专利号:US-2003180804-A1 优先权日:2001-10-29 标题:Solid phase synthesis of chemical libraries 发明人:PRYOR KENT E; LEWIS RONALD D; BROWN JASON W 权利人:CORVAS INT INC 摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.
专利号:US-6358928-B1 优先权日:1999-11-22 标 题 :Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases 发明人:RASNICK DAVID W 权利人:ENZYME SYSTEMS PRODUCTS 摘要:Novel alpha-amino and peptidyl sulfonyl imidazolides, a method for their synthesis, and a method for inhibiting serine proteases therewith are disclosed. Pharmaceutical compositions containing alpha-amino and peptidyl sulfonyl imidazolides and their use in the treatment of disease states characterized by an over-activity of serine proteases are also disclosed. Novel synthetic methods for the synthesis of sulfonyl derivatives, particularly alpha-amino and peptidyl sulfonyl derivatives, from thioic acid S-esters are also disclosed.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:RU-2118313-C1 优先权日:1997-05-06 标 题 :Method of synthesis of 1-(1-aminoethyl)-adamantane hydrochloride
专利号:WO-9918065-A1 优先权日:1997-10-03 标 题:Chiral amines 发明人:JOHNSON NICHOLAS BERNARD; BURK MARK JOSEPH; CASY GUY 权利人:CHIROTECH TECHNOLOGY LTD 摘要:An efficient synthesis of chiral amines (5) comprises preparing an enamide (4) from the oxime (2), and subjecting the enamide to catalytic asymmetric hydrogenation.
专利号:US-9150511-B2 优先权日:2011-05-24 标题 :Process for preparing saxagliptin and its novel intermediates useful in the synthesis thereof 发明人:KOVI RAVISHANKER; RAPOLE KESHAVRAO; NAIK ASHISH; KANNAPAN JAYARAMAN; MADALA MURALIKRISHNA; THAKOR SANJAY 权利人:APICORE US LLC 摘要:Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.