专利号:US-11746364-B2 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains 发明人:PLUSKAL TOMÃ?S; Weng jing-ke 权利人:WHITEHEAD INST BIOMEDICAL RES 摘要:Disclosed are methods, compositions, proteins, nucleic acids, cells, vectors, compounds, reagents, and systems for the preparation of kavalactones, flavokavains, and kavalactone and flavokavain biosynthetic intermediates using enzymes expressed in heterologous host cells, such as microorganisms or plants, or using in vitro enzymatic reactions. This invention also provides for the expression of the enzymes by recombinant cell lines and vectors. Furthermore, the enzymes can be components of constructs such as fusion proteins. The kavalactones produced can be utilized to treat anxiety disorder, insomnia, and other psychological and neurological disorders. The flavokavains produced can be utilized to treat various cancers including colon, bladder, and breast cancers.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-2019271015-A1 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains
专利号:US-10941429-B2 优先权日:2018-01-17 标 题:Enzymatic synthesis of kavalactones and flavokavains
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
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.
参考标题:Design And Synthesis Of Low Molecular Weight Compounds With Complement Inhibition Activity 作者:Hoshang E. Master,Shabana I. Khan,Krishna A. Poojari |发布日期:2005.8 摘要:An Attempt Was Made To Synthesize A Series Of Non-Cytotoxic Low Molecular Weight Compounds Of Varying Substitutions And Functionalities Having Pharmacophore Activity Like Carbonyl Compounds, Carboxylic Acid And Bioisosteres Like Tetrazole And Phenyl Acrylic Acid. The In Vitro Assay Of These Analogues For The Inhibition Of Complement Activity Revealed Significant Inhibitory Activity For Varying Substituents
合成参考文献
摘要:I. Hsu and L. F. Koons, J. Indian Chem. Soc. 44, 540 (1967).