Recent advances in antitrypanosomal chemotherapy: patent literature 2002 – 2004

Abstract

Sleeping sickness and Chagas disease (African and American trypanosomiases, respectively) are protozoan parasitic diseases threatening millions of people in sub-Saharan Africa and Latin America. Trypanosomiases are among the most neglected diseases in the world, desperately lacking financial support for investigation. The current chemotherapy of both diseases is poor and suffers from intolerable side effects and low efficacy in many cases. A review of the patent literature from 2002 to early 2005 claiming molecules with antitrypanosomal activity afforded 36 entries, equally shared between industry and acadaemia. Among the targets validated against trypanosomes, patents dealing with protease inhibitors were the most represented (16 patents). Other targets claimed in the patent literature included membrane architecture (sterol biosynthesis inhibitors, protein farnesyltransferase inhibitors), DNA (DNA binders, tubulin inhibitors) and pyrimidine metabolism (cytidine triphosphate [CTP] synthetase inhibitors). Natural products were also a great source of trypanocidal lead compounds (9 patents). A few patents claiming compounds with antitrypanosomal activity, but disclosing no specific target, were also encountered.

Keywords::

• Chagas disease
• chemotherapy
• DNA binder
• human African trypanosomiasis (HAT)
• protease inhibitor
• sleeping sickness
• sterol biosynthesis inhibitor
• Trypanosoma brucei
• Trypanosoma cruzi