(卤)-SIBUTRAMINEMETHANESULFOTE | 676598-10-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (卤)-SIBUTRAMINEMETHANESULFOTE
• 中文别名: 甲磺酸西布曲明
• 英文名称: Sibutramine methanesulfonate
• 英文别名: 1-[1-(4-chlorophenyl)cyclobutyl]-N,N,3-trimethylbutan-1-amine;methanesulfonic acid
• CAS: 676598-10-0
• 化学式: C18H30ClNO3S
• 分子量: 376.0
• InChiKey: MWKDQYLHASOIBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.24
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  66
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  西布曲明 以93的产率得到(卤)-SIBUTRAMINEMETHANESULFOTE
  参考文献：
  名称：

  包含西布曲明甲磺酸盐半水合物晶体的药物组合物

  摘要：

  本发明涉及用于治疗或者预防肥胖的药物组合物，其包括式(I)的新型西布曲明甲磺酸盐半水合物晶体。与西布曲明盐酸盐单水合物相比，根据本发明的西布曲明甲磺酸盐半水合物晶体在水中具有更高的溶解度，而且在高湿度/温度条件下具有增强的稳定性。

  公开号：

  CN1688297A

文献信息

• [EN] METHODS OF USING AND COMPOSITIONS COMPRISING DOPAMINE REUPTAKE INHIBITORS<br/>[FR] PROCEDES D'UTILISATION D'INHIBITEURS DE RECAPTAGE DE LA DOPAMINE ET COMPOSITIONS CONTENANT CES DERNIERS
  申请人：SEPRACOR INC

  公开号：WO2000010551A2

  公开（公告）日：2000-03-02

  Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites like desmethylsibutramine and didesmethylsibutramine and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3, antagonists.

  本发明涉及治疗和预防多种疾病和症状的方法，包括但不限于勃起功能障碍、情感障碍、体重增加、脑功能障碍、疼痛、强迫症、物质滥用、慢性疾病、焦虑、进食障碍、偏头痛和失禁。该方法包括给予多巴胺再摄取抑制剂和可选的其他药理活性化合物。还公开了包含多巴胺再摄取抑制剂和可选的其他药理活性化合物的制药组合物和剂型。优选的多巴胺再摄取抑制剂是外消旋或光学纯的西布曲明代谢物，如去甲基西布曲明和二去甲基西布曲明及其药学上可接受的盐、溶剂和包合物。优选的其他药理活性化合物包括影响中枢神经系统的药物，如5-HT3拮抗剂。
• 包含西布曲明甲磺酸盐半水合物晶体的药物组合物
  申请人：韩美控股株式会社

  公开号：CN1688297A

  公开（公告）日：2005-10-26

  本发明涉及用于治疗或者预防肥胖的药物组合物，其包括式(I)的新型西布曲明甲磺酸盐半水合物晶体。与西布曲明盐酸盐单水合物相比，根据本发明的西布曲明甲磺酸盐半水合物晶体在水中具有更高的溶解度，而且在高湿度/温度条件下具有增强的稳定性。
• [EN] PHARMACEUTICAL COMPOSITION COMPRISING CRYSTALLINE SIBUTRAMINE METHANESULFONATE HEMIHYDRATE<br/>[FR] COMPOSITION PHARMACEUTIQUE COMPRENANT DE L'HEMIHYDRATE DE METHANESULFONATE DE SIBUTRAMINE CRISTALLIN
  申请人：HANMI PHARM IND CO LTD

  公开号：WO2004030663A1

  公开（公告）日：2004-04-15

  The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate.

  本发明涉及一种用于治疗或预防肥胖症的药物组合物，包括公式（I）的新型结晶甲磺酸西布曲明半水合物。根据本发明，甲磺酸西布曲明半水合物晶体在水中的溶解度更高，在高湿度/温度条件下也比盐酸西布曲明单水合物稳定性更强。
• Pharmaceutical composition comprising crystalline sibutramine methanesulfonate hemihydrate
  申请人：——

  公开号：US20040068018A1

  公开（公告）日：2004-04-08

  The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate. 1

  本发明涉及一种用于治疗或预防肥胖症的药物组合物，包括式(I)的新型晶体硫酸甲磺酰西布曲明半水合物。根据本发明的晶体硫酸甲磺酰西布曲明半水合物与盐酸单水合物相比，在水中的溶解度更高，并在高湿度/高温环境下具有增强的稳定性。
• Controlled release dosage form
  申请人：TRIASTEK, INC.

  公开号：US10143626B2

  公开（公告）日：2018-12-04

  The present invention generally relates to a pharmaceutical dosage form and controlled release of biologically active agents, diagnostic agents, reagents, cosmetic agents, and agricultural/insecticide agents. In one embodiment, the dosage form has a substrate that forms a compartment, wherein the substrate includes at least a first piece and a second piece, wherein the first piece operably links to the second piece. The dosage form contains a drug content that is loaded into the compartment. The dosage form also has a releaser operably linked to the substrate which upon contact with water or body fluid is capable of separating the first and second piece to open the compartment and release the drug content.

  本发明一般涉及一种药物剂型和生物活性制剂、诊断制剂、试剂、化妆品制剂和农用/杀虫剂制剂的控制释放。在一个实施方案中，该剂型具有形成隔室的基质，其中基质至少包括第一片和第二片，其中第一片与第二片可操作地连接。剂型含有装入隔室的药物成分。该剂型还具有与基质可操作连接的释放器，该释放器在与水或体液接触时能够分离第一和第二片，从而打开隔室并释放药物成分。