(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate
• 英文别名: (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate salt；(5R)-7-chloro-5-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;2,4-dioxo-1H-pyrimidine-6-carboxylic acid
• 化学式: C₅H₄N₂O₄*C₁₁H₁₄ClN
• 分子量: 351.79
• InChiKey: OPWLNUCRCHHDDF-QRPNPIFTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.35
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  108
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  乳清酸 、 氯卡色林 、 (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate 在 (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate salt hydrate 、 Compound 1 、 2,6-二氧代-3H-嘧啶-4-羧酸酯 、 异丙醇 作用下， 以 乙腈 、 异丙醇 、 water. (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate salt hydrate 为溶剂， 反应 64.0h， 生成 (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate salt hydrate
  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
• 作为产物：
  描述：

  乳清酸 、 氯卡色林 生成 (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine orotate
  参考文献：
  名称：

  MODIFIED-RELEASE DOSAGE FORMS OF 5-HT2C AGONISTS USEFUL FOR WEIGHT MANAGEMENT

  摘要：

  本发明涉及利用含有(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并哌啶盐及其结晶形式的改良释放剂型的体重管理方法。本发明还涉及(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并哌啶盐、其结晶形式以及含有它们的改良释放剂型。

  公开号：

  EP3485878A1

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。
• ADMINISTRATION OF AN ANTI-OBESITY COMPOUND TO INDIVIDUALS WITH RENAL IMPAIRMENT
  申请人：Anderson Christen M.

  公开号：US20120252787A1

  公开（公告）日：2012-10-04

  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-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.

  本公开涉及一种通过确定个体的肾功能充分水平并向该个体处方或给予治疗有效量的(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、溶剂或水合物来进行体重管理的方法，前提是该个体的肾功能充分水平属于以下组合中的一种：无肾损伤、轻度肾损伤和中度肾损伤。此外，本公开还涉及一种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、溶剂或水合物治疗的方法，通过确定个体的肾功能充分水平并选择个体进行治疗，前提是该个体的肾功能充分水平属于以下组合中的一种：无肾损伤、轻度肾损伤和中度肾损伤。
• Modified-release dosage forms of 5-HT2C agonists useful for weight management
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US10226471B2

  公开（公告）日：2019-03-12

  The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.

  本发明涉及利用包含(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂卓盐及其结晶形式的缓释剂型进行体重管理的方法。本发明进一步涉及(R)-8-氯-1-甲基-2,3,4,5-四氢-1H-3-苯并氮杂卓盐、其结晶形式和包含它们的缓释剂型。
• MODIFIED-RELEASE DOSAGE FORMS OF 5-HT2C AGONISTS USEFUL FOR WEIGHT MANAGEMENT& xA;
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2611427A2

  公开（公告）日：2013-07-10
• ADMINISTRATION OF LORCASERIN TO INDIVIDUALS WITH RENAL IMPAIRMENT
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2611449A1

  公开（公告）日：2013-07-10