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Quinoline Inhibitors of Retroviral Integrase

Description of Invention:
The subject invention describes certain diketo quinolin-4-1 derivatives and their use as integrase inhibitors in the treatment of HIV infection. The results of in vitro integrase inhibition studies show that these derivatives have significant anti-integrase activity (e.g., an IC50 for strand transfer inhibition of not greater than 2 µM). Thus, these derivatives might be potentially important lead compounds for the development of integrase inhibitors. Since HIV integrase is an essential enzyme for effective viral replication, the development of such inhibitors of HIV integrase would thus potentially be useful and effective in the treatment of HIV infection.

Inventors:
Yves Pommier et al. (NCI)

Patent Status:
DHHS Reference No. E-187-2003/0 --
U.S. Provisional Application No. 60/552,423 filed 10 Mar 2004
PCT Application No. PCT/US2005/08202 filed 09 Mar 2005, which published as WO 2005/087759 on 22 Sep 2005
U.S. Patent Application No. 10/591,679 filed 01 Sep 2006

Portfolios:
Infectious Diseases

Infectious Diseases -Therapeutics-Anti-Viral-AIDS (only)
Infectious Diseases -Therapeutics


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


Web Ref: 933

Updated: 10/07

 

 
 
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