Assay for evaluating inhibition of pmn elastase by...

C - Chemistry – Metallurgy – 12 – P

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C12P 21/08 (2006.01) A61K 39/385 (2006.01) C07C 275/24 (2006.01) C07C 275/28 (2006.01) C07C 275/40 (2006.01) C07D 307/54 (2006.01) C07D 307/79 (2006.01) C07K 16/44 (2006.01) C12Q 1/37 (2006.01) G01N 33/577 (2006.01) G01N 33/62 (2006.01)

Patent

CA 2076403

151/CCP69 18525 TITLE OF THE INVENTION ASSAY FOR EVALUATING INHIBITION OF PMN ELASTASE BY N-SUBSTITUTED AZETIDINONES ABSTRACT OF THE INVENTION N-substituted azetidinones are a class of inhibitors of human leukocytes elastase which are known to be useful in the treatment of a wide variety of antiinflammatory and antidegenerative diseases. In inhibiting elastase, the therapeutic agents are shown to form a characteristic stable complex with the enzyme. In the assay disclosed herein, the inhibitor-enzyme complex is advantageously hydrolyzed and specific product(s) of the hydrolysis are measured. The assays are useful in a clinical setting, for determining appropriate dosage and assessing the effectiveness of treatment.

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