DERIVATIVES OF OLEANOLIC ACID AND δ-OLEANOLIC ACID AND MEDICAL USE THEREOF

• Main Authors: SUN, Hongbin, LIU, Liu, CHENG, Yalong, QIN, Luzhe, LI, Haobin, DAI, Liang, HU, Kaiwen, LIU, Jun
• Format: Patent
• Language: Chinese; English; French
• Published: 30.12.2020
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; STEROIDS

Disclosed are derivatives of novel pentacyclic triterpenoid AMPK agonists, oleanolic acid and δ-oleanolic acid, and medicinal use thereof, specifically, a compound represented by formula I or formula II, and a pharmaceutically acceptable salt or ester or solvate, which can be used for preparing AMPK agonists having the activity of enhancing an AMPK phosphorylation level and used for preparing a drug for preventing or treating AMPK-mediated diseases. The novel pentacyclic triterpenoid compounds of the present invention have significant AMPK agonist activity, and the activity thereof is significantly better than that of recognized AMPK agonist AICAR, and the compounds also have better pharmacokinetic properties such as oral bioavailability and very good safety. L'invention concerne des dérivés de nouveaux agonistes d'AMPK triterpénoïdes pentacycliques, de l'acide oléanolique et de l'acide δ-oléanolique, et une utilisation médicale associée, en particulier, un composé représenté par la formule I ou la formule II