Indazole derivatives and their therapeutic applications: a patent review (2013-2017)

ABSTRACT

Introduction: Indazoles are heterocyclic moieties rarely found in nature. They are nitrogen containing chemical compounds composed of a pyrazole ring condensed with a benzene ring. Various indazole derivatives have been described with a wide variety of biological activities. This has aroused great interest in the development of novel indazole based therapeutic agents.

Areas covered: Forty-two patents published within the last 5 years (2013–2017) describing derivatives with the indazole scaffold and their therapeutic applications were analysed.

Expert opinion: The indazole scaffold is of great pharmacological importance as it forms the basic structure of a large number of compounds with potential therapeutic value. Derivatives have been found to possess promising anticancer and anti-inflammatory activity and have also found application in disorders involving protein kinases (aside from cancer) and neurodegeneration. The compounds where mechanism of action is defined can afford new molecules with biological and therapeutic properties.

KEYWORDS:

• Indazole
• therapeutic applications
• anticancer
• anti-inflammatory
• neurological disorders
• protein kinases

Article highlights

• Indazole is an important heterocyclic system with great significance in the pharmaceutical industry as well as being a useful synthon for the synthesis of many bridgehead heterocycles.

• New indazole derivatives have been synthesised and patented for a wide variety of target pathways and conditions.

• Indazole derivatives are versatile agents having different therapeutic applications in diseases such as cancer, inflammation, bacterial infections and neurodegenerative disorders.

• As there is a continuous need for new molecules to be introduced in the treatment of these diseases, the use of substituted indazoles is a valid approach to expand on the number of new lead compounds for further development.

• The patent literature on indazole derivatives with the focus on various therapeutic uses, covering the years 2013-2017 is reviewed.

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Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties. Peer reviewers on this manuscript have no relevant financial or other relationships to disclose

Additional information

Funding

This paper has not been funded.