Patent Number: 7,465,720

Title: Proteasome inhibiting .beta.-lactam compounds

Abstract: Disclosed is a total synthesis of a biologically active .beta.-Lactam--Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. ##STR00001## Also disclosed are proteasome inhibiting compounds having the formula: ##STR00002## wherein: R.sub.1 is a cyclolower alkyl group; or R.sub.1 is a lower alkyl group; and R.sub.2 is either hydrogen or a lower alkyl group; R.sub.3 is either hydrogen or a lower alkyl group; R.sub.4 a halo-lower alkyl group; and R.sub.5 is either hydrogen or a lower alkyl group.

Inventors: Corey; Elias J. (Cambridge, MA), Hogan; Philip C. (St. John's, CA)

Assignee: President and Fellows of Harvard College

International Classification: C07D 487/04 (20060101); A61K 31/407 (20060101); C07D 263/26 (20060101); C07D 487/10 (20060101); C07F 7/10 (20060101); C07D 405/04 (20060101)

Expiration Date: 2021-12-16 0:00:00