专利号:US-8067465-B2 优先权日:2002-01-15 标题:Tricyclic-bis-enone derivatives and methods of use thereof 发明人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO 权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE 摘要: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.
专利号:US-8772301-B2 优先权日:2009-12-18 标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof 发明人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D 权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-8067394-B2 优先权日:2006-11-17 标 题:Synthesis and biological activities of new tricyclic-bis-enones (TBEs) 发明人:HONDA TADASHI; SUNDARARAJAN CHITRA; GRIBBLE GORDON W; SPORN MICHAEL B; LIBY KAREN T 权利人:HONDA TADASHI; SUNDARARAJAN CHITRA; GRIBBLE GORDON W; SPORN MICHAEL B; LIBY KAREN T; DARTMOUTH COLLEGE 摘要:This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-γ, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
专利号:WO-0214257-A2 优先权日:2000-08-11 标题 :SYNTHESIS OF Α,Ω-DIESTERS
专利号:WO-2014151181-A1 优先权日:2013-03-15 标题 :A novel method for synthesizing tbe-31 发明人:HONDA TADASHI; SAITO AKIRA; ZHENG SUQING 权利人:UNIV NEW YORK STATE RES FOUND 摘要:A process for the synthesis of (±)-(4bS,8aR,10aS)-10a-ethynyl-4b,8,8-trimethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarbonitrile ('TBE-31'), which is useful for the treatment of various diseases and disorder in mammals. (±)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; (±)-8a-(Hydroxymethyl)-1,4a-dimethyl-4,4a,6,7,8,8a,9,10-octahydrophenanthren-2(3H)-one; (±)-(2R,4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; (±)-(2S,4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-2,3,4,4a,6,7,8,8a,9,10-decahydrophenanthren-2-ol; and (±)-(4aS,8aS)-8a-(Hydroxymethyl)-1,4a-dimethyl-4,4a,6,7,8,8a,9,10-octahydrophenanthren-2(3H)-one (4).
专利号:US-2009137557-A1 优先权日:2005-11-22 标题 :Calcilytic Compounds 发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.