欧盟法规
C&L通报专利信息
专利号:US-7605241-B2
优先权日:2005-01-10
标题 :Synthesis of inhibitors of p90Rsk
发明人:HECHT SIDNEY M; MALONEY DAVID J
权利人:UNIV VIRGINIA
摘要:The synthesis of the naturally occurring kaempferol glycoside SLO1O1-1, as well as analogs thereof, has been accomplished, as has its biochemical evaluation. SLO1O1-1 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthetic scheme of the invention verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.
专利号:US-2016207894-A1
优先权日:2013-10-17
标 题:Synthesis of Diacids, Dialdehydes, or Diamines from THF-Diols
发明人:STENSRUD KENNETH
权利人:ARCHER DANIELS MIDLAND CO
摘要:A simple and elegant chemical process for the synthesis of oxygenated products, such as acids and aldehydes, or other derivative products, such as amines and nitriles, of cyclic bifunctional molecules made from renewable, bio-based sources such as HMF and/or its reduction product, 2,5-bis(hydroxymethyl)-tetrahydrofuran (bHMTHF) is described. In general, the process involves: a) generating a tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) from bHMTHFs using a sulfonate; b) displacing nucleophilically at least a sulfonate leaving group from the tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) to form a THF-dinitrile; and either c) oxidizing the THF-dinitrile with an acid having a pKa of ≦0 to generate a di-acid, or d) reducing partially the THF-dinitrile to generate a di-aldehyde, or e) reducing fully the THF-dinitrile to generate a di-amine.
专利号:US-9487537-B2
优先权日:2013-06-12
标 题:Synthesis of isohexide dicarbamates and derivatives thereof
发明人:STENSRUD KENNETH
权利人:ARCHER DANIELS MIDLAND CO; ARCHER DANIELS MIDLAND CO
摘要:Dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The dicarbamates of HMF-reduction products can serve as precursor materials from which various derivative compounds can be synthesized.
专利号:US-4061685-A
优先权日:1975-02-07
标题 :Catalytic synthesis of phenols
发明人:WEIGERT FRANK JULIAN
权利人:DU PONT
摘要:A phenol is produced by heating water and a cyclic or acyclic alkane or alkene of 6-10 carbon atoms at a temperature of 350 DEG to 700 DEG C in the presence of a metal oxide catalyst. Exemplary is the heating of water and cyclohexane in a nitrogen atmosphere and in the presence of ZnO/TiO2 to produce phenol.
专利号:US-9399653-B2
优先权日:2010-03-03
标 题 :Methods and systems for preparing irreversible inhibitors of protein tyrosine phosphatases
发明人:CAIRO CHRISTOPHER WARREN; TULSI NARESH SINGH; DOWNEY ALAN MICHAEL
权利人:CAIRO CHRISTOPHER WARREN; TULSI NARESH SINGH; DOWNEY ALAN MICHAEL; UNIV ALBERTA
摘要:Described herein are the preparation and use of novel bromo-phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples.
专利号:US-8022235-B2
优先权日:2007-06-01
标 题 :Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use
发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC
权利人:CELLECTAR INC
摘要:The present invention discloses boronic acids and esters of phospholipid ether analogs and methods for their synthesis and use. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells.