<A> ArQule, Inc. Granted U.S. Patent for Aminimide Biological Mimetic
MEDFORD, Mass. -- ArQule, Inc. (Nasdaq: ARQL) today announced that it has received from the U.S. Patent and Trademark Office, Patent No. 5,705,585, entitled "Aminimide-Containing Molecules and Materials as Molecular Recognition Agents," broadly covering aminimide-containing molecules that can potentially serve as mimetics of peptides, nucleotides, polysaccharides and lipids. This patent provides ArQule with fundamental patent coverage to apply its technologies to the design and development of a new family of compounds that can imitate the biological activity of major types of biological molecules.
"While the potency and specificity of naturally-occurring peptides makes them very desirable as binding ligands, in general they lack the pharmacological properties that make good drugs. For example, peptides have short half lives and must be administered intravenously, which are major drawbacks. With this new chemistry, we can create unique molecules that function like peptides, with the potential for incorporating improved pharmacological properties such as oral bioavailability," said Joseph C. Hogan Jr., Ph.D., Chairman, CSO and Senior Vice President of Research of ArQule, Inc. and the author of the patent.
One way to develop a pharmaceutical product is to identify the naturally occurring peptide that an enzyme binds to and acts upon, and then present its chemical mimic to the enzyme to block the enzyme's action. Such an approach was demonstrated by Dr. Hogan and ArQule scientists together with a scientific team at Brandeis University, published in Science, July 1995, in which they designed a peptide mimetic aminimide molecule that inhibited elastase, and bound to the active site of the enzyme in the same manner as the template peptide.
This chemistry enables the Company's chemists to utilize aminimides to form a "scaffold" which closely resembles the amino acid chain of a peptide. This capability is particularly timely in the drug discovery industry, since many scientists are currently applying phage display and other technologies to discover peptides with desirable biological activity. Once such peptides are identified, the ArQule chemistry can be applied to design molecules that imitate their biological activity, with improved pharmaceutical profiles. In addition, aminimide chemistry can also be applied to produce mimetics of polynucleotides, polysaccharides and lipids.
Eric B. Gordon, ArQule's President and Chief Executive Officer, added: "ArQule's business strategy is to help the pharmaceutical industry fill its pipeline with new IND candidates, and this new technology will provide yet another method of designing pharmaceutical compounds rapidly and effectively. We look forward to providing this capability to our many collaborators as an important new component of their drug discovery programs. We have developed and will continue to develop many such novel and proprietary chemistries to sustain our leadership, and will continue to protect them through both patent coverage and trade secret strategies."
ArQule, Inc. is a leading chemistry company in accelerated drug discovery using its proprietary high throughput lead generation and lead optimization technologies. ArQule provides new pathways to product discovery by integrating five core technologies -- modular building block technology, structure-guided design, high speed parallel chemical synthesis, information technology and an Automated Molecular Assembly Plant (AMAP(TM)) parallel synthesis system to accelerate the identification and optimization of drug and product development candidates in the pharmaceutical, biotechnology, and agrochemical industries. ArQule is based in Medford, Massachusetts.
Statements in this press release that are not strictly historical are "forward looking" statements as defined in the Private Securities Litigation Reform Act of 1995. The actual results may differ from those projected in the forward looking statement due to risks and uncertainties that exist in the Company's operations and business environment, described more fully in the Company's Form 10-K for the year ended December 31, 1996 and the Registration Statement of Form S-1 dated April 4, 1997, filed with the Securities and Exchange Commission.
/CONTACT: Eric B. Gordon, President and CEO of ArQule, 781-395-4100,
arqule.com or Investor Relations, Marcia A. Kean of Feinstein Kean Partners, 617-577-8110/
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