5-Substituted Derivatives of Conformationally Locked Nucleoside Analogues
Description of Invention:
This invention relates to 5-substituted derivatives of conformationally locked nucleoside analogues and methods of using these derivatives as antiviral and anticancer agents. The compounds contemplated by the invention are nucleoside analogues where the 5-substituent is a halogen, alkyl, alkene, halovinyl or alkyne group, and the nucleotide base is cytosine or uracil. The analogues are particularly effective in treating viral infections, specifically infections of DNA viruses such as Herpes simplex virus (HSV), Varicella zoster virus (VSV), Epstein Barr virus (EBV), and Cytomegalovirus (CMV) as well as members of the Poxviridae family. The inventors have demonstrated in plaque reduction assays that 5-substituted uracils (bromo, iodo, and bromovinyl) attached to a bicyclo[3.1.0]hexane template are thirty times more potent than acyclovir against HSV-1 and HSV-2.
Inventors:
Victor Marquez and Pamela Russ (NCI)
Patent Status:
DHHS Reference No. E-249-2000/0 --
U.S. Provisional Application No. 60/220,934 filed 26 Jul 2000
PCT Application No. PCT/US01/23246 filed 24 Jul 2001, which published as WO 02/08204 on 31 Jan 2002
U.S. Patent Application No. 10/346,762 filed 15 Jan 2003 Licensing Status:
Limited field(s) of use may be available
For Additional Information Please Contact: Robert M. Joynes J.D.
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
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Phone: (301)594-6565
Email: joynesr@mail.nih.gov
Fax: (301) 402-0220
