Title:
HYDROGEN PERSULFIDE PRODRUG AND PHARMACEUTICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/011599
Kind Code:
A1
Abstract:
Disclosed are a hydrogen persulfide prodrug and a pharmaceutical use thereof, belonging to the field of pharmaceutics. The structure of the hydrogen persulfide prodrug is as shown in formula I. The provided hydrogen persulfide prodrug can release H2S2 under the action of an esterase; the hydrogen persulfide prodrug has good stability in PBS, and will not degrade and release H2S2 in the absence of the esterase. In addition to releasing H2S2 under the action of the esterase, most of the remaining by-products of the hydrogen persulfide prodrug are endogenous substances or drug excipients or food additives approved by the FDA, and thus said prodrug has high safety. The provided hydrogen persulfide prodrug can exert an effective analgesic effect in vivo, and the analgesic effect in vivo is better than that of reference compound 301. The hydrogen persulfide prodrug has good clinical application prospects in the preparation of analgesic drugs.
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Inventors:
KE BOWEN (CN)
Application Number:
PCT/CN2022/110332
Publication Date:
February 09, 2023
Filing Date:
August 04, 2022
Export Citation:
Assignee:
UNIV SICHUAN (CN)
International Classes:
C07C321/12; A61K31/095; A61P25/00
Foreign References:
| CN102307889A | 2012-01-04 |
Other References:
PAVLOV V. A., LASKOVICS F. M., MAZUR A. W.: "Developments in the large-scale preparation of oligonucleotides in solution", PHOSPHORUS, SULFUR, AND SILICON AND THE RELATED ELEMENTS, vol. 191, no. 11-12, 1 December 2016 (2016-12-01), pages 1509 - 1512, XP093033070, ISSN: 1042-6507, DOI: 10.1080/10426507.2016.1212343
BÖHME HORST, ROEHR JÜRGEN, SCHLEPHACK WERNER: "über α-Hydroxyalkyl-acyl-sulfide und Alkenyl-acyl-sulfide", JUSTUS LIEBIGS ANNALEN DER CHEMIE, VERLAG CHEMIE GMBH., DE, vol. 648, no. 1, 11 December 1961 (1961-12-11), DE , pages 15 - 21, XP093033078, ISSN: 0075-4617, DOI: 10.1002/jlac.19616480104
YU BINGCHEN, ZHENG YUEQIN, YUAN ZHENGNAN, LI SHANSHAN, ZHU HE, DE LA CRUZ LADIE KIMBERLY, ZHANG JUN, JI KAILI, WANG SIMING, WANG B: "Toward Direct Protein S-Persulfidation: A Prodrug Approach That Directly Delivers Hydrogen Persulfide", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, vol. 140, no. 1, 10 January 2018 (2018-01-10), pages 30 - 33, XP093033081, ISSN: 0002-7863, DOI: 10.1021/jacs.7b09795
BÖHME HORST, ROEHR JÜRGEN, SCHLEPHACK WERNER: "über α-Hydroxyalkyl-acyl-sulfide und Alkenyl-acyl-sulfide", JUSTUS LIEBIGS ANNALEN DER CHEMIE, VERLAG CHEMIE GMBH., DE, vol. 648, no. 1, 11 December 1961 (1961-12-11), DE , pages 15 - 21, XP093033078, ISSN: 0075-4617, DOI: 10.1002/jlac.19616480104
YU BINGCHEN, ZHENG YUEQIN, YUAN ZHENGNAN, LI SHANSHAN, ZHU HE, DE LA CRUZ LADIE KIMBERLY, ZHANG JUN, JI KAILI, WANG SIMING, WANG B: "Toward Direct Protein S-Persulfidation: A Prodrug Approach That Directly Delivers Hydrogen Persulfide", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, vol. 140, no. 1, 10 January 2018 (2018-01-10), pages 30 - 33, XP093033081, ISSN: 0002-7863, DOI: 10.1021/jacs.7b09795
Attorney, Agent or Firm:
GAOYUNG INTELLECTUAL PROPERTY AGENCY (GENERAL PARTNERSHIP) (CN)
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