专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-11613514-B2 优先权日:2016-03-25 标题:Crystal forms and methods of synthesis of (2R, 6R)-hydroxynorketamine and (2S, 6S)-hydroxynorketamine 发明人:THOMAS CRAIG; ZARATE CARLOS; MOADDEL RUIN; GOULD TODD; ZANOS PANOS; MORRIS PATRICK 权利人:US HEALTH; UNIV MARYLAND 摘要:The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts.
专利号:US-8846614-B2 优先权日:2011-08-25 标 题 :Process for the synthesis of 37-mer peptide pramlintide 发明人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL 权利人:MOHE NIKHIL UMESH; CHAVRE PRAFUL SHAMRAO; DESHMUKH BHARTI PRABHAKARRAO; MURALIDHARAN CHANDRAKESAN; LOBO LESTER JOHN; PAWAR DIGAMBER SHRIPATI; SAKSENA DIVYA LAL; USV LTD 摘要:A process for the production of pramlintide, a 37-mer peptide, is provided. The synthesis provides a high yield synthesis of the peptide in relatively pure form. Further purification can be achieved by preparative HPLC.
专利号:US-2007122842-A1 优先权日:2005-11-30 标题 :Massively parallel synthesis of proteinaceous biomolecules 发明人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 权利人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 摘要:Methods for fabricating dense arrays of polymeric molecules in a highly multiplexed manner are provided using semiconductor-processing-derived lithographic methods. Advantageously, the methods are adaptable to the synthesis of a variety of polymeric compounds. For example, arrays of peptides and polymers joined by peptide bonds may be fabricated in a highly multiplexed manner.
专利号:US-4242256-A 优先权日:1977-03-15 标 题 :Synthesis of peptide analogues 发明人:SHARPE ROBERT; SZELKE MICHAEL 权利人:SHARPE ROBERT; SZELKE MICHAEL 摘要:Compounds being analogues of a dipeptide in which the nitrogen atom of the linking amide group of the dipeptide is replaced by trivalent group ##STR1## and in which, optionally, the carbonyl function of this linking group is replaced by the divalent group --CH 2 -- are of value in the synthesis of isosterically modified peptides.
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