专利号:US-7390801-B2 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries
专利号:US-2005009151-A1 优先权日:2003-07-10 标 题 :Methods for the stereospecific and enantiomeric enrichment of beta-amino acids 发明人:CHASE MATTHEW; CLAYTON ROBERT; LANDIS BRYAN; BANERJEE AMIT 权利人:PHARMACIA CORP 摘要:The present invention relates to methods for the stereospecific synthesis and for the enantiomeric enrichment of β-amino acids. A novel D-β-aminotransferase, which exhibits stereoselectivity for D-β-phenylalanine, (D-3 amino-3-phenylpropinine acid) was purified from a newly-isolated strain of Variouorax paradoxus . A novel L-β-aminotransferase was purified from a newly-isolated strain of Alcaligenes eutrophus . The D- and L-β-aminotransferases can be used to facilitate the stereoselective biosynthesis of β-D-phenylalanine or β-L-phenylalanine, from a mixture of L-glutamic acid or L-alanine, respectively, and 3-keto-3-phenylpropionic acid in the presence of the cofactor pyridoxal phosphate.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:US-7153847-B2 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
专利号:US-2005215541-A1 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
[参考文献]: Holger Bühler, Et Al. Inversion Of Stereoselectivity By Applying Mutants Of The Hydroxynitrile Lyase From Manihot Esculenta. Chembiochem. 2005 Apr;6(4):711-7.
合成参考文献
摘要:Maison, W., Science of Synthesis Knowledge Updates, (2020) 1, 407.