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Novel Antimalarial Compounds, Methods of Synthesis Thereof, Pharmaceutical Compositions Comprising Same, and Methods of Using Same for Treatment and Prevention of Malaria

Description of Invention:
According to data recently reported by the World Health Organization (WHO), the death rate from malaria exceeds one million individuals per year. The Public Health Service seeks exclusive or non-exclusive licensee(s) to develop and commercialize the technology claimed within the portfolio of U.S. patents issued and pending, and corresponding international patents issued and pending. These patents and pending applications claim an exceptionally broad universe of novel naphthylisoquinoline alkaloid compounds, and methods of total synthesis thereof.

Representative examples of these compounds have been shown to have potent in vitro activity against malaria parasites, including parasites that are highly resistant to available antimalarial drugs. Representative examples have also been shown to have potent in vivo activity against malaria parasites in animal models. Pharmaceutical compositions comprising these compounds, as well as methods of using the compounds to treat or prevent a malarial infection of a host, are claimed. The relative structural simplicity of this class of compounds, and the ready synthetic access thereto, provide unprecedented opportunities for structure-activity relationship (SAR), lead-optimization and antimalarial drug development.

Inventors:
Michael R. Boyd (NCI) et al.

Patent Status:
DHHS Reference No. E-090-1994/0-US-01, issued as U.S. Patent 5,639,761 on 17 Jun 1997
DHHS Reference No. E-090-1994/0-US-07, issued as U.S. Patent 6,627,641 on 30 Sep 2003
DHHS Reference No. E-200-1994/0-US-01, issued as U.S. Patent 5,552,550 on 03 Sep 1996
DHHS Reference No. E-200-1994/0-US-02, issued as U.S. Patent 5,763,613 on 09 Jun 1998
DHHS Reference No. E-200-1994/2-US-01, issued as U.S. Patent 6,140,339 on 31 Oct 2000
DHHS Reference No. E-200-1994/2-US-08, issued as U.S. Patent 6,331,630 on 18 Dec 2001
DHHS Reference No. E-201-1994/0-US-01, issued as U.S. Patent 5,571,919 on 05 Nov 1996
DHHS Reference No. E-201-1994/1-US-01, issued as U.S. Patent 5,578,729 on 26 Nov 1996
DHHS Reference No. E-201-1994/0-US-02, issued as U.S. Patent 5,789,594 on 04 Aug 1998
DHHS Reference No. E-201-1994/1-US-03, issued as U.S. Patent 5,786,482 on 28 Jul 1998

Relevant Publication:

The technology is further described in the following publications: J. Nat Prod. 1997 Jul.;60(7):677-83 and Bioorg. Med. Chem. Lett. 1998 Jul.;8(13): 1729-34.

Portfolios:
Infectious Diseases

Infectious Diseases -Therapeutics-Anti-Parasitic
Infectious Diseases -Therapeutics


For Additional Information Please Contact:
RC Tang JD, LLM
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/435-5031
Email: tangrc@mail.nih.gov
Fax: 301/402-0220

Web Ref: 219

Last Updated On: 11/03


 
 
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