Aminoalkyl Substituted O6-Benzylguanine Derivatives as Inactivators of O6-Alkylguanine-DNA Alkyltransferase and Adjuvants for Chemotherapy
Description of Invention:
This present invention describes novel class of compounds that inactivate the DNA repair protein O6-alkylguanine-DNA alkyltransferase (AGT). Inactivation of this protein improves therapeutic effectiveness of chemotherapy drugs that modify O6-position of DNA guanine residues.
These new compounds have several advantages over the existing O6-benzylguanine compounds in terms of being more water soluble, being more potent, and the compounds are more readily formulated in water or phosphate buffered saline solutions than O6-benzylguanine compounds.
The existing O6-benzylguanine compounds are currently in Phase II and III clinical trials. The new aminoalkyl substituted O6-benzylguanine derivatives are currently in preclinical trials.
Applications and Modality:
New compounds have potential to improve chemotherapy treatment with anticancer agents.
New compounds are more water soluble, more readily formulated and more potent than existing O6-benzylguanine compounds.
Market:
600,000 deaths from cancer related diseases were estimated in 2006.
In 2006, cancer drug sales were estimated to be $25 billion.
Development Status:
The technology is currently in the pre-clinical stage of development.
Patent Status:
DHHS Reference No. E-307-2004/1 --
U.S. Patent Application No. 11/683,310 filed 07 Mar 2007
Relevant Publication: A manuscript directly related to the above technology will be available as soon as it is accepted for publication.
Licensing Status: Available for exclusive and non-exclusive licensing.
Portfolios: Cancer
Cancer -Therapeutics-Conventional Chemotherapy-Antimetabolites Cancer -Therapeutics-Conventional Chemotherapy-Other Cancer -Therapeutics Cancer -Research Materials
For Additional Information Please Contact: Adaku Nwachukwu J.D.
NIH Office of Technology Transfer
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Rockville, MD 20852-3804
Phone: 301 435-5560
Email: madua@mail.nih.gov
Fax: 301 402-0220