Hydrolytic enzyme inhibitors and substrates and assays,...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/10 (2006.01) A61K 31/685 (2006.01) C12Q 1/34 (2006.01)

Patent

CA 2064793

The present invention provides novel hydrolytic enzyme inhibitors (inactivators) and substrates that have three functional parts: 1) a moiety that is specifically cleavable upon contact of the compound with a specific hydrolytic enzyme which moiety when cleaved is detectable and measurable, 2) a moiety that is recongnized by a specific hydrolytic enzyme and which interacts therewith and the substrate is specifically cleavable upon such interaction and 3) a linker moiety linking moieties 1) and 2). These novel compounds are useful in assays to detect and mesure levels of hydrolytic enzyme activity and are also useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phopholipases, lipases, esterases, proteases, etc.

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