Patent Evaluation: Pyrrolidinones as Aggregation Inhibitors

Summary

Novelty: Novel cyclic imino derivatives are disclosed as aggregation inhibitors. The compounds are potentially useful for inhibiting bone resorption, as antithrombotic and anti-aggregation agents, and as tumour metastasis inhibitors.

Biology: Fibrinogen-binding and platelet aggregation inhibition assays were used to evaluate the compounds. In these assays, the specified compound showed an IC₅₀ = 0.032 μM for fibrinogen binding and EC₅₀ = 0.9 μM for platelet aggregation.

Chemistry: Over ninety syntheses are described in detail and well over three hundred compounds are exemplified. (3S,5S)-5((4′-amidino-4-biphenylyl)oxymethyl)-3-carboxy-methyl-1-(3-phenylpropyl)-2-pyrrolidinone is one of twenty-two specifically claimed compounds.

Structure: