2-(4-methylpiperazin-1-yl)-2-oxoethyl 2-(4-chlorobenzoylamino)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(4-methylpiperazin-1-yl)-2-oxoethyl 2-(4-chlorobenzoylamino)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionate
• 英文别名: 2-(4-Methylpiperazin-1-yl)-2-oxoethyl 2-(4-chlorobenzoylamino)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionate；[2-(4-methylpiperazin-1-yl)-2-oxoethyl] 2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1H-quinolin-4-yl)propanoate
• 化学式: C₂₆H₂₇ClN₄O₅
• 分子量: 510.977
• InChiKey: MTQTYLJORZRFGP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  108
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-(2-bromoacetyl)-4-methylpiperazin-1-ium bromide 、 瑞巴派特 以to afford the title compound as a white solid (0.1 g)的产率得到2-(4-methylpiperazin-1-yl)-2-oxoethyl 2-(4-chlorobenzoylamino)-3-(2-oxo-1,2-dihydroquinolin-4-yl)propionate
  参考文献：
  名称：

  NOVEL REVAMIPIDE PRODRUGS, PREPARATION METHOD AND USE THEREOF

  摘要：

  本发明公开了一种新型的雷巴韦胺前药，其制备方法和使用方法。同时，提供了一种包含该新型雷巴韦胺前药作为活性成分的制药组合物。该雷巴韦胺前药的吸收速度比雷巴韦胺本身提高了25倍，可用于预防或治疗胃溃疡、急性胃炎、慢性胃炎、干眼症、癌症、骨关节炎、类风湿性关节炎或肥胖症。

  公开号：

  US20150141409A1

文献信息

• NOVEL REVAMIPIDE PRODRUGS, PREPARATION METHOD AND USE THEREOF
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US20150141409A1

  公开（公告）日：2015-05-21

  Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

  揭示了一种新型的雷巴米特前药，以及其制备方法和用途。此外，提供了一种含有该新型雷巴米特前药作为活性成分的药物组合物。与雷巴米特本身相比，雷巴米特前药的吸收速率增加了25倍，可用于预防或治疗胃溃疡、急性胃炎、慢性胃炎、干眼症、癌症、骨关节炎、类风湿性关节炎或肥胖症。
• ORALLY ADMINISTRABLE PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF DRY EYE SYNDROME, COMPRISING REBAMIPIDE OR PRODRUG THEREOF
  申请人：Samjin Pharmaceutical Co., Ltd.

  公开号：EP2987491A1

  公开（公告）日：2016-02-24

  Disclosed is an oral pharmaceutical composition for preventing or treating dry eye syndrome, which comprises rebamipide or a prodrug thereof, or a pharmaceutically acceptable salt thereof, as an active ingredient. The compounds can treat dry eye syndrome via oral route, and can be thus employed safely and conveniently compared to conventional eye drops.

  本发明公开了一种用于预防或治疗干眼症的口服药物组合物，其活性成分包括瑞巴派特或其原药或其药学上可接受的盐。该化合物可通过口服途径治疗干眼症，与传统眼药水相比，使用安全方便。
• NOVEL REBAMIPIDE PRODRUG, METHOD FOR PRODUCING SAME, AND USAGE THEREOF
  申请人：Samjin Pharmaceutical Co., Ltd.

  公开号：EP2865669B1

  公开（公告）日：2021-04-28
• ORAL PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DRY EYE SYNDROME COMPRISING REBAMIPIDE OR A PRODRUG THEREOF
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US20160081922A1

  公开（公告）日：2016-03-24

  Disclosed is an oral pharmaceutical composition for preventing or treating dry eye syndrome, which comprises rebamipide or a prodrug thereof, or a pharmaceutically acceptable salt thereof, as an active ingredient. The compounds can treat dry eye syndrome via oral route, and can be thus employed safely and conveniently compared to conventional eye drops.
• COMPOSITION FOR PREVENTING OR TREATING SJOGREN'S SYNDROME
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US20210393642A1

  公开（公告）日：2021-12-23

  Provided is a composition for preventing or treating Sjogren's syndrome. A composition for preventing or treating Sjogren's syndrome includes a compound represented by a specific chemical formula, or a pharmaceutically acceptable salt thereof, and has the effect of preventing or treating Sjogren's syndrome.