Oleanolic acid derivatives for pharmaceutical use: a patent review

Area of Science:

• Natural Product Chemistry
• Pharmacology
• Medicinal Chemistry

Background:

• Oleanolic acid is a pentacyclic triterpene with a history of use as an OTC hepatoprotective agent in China.
• It and its derivatives exhibit diverse biological activities, suggesting broad therapeutic applications.

Purpose of the Study:

• To review patents on oleanolic acid and its derivatives from 1971-2015.
• To focus on their preparation, pharmaceutical compositions, and various medical uses.

Main Methods:

• Analysis of representative patent publications.
• Emphasis on Chinese patents detailing therapeutic applications.
• Review of anticancer, anti-osteoporosis, anti-obesity, anti-diabetic, lipid-lowering, anti-inflammatory, antioxidant, immune-regulatory, and hepatoprotective effects.

Main Results:

• Patents cover preparation, formulations, and diverse therapeutic uses of oleanolic acid derivatives.
• Significant patent activity highlights potential in multiple disease areas.
• Anticancer, metabolic, and immunological applications are prominent.

Conclusions:

• Detailed efficacy studies are needed to confirm clinical potential.
• Identifying protein targets is crucial for drug development and new lead compound discovery.
• Oleanolic acid has substantial potential for drug repositioning, especially in metabolic and immunological disorders.