(1RS,2RS)-1-methyl-2, 3-diphenylpropylamine

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: (1RS,2RS)-1-methyl-2, 3-diphenylpropylamine
• 英文别名: N-2,3-diphenyl-1-methylpropylamine；3,4-Diphenylbutan-2-amine
• 化学式: C₁₆H₁₉N
• 分子量: 225.334
• InChiKey: QTSZOGCIAOJLQV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  4-氯-a-甲基-b-苯基-苯丙胺盐酸盐(1:1) 、 氯贝酸 、 (1RS,2RS)-1-methyl-2, 3-diphenylpropylamine 在 草酰氯 、 N,N-二甲基甲酰胺 、 碳酸氢钠 作用下， 以 二氯甲烷 、 水 为溶剂， 反应 0.5h， 生成 N-(2,3-diphenyl-1-methylpropyl)-2-(4-chlorophenoxy)-2-methylpropanamide
  参考文献：
  名称：

  [EN] SUBSTITUTED AMIDES ACTIVE AT THE CANNABINOID-1 RECEPTOR
  [FR] AMIDES SUBSTITUES ACTIFS AU NIVEAU DU RECEPTEUR DE CANNABINOIDE-1

  摘要：

  结构式（I）的新化合物是大麻素-1（CB1）受体的拮抗剂和/或逆向激动剂，并且可用于治疗、预防和抑制由CB1受体介导的疾病。本发明的化合物可作为中枢作用药物用于治疗精神病、记忆障碍、认知障碍、偏头痛、神经病、神经炎性疾病包括多发性硬化和吉兰-巴雷综合征以及病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、压力、癫痫、帕金森病、运动障碍和精神分裂症。这些化合物还可用于治疗物质滥用障碍、肥胖症或进食障碍的治疗，以及治疗哮喘、便秘、慢性肠道假性梗阻和肝硬化。

  公开号：

  WO2004048317A1

文献信息

• [EN] SUBSTITUTED AMIDES<br/>[FR] AMIDES SUBSTITUES
  申请人：MERCK & CO INC

  公开号：WO2003077847A2

  公开（公告）日：2003-09-25

  Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

  结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗、预防和抑制由CB1受体介导的疾病。本发明的化合物可作为中枢作用药物，用于治疗精神病、记忆障碍、认知障碍、偏头痛、神经病、神经炎性疾病（包括多发性硬化和格林-巴利综合征）以及病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、压力、癫痫、帕金森病、运动障碍和精神分裂症。这些化合物还可用于治疗物质滥用障碍、肥胖症或进食障碍，以及哮喘、便秘、慢性肠假性梗阻和肝硬化的治疗。
• Substituted amides
  申请人：——

  公开号：US20040058820A1

  公开（公告）日：2004-03-25

  Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

  结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗、预防和抑制由CB1受体介导的疾病。本发明的化合物可作为中枢作用药物用于治疗精神病、记忆障碍、认知障碍、偏头痛、神经病、神经炎症性疾病，包括多发性硬化症和格林-巴利综合症以及病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、应激、癫痫、帕金森病、运动障碍和精神分裂症。这些化合物还可用于治疗物质滥用障碍、肥胖症或进食障碍，以及哮喘、便秘、慢性肠假性梗阻和肝硬化的治疗。
• Aralkyl amines as cannabinoid receptor modulators
  申请人：Shah K. Shrenik

  公开号：US20070088058A1

  公开（公告）日：2007-04-19

  Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

  结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗、预防和抑制由CB1受体介导的疾病。本发明的化合物可用作中枢作用药物，用于治疗精神病、记忆障碍、认知障碍、偏头痛、神经病、神经炎性疾病（包括多发性硬化和格林-巴利综合症）、病毒性脑炎、脑血管意外和头部创伤的炎症后遗症、焦虑症、压力、癫痫、帕金森病、运动障碍和精神分裂症。该化合物还可用于治疗物质滥用障碍，包括酒精和尼古丁成瘾，治疗肥胖症或进食障碍，以及治疗哮喘、便秘、慢性肠假性梗阻和肝硬化。
• Substituted amic acid derivatives useful for treatment of arteriosclerosis
  申请人：BANYU PHARMACEUTICAL CO., LTD.

  公开号：EP0611749A1

  公开（公告）日：1994-08-24

  A compound of the formula (I) or its pharmaceutically acceptable salt or ester: wherein each of which are the same or different, is an aryl group or a heteroaromatic ring group; A is a C₃₋₈ linear saturated or unsaturated aliphatic hydrocarbon group which may have substituent(s) selected from the group consisting of a lower alkyl group, a hydroxyl group, a lower alkoxy group, a carboxyl group, an aryl group and an aralkyl group; Q is a single bond or a group of the formula -CO-O-, -O-CO-, -CH₂CH₂-, -CH=CH-, -OCH₂-, -SCH₂-, -CH₂O- or -CH₂S-; each of R¹, R², R³ and R⁴ which are the same or different, is a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxyl group, a lower alkoxy group, or an aryl or heteroaromatic ring group which may have substituent(s) selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; each of R⁵, R⁶ and R⁷ which are the same or different, is a hydrogen atom or a lower alkyl group; and R⁸ is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or an aralkyl group, provided that when Q is a single bond, are not simultaneously 4-chlorophenyl groups.

  式 (I) 的化合物或其药学上可接受的盐或酯： 其中 A 是 C₃₋₈线型饱和或不饱和脂肪族烃基，其取代基可选自低级烷基、羟基、低级烷氧基、羧基、芳基和芳烷基；Q 是单键或式 -CO-O-、-O-CO-、-CH₂CH₂-、-CH=CH-、-OCH₂-、-SCH₂-、-CH₂O- 或 -CH₂S- 的基团；R¹、R²、R³ 和 R⁴ 中相同或不同的每一个是氢原子、卤素原子、低级烷基、羟基、低级烷氧基或芳基或杂芳环基，其取代基可选自卤素原子、低级烷基和低级烷氧基组成的组；相同或不同的 R⁵、R⁶ 和 R⁷ 均为氢原子或低级烷基；R⁸ 为氢原子、低级烷基、低级烯基、低级炔基或芳烷基，条件是 Q 为单键、 不同时为 4-氯苯基。
• SUBSTITUTED AMIDES
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP1496838B1

  公开（公告）日：2010-11-03