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-4665074-A 优先权日:1984-05-10 标 题:6-(polyfluoroalkoxyphenyl) pyridazinones, their compositions, synthesis and use 发明人:AMSCHLER HERMANN 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:6-aryl-3[2H]pyridazinones of formula I (I) in which one of the substituents R1 and R2 denotes hydrogen or (C1-C4)-alkoxy, and the other denotes polyfluoro-(C1-C4)-alkoxy, and their pharmacologically-tolerated salts are suitable as bronchospasmolytic and cardiotonic active compounds. Processes for their preparation and appropriate medicaments are indicated.
专利号:US-2006211603-A1 优先权日:2004-08-18 标 题:Ramoplanin derivatives possessing antibacterial activity 发明人:RAJU BORE G; CIABATTI ROMEO; MAFFIOLI SONIA I; SINGH UPINDER; ROMANO GABRIELLA; MICHELUCCI ELENA; TISENI PAOLO S; CANDIANI GIANPAOLO; KIM BUM; O'DOWD HARDWIN 权利人:VICURON PHARM INC 摘要:Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.
专利号:US-2013203709-A1 优先权日:2010-08-09 标 题 :Acylsulfonamides and processes for producing the same 发明人:MANETSCH ROMAN; KULKARNI SAMEER; IYAMU IREDIA D; WANG HONG-GANG; DOI KENICHIRO; GUIDA WAYNE; SANTIAGO DANIEL; DU BOULAY COURTNEY 权利人:MANETSCH ROMAN; KULKARNI SAMEER; IYAMU IREDIA D; WANG HONG-GANG; DOI KENICHIRO; GUIDA WAYNE; SANTIAGO DANIEL; DU BOULAY COURTNEY; PENN STATE RES FOUND; UNIV SOUTH FLORIDA 摘要:The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
专利号:US-8524947-B2 优先权日:2008-02-22 标题 :Acylsulfonamides and processes for producing the same 发明人:WANG HONG-GANG; MANETSCH ROMAN; HU XIANGDONG; KULKARNI SAMEER; SUN JIAZHI 权利人:WANG HONG-GANG; MANETSCH ROMAN; HU XIANGDONG; KULKARNI SAMEER; SUN JIAZHI; UNIV SOUTH FLORIDA; H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
[参考文献]: A W Nicholls, Et Al. Nmr Spectroscopic And Theoretical Chemistry Studies On The Internal Acyl Migration Reactions Of The 1-O-Acyl-Beta-D-Glucopyranuronate Conjugates Of 2-, 3-, And 4-(Trifluoromethyl) Benzoic Acids. Chem Res Toxicol. 1996 Dec;9(8):1414-24.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要:Yerien, D. E.; Barata-Vallejo, S.; Postigo, A., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 9.