PATENT ASSIGNMENT
QUARTERLY FOR THE PERIOD THROUGH DECEMBER 31, 2009
Patents
The following assignments on behalf of the Board of Trustees of the University of
Kentucky Research Foundation have been executed:
1. U.S. Patent Application Serial Number: (to be assigned)
Filed: October 6, 2009
Title: "Enantioselective Synthesis of (+) and (-)-2-[1-(2,6-Dichlorophenoxy)-
Ethyl]- 1,3-Diazacyclopent-2- Ene”
Inventors: Drs. Peter A. Crooks and Ashish Pramod Vartak (Pharmaceutical
Sciences)
Technical Description: This invention relates to a method for the
enantioselective synthesis of (+) and (-) lofexidine or 2-[1-(2,6)-
dichlorophenoxy)-ethyl]-1,3-diazacylopent-2-ene.
Summary: Lofexidine is used to treat a variety of disorders, including
hypertension and opiate withdrawal. Current fonnulations of lofexidine include a
mixture ofthe mirror image molecules of lofexidine, (+)-lofexidine and (-)-
lofexidine. While (+)-lofexidine is much more effective at treating hypertension,
a mixture has been used because creating pure (+)-lofexidine has been too
expensive. The inventors have invented a method of selectively synthesizing
highly purified (+)-lofexidine [or (-)-lofexidine] that is much less expensive than
current methods of synthesis, opening the possibility of using these purified fonns
clinically.
2. U.S. Patent Application Serial Number: (to be assigned)
Filed: October 9, 2009
Title: "Use of Tris-Quaternary Ammonium Salts As Pain-Modulating Agents”
Inventors: Drs. Joseph R. Holtman (Anesthesiology), Peter A. Crooks, Linda P.
Dwoskin and J. Michael McIntosh (Phannaceutical Sciences)
Teclmical Description: This invention relates to the use of tris-quaternary
ammonium salts for pain modulation.
Summary: Pain management is a critical health issue. The financial loss due to
pain has been estimated at $100 billion per year as a result of medical fees,
decreased productivity, litigation, and the cost of drugs. Current drugs used to
treat pain are either only moderately effective or are highly addictive. The
inventors have developed a novel class of drugs that have been shown to decrease
pain in laboratory animals and that may provide more effective pain relief without
being addictive.