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Substituted Triazine and Purine Compounds for the Treatment of Chagas Disease and African Trypanosomiasis

Posted Jun 15 2010 5:00pm

Description of Invention:
Parasitic protozoa are responsible for a wide variety of infections in both humans and animals. Trypanosomiasis poses health risks to millions of people across multiple countries in Africa and North and South America. Visitors to these regions, such as business travelers and tourists, are also at risk for contracting parasitic diseases. There are two types of African trypanosomiasis, also known as sleeping sickness. One type is caused by the parasite Trypanosoma brucei gambiense, and the other is caused by the parasite Trypanosoma brucei rhodesiensi. If left untreated, African sleeping sickness results in death. Chagas disease, caused by Trypanosoma cruzi (T. cruzi), affects millions of people in Mexico and South and Central America. Untreated, Chagas disease causes decreased life expectancy and can also result in death.

The subject invention covers novel triazine and purine compounds that are inhibitors of key proteases (cruzain and Rhodesian) of the parasites Trypanosoma brucei rhodesiensi and Trypanosoma cruzi, respectively.

Prophylactic and therapeutic treatment of African trypanosomiasis and Chagas disease

  • Novel compounds against the cysteine proteases, cruzain and rhodesain
  • Compounds possess low nanomolar inhibitory potential against cruzain and rhodesain

Development Status:
In vitro and in vivo data are available upon request and upon execution of an appropriate confidentiality agreement.

Craig J Thomas (NHGRI)

Patent Status:
HHS, Reference No. E-267-2008/0
PCT, Application No. PCT/US2009/063078 filed 03 Nov 2009

Relevant Publication:
  1. Mott BT et al. Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem. 2010 Jan 14;53(1):52-60. [ PubMed: 19908842 ]

Licensing Status:
Available for licensing.

Collaborative Research Opportunity:
The NIH Chemical Genomics Center (NCGC) is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize appropriate lead compounds described in the patent application. Please contact Dr. Craig J. Thomas ( ) or Claire Driscoll ( ), Director of the NHGRI Technology Transfer Office, for more information.

Infectious Diseases
Infectious Diseases - Therapeutics
Rare Diseases
Neglected Diseases
In-vivo Data
In-vitro Data

For Additional Information Please Contact:
Kevin Chang Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-5018
Fax: 301-402-0220

Ref No: 1914

Updated: 06/2010

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