Yale Grants Exclusive License to ArQule Inc. for Chemical Method Of Creating Drugs that Could Help Fight AIDS, Emphysema

The Yale Office of Cooperative Research – OCR– and ArQule Inc. of Medford, Massachusetts, announced today that Yale University has granted the company an exclusive license for the development of patent-pending discoveries made by Harry Wasserman, the Eugene Higgins Professor Emeritus of Chemistry at Yale, and his former post doctoral associate, Wen-Bin Ho. The discoveries could help the company develop drugs for treating a wide-range of disorders, including cardiovascular diseases, emphysema, AIDS and Alzheimer’s disease.

The Yale chemists’ methods make it possible to rapidly and efficiently synthesize alpha-ketoamide-based compounds, which research has shown can block or inhibit key enzymes called proteases. Most AIDS medications now in clinical trials or entering the market are classified as protease inhibitors. As part of the agreement, ArQule also will support continued research in Professor Wasserman’s laboratory.

“We are very excited about this opportunity to work with ArQule on promising new pharmaceuticals,” said Dr. Gregory E. Gardiner, a former director of research and development for Pfizer Inc., who recently became director of Yale’s expanded OCR office. “Dr. Wasserman’s discovery complements one of ArQule’s core technologies, which is based on a series of organic molecules that form a molecular scaffold to which functional elements can be attached. This enables the company to generate a large number of chemical compounds with varied structures as scientists search for the most effective drugs against a particular disease.”

This agreement is an example of how Yale’s efforts to bring its research discoveries to the marketplace are generating solid results for the University and for the public, said Dr. Gardiner, adding that Yale has negotiated more than 200 license agreements since the OCR was founded in 1982. During that same period, Yale earned $15 million in royalties from numerous U.S. and foreign patents and from technology licenses.

Among Yale’s major discoveries are an AIDS medication called ZeritTM –d4T– recently launched by Bristol Myers Squibb, and a Lyme disease vaccine now in clinical trials for humans by SmithKline Beecham and for animals by Pfizer. Yale has a large program in antiviral research directed at hepatitis and has made important contributions to biotechnology in the areas of ribozymes and gene sequencing, Dr. Gardiner said.

Yale’s scientists also made the fundamental discovery in electrospray mass spectrometry, which allows the accurate measurement of the molecular weight of macromolecules. In addition to work in life sciences, Yale is developing important inventions in semiconductor chip fabrication and fiber optics. Overall, the value of public companies founded on inventions by Yale scientists is about $750 million.

“Yale’s highly promising technology will enhance our ability to discover and optimize small molecule compounds that mimic the specific and potent activity of certain protease inhibitors,” said David L. Coffen, Ph.D., vice president of chemistry at ArQule. “The alpha-ketoamide chemistry readily integrates into ArQule’s Chemistry Operating System, a molecular building-block system for the high- speed, parallel synthesis of pure, well-characterized small molecule organic compounds.”

ArQule’s drug discovery programs involve collaborations with major pharmaceutical companies, biotechnology companies and academic researchers, including Abbott Laboratories, Solvay Duphar and Pharmacia Biotech.

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