美他佐辛 | 3734-52-9

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 6,7-苯并吗啡烷
• 中文名称: 美他佐辛
• 中文别名: 甲基镇痛新；间唑新
• 英文名称: metazocine
• 英文别名: 8-Hydroxy-2,6-methano-3,6,11-trimethyl-1,2,3,4,5,6-hexahydro-3-benzazocin；1,2,3,4,5,6-Hexahydro-3,6,11-trimethyl-8-hydroxy-2,6-methan-3-benzazocin；α-2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan；β-2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan；2'-Hydroxy-2,5,9-trimethyl-6,7-benzomorphan；2,5,9-Trimethyl-2'-hydroxy-6,7-benzomorphan；1,10,13-trimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol
• CAS: 3734-52-9
• 化学式: C₁₅H₂₁NO
• 分子量: 231.338
• InChiKey: YGSVZRIZCHZUHB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  美他佐辛 、 苯甲酰氯 以77%的产率得到
  参考文献：
  名称：

  HORI, MIKIO;BAN, MASATOSHI;IMAI, EIJI;IWATA, NORIYUKI;SUZUKI, YOSHINARI;B+, J. MED. CHEM., 1985, 28, N 11, 1656-1666

  摘要：

  DOI：
• 作为产物：
  描述：

  N-methyl-2-(4-methoxybenzyl)-3,4-dimethyl-1,2,5,6-tetrahydropyridine 在 氢溴酸 作用下， 以 水 为溶剂， 反应 24.0h， 以62%的产率得到美他佐辛
  参考文献：
  名称：

  A Short Synthesis of Benzomorphane Analgesics (±)-Metazocine and (±)-Phenazocine

  摘要：

  A three step synthesis of (+/-)-metazocine and (+/-)-phenazocine starting with 3,4-lutidine is described. The key step involves Lewis acid promoted lithiation/electrophilic substitution reaction of N-alkyl-3,4-dimethyl-1,2,5,6- tetrahydropyridine.

  DOI：

  10.1080/00397910903531722

文献信息

• Controlled-release compositions containing opioid agonist and antagonist
  申请人：——

  公开号：US20020010127A1

  公开（公告）日：2002-01-24

  Controlled-release dosage forms containing an opioid agonist; an opioid antagonist; and a controlled release material release during a dosing interval an analgesic or sub-analgesic amount of the opioid agonist along with an amount of said opioid antagonist effective to attenuate a side effect of said opioid agonist. The dosage form provides analgesia for at least about 8 hours when administered to human patients. In other embodiments, the dose of antagonist released during the dosing interval enhances the analgesic potency of the opioid agonist.

  含有阿片激动剂、阿片拮抗剂和受控释放材料的控释剂型，其在给药间隔期间释放阿片激动剂的镇痛或亚镇痛量以及足以减轻所述阿片激动剂的副作用的阿片拮抗剂的量。当给予人类患者时，该剂型提供至少约8小时的镇痛作用。在其他实施例中，给药间隔期释放的拮抗剂剂量增强了阿片激动剂的镇痛效力。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
  申请人：Cerulean Pharma Inc.

  公开号：US20130196906A1

  公开（公告）日：2013-08-01

  Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.

  提供了关于使用CDP-治疗剂偶联物治疗疾病或紊乱的方法，例如自身免疫疾病、炎症性疾病、中枢神经系统紊乱、心血管疾病或代谢紊乱。还提供了CDP-治疗剂偶联物、包含CDP-治疗剂偶联物的颗粒以及包含CDP-治疗剂偶联物的组合物。
• 3,4,6-Substituted pyridazines for treating neuropathic pain and associated syndromes
  申请人：Sultzbaugh Lance

  公开号：US20070191365A1

  公开（公告）日：2007-08-16

  The present invention is directed to the use of 3,4,6-substituted pyridazines such as those characterized by structure I for treating conditions such as neuropathic pain among others.

  本发明涉及使用3,4,6-取代吡啶嗪，如结构I所示的化合物，用于治疗神经病痛等疾病。
• [EN] BUPRENORPHINE ANALOGS<br/>[FR] ANALOGUES DE BUPRÉNORPHINE
  申请人：PURDUE PHARMA LP

  公开号：WO2012038813A1

  公开（公告）日：2012-03-29

  The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R 3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

  本发明涉及如下所示的公式(I)、公式(IA)或公式(IB)的丁丙诺啡类似物化合物，其中R1、R2、R8、R 3a、R 3b、G、X、Z和Y的定义如本文所述。本发明的化合物可用于治疗疼痛、便秘以及通过阿片类和ORL-1受体的活性调节的其他状况。
• PYRIDINE AND PIPERIDINE DERIVATIVES AND USE THEREOF
  申请人：Purdue Pharma L.P.

  公开号：US20150141434A1

  公开（公告）日：2015-05-21

  The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R 1 , R 4 , X, G, n, p, W 1 , W 2 , W 3 , W 4 , and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.

  本发明提供了一种用作钠通道阻断剂的化合物。在一方面，本发明提供了公式I的化合物： 或其药用可接受的盐、溶剂化物、水合物或对映异构体，其中R1、R4、X、G、n、p、W1、W2、W3、W4和E环在公开中定义。在某些实施例中，本发明提供了上述公式II-XIII的化合物。本发明还提供了使用上述任何讨论公式的化合物来治疗对钠通道阻断有反应的疾病。在一个实施例中，发明化合物用于治疗疼痛。

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