Methods for solid-phase synthesis of hydroxylamine compounds and derivatives, and combinatorial libraries thereof
AssigneeVersicor, Inc.
InventorsDinesh V. Patel, Khehyong Ngu
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Abstract
A novel method for generating hydroxylamine, hydroxamic acid, hydroxyurea, and hydroxylsulfonamide compounds is disclosed. The method involves the nucleophilic attack of an alkoxyamine on a suitable solid phase support. Techniques of combinatorial chemistry can then be applied to the immobilized alkoxyamine to generate a diverse set of compounds. Cleavage of the compounds from the support yields a library of hydroxylamine or hydroxylamine derivative compounds, which can be screened for biological activity (e.g., inhibition of metalloproteinases).
Claims27
A method of inhibiting a deformylase enzyme, comprising administration of one or more compounds selected from the group consisting of
- wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, alkyl, heteroalkyl, aryl, heteroaryl, and heterocyclic moieties and naturally and non-naturally occurring amino acid side chains;
- or a stereoisomer, protected derivative, or salt thereof.
Dependencies are inferred from the claim text.