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Novel Antimalarial Compounds, Methods of Synthesis Thereof, Pharmaceutical Compositions Comprising Same, and Methods of Using Sa

Posted Jun 14 2010 5:00pm

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.

Michael R Boyd (NCI)

Patent Status:
HHS, Reference No. E-090-1994/0
US, , Patent No. 5,639,761, Issued 17 Jun 1997
US, , Patent No. 5,571,919, Issued 05 Nov 1996
US, , Patent No. 5,578,729, Issued 26 Nov 1996
US, , Patent No. 5,789,594, Issued 04 Aug 1998
US, , Patent No. 5,786,482, Issued 28 Jul 1998
US, , Patent No. 6,627,641, Issued 30 Sep 2003
HHS, Reference No. E-090-1994/0
HHS, Reference No. E-201-1994/0
HHS, Reference No. E-201-1994/1
HHS, Reference No. E-200-1994/0
HHS, Reference No. E-200-1994/2
PCT, Application No. PCT/US98/27407 filed 23 Dec 1998
PCT, Application No. PCT/US95/01717 filed 13 Feb 1995

Relevant Publication:
  1. 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.

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

For Additional Information Please Contact:
Admin. Licensing Spec-InfectDis
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-496-7057
Fax: 301-402-0220

Ref No: 219

Updated: 06/2010

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