminomethyl-1-hydroxy-cyclohexyl)phenyl 2-(6-methoxy-naphthalen-2-yl)-propionate
• 英文别名: [3-[2-[(Dimethylamino)methyl]-1-hydroxycyclohexyl]phenyl] 2-(6-methoxynaphthalen-2-yl)propanoate
• CAS: 269079-67-6
• 化学式: C₂₉H₃₅NO₄
• 分子量: 461.601
• InChiKey: HENAWWPPFYOHNA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  34
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Novel esters derived from (rr,ss)-2-hydroxybenzoate of 3-(2-dimethylaminomethyl-1-hydroxycyclohexyl)phenyl
  申请人：——

  公开号：US20030100598A1

  公开（公告）日：2003-05-29

  New esters derived from substituted phenyl-cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.

  新的酯类化合物来源于取自曲马多（Tramadol）的取代苯基-环己基化合物，其制备方法以及它们用于制备具有镇痛性质的药物。这些新化合物的通式（I）具有比曲马多更高的镇痛活性，更低的毒性和更长的有效时间。
• NEW ESTERS DERIVED FROM SUBSTITUTED PHENYL-CYCLOHEXYL COMPOUNDS
  申请人：VITA-INVEST, S.A.

  公开号：EP1127871A1

  公开（公告）日：2001-08-29

  New csters derived from substituted phenyl cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analges activcity, a lower toxicity and a longer effective time period than Tramadol.

  从曲马多衍生的取代苯基环己基化合物的新酯类、获得过程及其在制备具有镇痛特性的药物中的用途。与曲马多相比，这些通式（I）的新化合物具有更高的镇痛活性、更低的毒性和更长的有效期。
• New esters derived from substituted phenyl-cyclohexyl compounds
  申请人：VITA-INVEST, S.A.

  公开号：EP1219594A1

  公开（公告）日：2002-07-03

  New esters derived from substituted phenylcyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.

  由取代苯基环己基化合物衍生的新酯类，这些化合物是从曲马多衍生出来的，它们的获得过程以及它们在制备具有镇痛特性的药物中的用途。与曲马多相比，这些通式（I）的新化合物具有更高的镇痛活性、更低的毒性和更长的有效期。
• TAMPER-RESISTANT DOSAGE FORM WITH IMMEDIATE RELEASE AND RESISTANCE AGAINST SOLVENT EXTRACTION
  申请人：Grünenthal GmbH

  公开号：EP3698776A1

  公开（公告）日：2020-08-26

  The invention relates to a tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, preferably selected from opioids; a polyalkylene oxide having a weight average molecular weight within the range of from 200,000 g/mol to 2,000,000 g/mol, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 20 wt.-%, based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.

  本发明涉及一种防篡改药物剂型，其包括多种颗粒，这些颗粒包括药理活性化合物，优选选自阿片类药物；聚环氧烷，其重量平均分子量在200,000g/mol至2,000,000g/mol范围内；以及崩解剂；其中，药理活性化合物分散在由聚环氧烷和崩解剂组成的基质中；其中，基于颗粒的总重量，崩解剂的含量超过20重量％；其中，基于颗粒的总重量，聚环氧烷的含量至少为25重量％；以及其中，该剂型可在药理活性化合物和崩解剂的作用下立即崩解。其中，基于颗粒的总重量，崩解剂的含量超过 20 wt.-%；其中，基于颗粒的总重量，聚氧化亚烷烃的含量至少为 25 wt.-%；其中，根据 Ph. Eur.
• Abuse-proofed dosage form
  申请人：GRÜNENTHAL GMBH

  公开号：US10058548B2

  公开（公告）日：2018-08-28

  The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.

  本发明涉及一种热成型而不变色并可防止滥用的剂型，它包括至少一种断裂强度至少为 500 N 的合成或天然聚合物，以及一种或多种可能被滥用的活性物质。本发明还涉及生产上述剂型的相应方法。