To: scaram(o)uche who wrote (434 ) 12/19/2000 11:39:52 AM From: scaram(o)uche Read Replies (1) | Respond to of 1833 continuing...... RESPIRATORY DISEASES In July 1999, we purchased certain assets from Cadus Pharmaceutical Corporation including a program focused on the adenosine receptor family. 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 research and development efforts have led to high quality proprietary lead compounds for each. The adenosine A(1) receptor is targeted for the treatment of the bronchioconstriction associated with the acute phase of an asthma attack, while the adenosine A(2B) receptor is believed to mediate the inflammatory components produced by mast cells and associated with the longer term damage caused by the disease. There are more than 17 million asthma sufferers in the United States alone, approximately 25% of whom are children. We are currently developing several sub-type specific inhibitors of the adenosine receptor family. OSIC-113760, an adenosine A(1) receptor inhibitor will undergo evaluation, with the goal of identifying a drug candidate to treat the acute phase of an asthma attack. Adenosine A(2B) receptor targeted compounds will undergo evaluation with the goal of identifying drug candidates to treat the longer term damage associated with chronic asthma. In addition to these adenosine receptor antagonists, we have discovered an inhibitor of the Interleukin-4, or IL-4, gene expression as part of our long term alliance with Aventis Pharmaceuticals Inc. in gene transcription drug discovery. The IL-4 gene mediates and sustains allergic asthmatic inflammatory responses. We have identified additional sub-type specific adenosine receptor inhibitors as a result of our asthma program. These include an adenosine A(2A) inhibitor for the treatment of Parkinson's disease, an adenosine A(3) inhibitor for the treatment of glaucoma and an adenosine A(1) receptor, CDS-096370, for the treatment of congestive heart failure. CDS-096370 has been licensed to Solvay Pharmaceuticals, B.V. for advanced pre-clinical and clinical development. (snip) Solvay Pharmaceuticals, B.V. With the acquisition of the assets of Cadus in July 1999, we assumed a collaborative research and license agreement effective as of November 1, 1995, which Cadus had with Solvay. The collaboration is directed toward GPCR drug discovery in differing fields of use. Our fields of use include cancer, asthma and inflammatory diseases. Solvay's fields of use include cardiovascular, central nervous system disorders and gastrointestinal diseases. In exchange for milestone and royalty payments, Solvay maintains sole responsibility for pre-clinical and clinical development as well as marketing and commercialization of any lead compound it discovers from its use of the screens developed as part of the collaboration. The term of the research program expires December 31, 2000, and we have elected not to continue collaboration with Solvay, but rather to focus our research in cancer in our proprietary programs.