Patent Number: 8,067,465

Title: Tricyclic-bis-enone derivatives and methods of use thereof

Abstract: Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.

Inventors: Honda; Tadashi (Hanover, NH), Favaloro; Frank G. (Norfolk, MA), Gribble; Gordon W. (Lebanon, NH), Sporn; Michael B. (Tunbridge, VT), Suh; Nanjoo (White River Junction, VT)

Assignee: The Trustees of Dartmouth College

International Classification: A61K 31/275 (20060101); C07C 255/47 (20060101)

Expiration Date: 2020-11-29 0:00:00