Novel Non-Nucleoside Agents for the Inhibition of HIV Reverse Transcriptase for the Treatment of HIV-1
Description of Invention:
Despite recent developments in drug and compound design to combat the human immunodeficiency virus (HIV), there remains a need for a potent, non-toxic compound that is effective against wild type reverse transcriptase (RT) as well as RTs that have undergone mutations and thereby become refractory to commonly used anti-HIV compounds. There are two major classes of RT inhibitors. The first comprises nucleoside analogues, which are not specific for HIV-RT and are incorporated into cellular DNA by host DNA polymerases. Nucleoside analogues can cause serious side effects and have resulted in the emergence of drug resistance viral strains that contain mutations in their RT. The second major class of RT inhibitors comprises non-nucleoside RT inhibitors (NNRTIs) that do not act as DNA chain terminators and are highly specific for HIV-RT. This technology is a novel class of NNRTIs (substituted benzimidazoles) effective in the inhibition of HIV-RT wild type as well as against variant HIV strains resistant to many non-nucleoside inhibitors. These NNRTIs are highly specific for HIV-1 RT and do not inhibit normal cellular polymerases, resulting in lower cytotoxicity and fewer side effects that the nucleoside analogues, such AZT. This novel class of compounds could significantly improve the treatment of HIV by increasing compliance with therapy.
Inventors:
Christopher A. Michejda (NCI) Marshall Morningstar (NCI) Thomas Roth (NCI)
Patent Status:
DHHS Reference No. E-076-1997/1 --
U.S. Patent 6,369,235 issued 09 Apr 2002
U.S. Patent 6,894,068 issued 17 May 2005
For Additional Information Please Contact: Sally Hu PhD MBA
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: (301) 435-5606
Email: hus@mail.nih.gov
Fax: (301) 402-0220
