Benzodiazepine derivative and use thereof

• US 9,994,578 B2
• Filed: 07/22/2015
• Issued: 06/12/2018
• Est. Priority Date: 07/23/2014
• Status: Active Grant

• Current Assignee: Jiangsu Nhwaluokang Pharmceutical Research and Development Co., Ltd.
• Original Assignee: Jiangsu Nhwaluokang Pharmceutical Research and Development Co., Ltd.
• Inventors: Li, Qingeng, Wang, Tao, Xie, Jianyong, Zhang, Guisheng, Xu, Xiangqing
• Primary Examiner(s): COLEMAN, BRENDA LIBBY
• Application Number:
  US15/327,969
• Publication Number:
  US 20170217965A1
• Time in Patent Office: 1,056 Days
• CPC Class Codes: A61P 1/06 Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: C07D 487/04 Ortho-condensed systems

Abstract

The present invention relates to a new benzodiazepine derivative, pharmaceutically acceptable salt thereof, preparation method therefor, and use thereof. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have obvious anesthetic effect and low toxicity in body, thereby enhancing the medication safety. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have sedative, hypnotic, and anesthetic effect, and can be used as sedative, hypnotic, and anesthetic drugs.

Claims

1. A compound of formula (I) or a pharmaceutically acceptable salt thereof:

2. The compound according to claim 1 or the pharmaceutically acceptable salt thereof, wherein the pharmaceutically acceptable salt is presented by formula (Ia):

3. The compound according to claim 1 or the pharmaceutically acceptable salt thereof, which is selected from the group consisting of remimazolam acid ethyl ester, remimazolam acid ethyl ester p-toluenesulfonate, remimazolam acid ethyl ester benzenesulfonate, remimazolam acid ethyl ester methanesulfonate and remimazolam acid ethyl ester ethanesulfonate.

4. A pharmaceutical composition, comprising the compound according to claim 1 or the pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

5. A method for providing anesthesia, comprising administrating the compound according to claim 1 or the pharmaceutically acceptable salt thereof to a subject in need thereof.

6. A method for providing sedation, comprising administrating the compound according to claim 1 or the pharmaceutically acceptable salt thereof optionally in combination with opiates to a subject in need thereof.

7. The compound according to claim 2 or the pharmaceutically acceptable salt thereof, wherein said acid is hydrochloric acid (HCl), hydrobromic acid (HBr), methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, or a combination thereof.