(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate | 1362911-02-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate
• 英文别名: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate salt；(R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate salt；(5R)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;(2S)-5-oxopyrrolidine-2-carboxylic acid
• CAS: 1362911-02-1
• 化学式: C₅H₇NO₃*C₁₁H₁₄ClN
• 分子量: 324.807
• InChiKey: IGYALZWCULJTGN-YYTBSQRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.94
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  78.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  L-焦谷氨酸 、 氯卡色林 以 乙酸乙酯 为溶剂， 反应 16.0h， 生成 (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate
  参考文献：
  名称：

  Administration of an anti-obesity compound to individuals with renal impairment

  摘要：

  本公开涉及通过确定个体的肾功能充分水平并向该个体开具或施用(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂环或其药学上可接受的盐、溶剂或水合物的治疗有效量来进行个体的体重管理的方法，前提是个体的肾功能充分水平属于以下组合中的一种：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。此外，本公开还涉及通过确定个体的肾功能充分水平并从需要体重管理的多个个体中选择个体进行(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂环或其药学上可接受的盐、溶剂或水合物的治疗，如果个体的肾功能充分水平属于以下组合中的一种：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。

  公开号：

  US08999970B2

文献信息

• ADMINISTRATION OF LORCASERIN TO INDVIDUALS WITH RENAL IMPAIRMENT
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2939677A1

  公开（公告）日：2015-11-04

  The present disclosure relates to methods for weight management in an individual in need thereof by determining the level of renal sufficiency of the individual and prescribing or administering a therapeutically effective amount of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-ben-zazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof to the individual, provided that the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment. In addition, the disclosure relates to a method for selecting an individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-ben-zazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof from a plurality of individuals in need of weight management by determining the level of renal sufficiency of the individual and selecting the individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-ben-zazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof if the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment.

  本公开涉及一种通过确定个体的肾功能充分性水平并向该个体开具或给予(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并噁唑啉或其药学上可接受的盐、溶剂或水合物的治疗有效量来进行个体的体重管理的方法，前提是该个体的肾功能充分性水平选自以下组合：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。此外，本公开涉及一种通过确定个体的肾功能充分性水平并从需要体重管理的众多个体中选择个体进行(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并噁唑啉或其药学上可接受的盐、溶剂或水合物治疗的方法，如果该个体的肾功能充分性水平选自以下组合：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。
• [EN] SALTS OF LORCASERIN WITH OPTICALLY ACTIVE ACIDS<br/>[FR] SELS DE LORCASÉRINE DOTÉS D'ACIDES OPTIQUEMENT ACTIFS
  申请人：ARENA PHARM INC

  公开号：WO2012030938A1

  公开（公告）日：2012-03-08

  Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.

  含有光学活性酸的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并哌啶盐，以及包括它们的药物组合物，可用于诸如体重管理等用途。
• SALTS OF LORCASERIN WITH OPTICALLY ACTIVE ACIDS
  申请人：Blackburn Anthony C.

  公开号：US20130310369A1

  公开（公告）日：2013-11-21

  Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.

  8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并嗪的盐，与手性酸混合制成的药物组合物，可用于体重管理等用途。
• Salts of lorcaserin with optically active acids
  申请人：Blackburn Anthony C.

  公开号：US09248133B2

  公开（公告）日：2016-02-02

  Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.

  含有手性酸的8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并嗪盐，以及包含它们的药物组合物，可用于体重管理等用途。
• Administration of an anti-obesity compound to individuals with renal impairment
  申请人：Anderson Christen M.

  公开号：US08999970B2

  公开（公告）日：2015-04-07

  The present disclosure relates to methods for weight management in an individual in need thereof by determining the level of renal sufficiency of the individual and prescribing or administering a therapeutically effective amount of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof to the individual, provided that the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment. In addition, the disclosure relates to a method for selecting an individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof from a plurality of individuals in need of weight management by determining the level of renal sufficiency of the individual and selecting the individual for treatment with (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine or a pharmaceutically acceptable salt, solvate or hydrate thereof if the individual has a level of renal sufficiency selected from the group consisting of: no renal impairment, mild renal impairment, and moderate renal impairment.

  本公开涉及通过确定个体的肾功能充分水平并向该个体开具或施用(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂环或其药学上可接受的盐、溶剂或水合物的治疗有效量来进行个体的体重管理的方法，前提是个体的肾功能充分水平属于以下组合中的一种：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。此外，本公开还涉及通过确定个体的肾功能充分水平并从需要体重管理的多个个体中选择个体进行(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂环或其药学上可接受的盐、溶剂或水合物的治疗，如果个体的肾功能充分水平属于以下组合中的一种：无肾功能障碍、轻度肾功能障碍和中度肾功能障碍。