To: scaram(o)uche who wrote (726 ) 2/19/2002 12:33:34 AM From: scaram(o)uche Respond to of 1833 GPCR -- Directed Drug Discovery In August, 1999, OSI purchased certain assets of Cadus Pharmaceutical Corporation. In this acquisition, OSI acquired Cadus' drug discovery programs focused on G-protein coupled receptors or GPCRs. These receptors are one of the most important families of targets for drug discovery in the pharmaceutical industry. Approximately, forty percent of the currently marketed pharmaceutical products target GPCRs. The acquired programs include Cadus' discovery program in adenosine receptors, an important family of GPCR's. These programs will form the core of OSI-owned and funded candidate development programs in the coming year. The improved understanding of the physiology, pharmacology and molecular biology of adenosine and adenosine receptors in recent years has provided a solid foundation for active research and development in this field. Currently, four adenosine receptor subtypes, A(1), A(2A) , A(2B) and A(3), have been characterized and R&D efforts have led to high quality proprietary lead compounds for each. Several adenosine receptor compounds are under development by OSI. Promising adenosine A(1) and adenosine A(2B) receptor targeted compounds will undergo evaluation as candidates for asthma, with the dual goals of identifying an IND-track candidate against both targets and simultaneously assessing and executing the best commercialization strategy. The A(1) compound is targeted for the treatment of the bronchoconstriction associated with the acute phase of an asthma attack while the A(2B) compound is directed toward blocking the inflammatory components produced by mast cells and associated with the longer term damage caused by the disease. OSI also has potent and selective A(2A) targeted compounds that have potential for development as both anti-angiogenesis agents and for the treatment of Parkinson's disease . Additionally, OSI has a selective adenosine A(3) targeted compound that is undergoing extensive evaluation in animal models for glaucoma. The targets of Parkinson's disease and glaucoma are examples of programs outside OSI's disease area focus and may be out-licensed or earlier partnered in the development process. In addition, an A(1) targeted compound, CDS-096370, has potential for use in the treatment of congestive heart failure and renal failure. This candidate has been licensed to Solvay for advanced pre-clinical and clinical development. Kyowa Hakko Has Obtained Encouraging Clinical Results in a New Approach To Treatment of Parkinson's Disease TOKYO, Feb. 18 /PRNewswire/ -- Kyowa Hakko, a leading Japanese research-based pharmaceutical and biotechnology company, has successfully completed two Phase 2A clinical trials in the United States which demonstrate potential for the treatment of Parkinson's disease for Kyowa Hakko's proprietary compound KW-6002. The details of these studies will be announced at the American Academy of Neurology (AAN) Conference in Denver this April. KW-6002 is a selective A2A antagonist that provides a unique and promising mechanism of action for the treatment of Parkinson's disease. It is confirmed that KW-6002, in either mono or combination therapy with levodopa or dopamine agonists, improves the symptoms of Parkinson's disease in an animal model (i.e. Parkinsonian monkey model) without increasing incident or severity of dopaminergic related side effects or inducing or worsening dyskinesia. "KW-6002 has potential as a new type of Parkinson's drug therapy that differs in mechanism from present dopamine related agents including levodopa, dopamine agonists and COMT inhibitors," says Tadashi Hirata, Ph.D., President and CEO of Kyowa Hakko. "We expect that KW-6002 will be an important contribution to the treatment and well-being of Parkinson's disease patients." Dr. Hirata continued, "we have submitted patent applications worldwide for use of this new class of drugs to treat Parkinson's disease." Currently, Kyowa Hakko is preparing for pivotal Phase IIb and Phase III trials in the United States and elsewhere in the world. Dr. Hirata added that the global development of KW-6002 for treating Parkinson's disease demonstrates Kyowa Hakko's commitment to develop innovative pharmaceutical products for the global marketplace and to maximize our Pharmaceuticals business and new technologies. About Kyowa Hakko Kyowa Hakko (http://www.kyowa.co.jp ), a leading Japanese research-based pharmaceutical and biotechnology company, is devoted to discovering, developing, manufacturing, and marketing quality pharmaceutical products and bio-chemicals such as amino acids. Six compounds including KW-6002 and KW-7158(an agent for treating urinary incontinence) as strategic themes are now under development overseas. Additionally, its pharmaceutical central research is focused on two therapeutic fields and drug discovery utilizing antibody-based technologies. Those therapeutic fields include cancer and allergies, where Kyowa Hakko has a strong background worldwide with products such as Mitomycin and Olopatadine. CONTACT: Ichiro Matsuura Manager, Corporate Communications Department Kyowa Hakko Kogyo Co., Ltd. TEL +81-3-3282-1903 FAX +81-3-3282-0990 E-mail pr@kyowa.co.jp URL kyowa.co.jp SOURCE Kyowa Hakko Kogyo Co., Ltd. Web Site: kyowa.co.jp