专利号:US-8809526-B2 优先权日:2010-07-19 标题 :Synthesis of cyclopentaquinazolines 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT; ONYX PHARMA INC 摘要:A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N—{N-{4-[N-((6S)-2 -hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2 -ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801).
专利号:WO-9217496-A1 优先权日:1991-03-18 标题 :Isolation and sequence of the acetyl coa:deacetylcephalosporin acetyltransferase gene 发明人:MATHISON LORILEE; SOLIDAY CHARLES L; RAMBOSEK JOHN A 权利人:PANLABS INC 摘要:The invention relates to a DNA sequence with a nucleotide sequence encoding a polypeptide in a host cell having Cephalosporin C synthetase (DAC acetyltransferase) activity which is the last enzyme in the synthesis of cephalosporins. Embodiments of the invention relate to methods and compositions for detecting the gene or its product, mutants and hybrids of the gene, replicative cloning and expression vectors, and processes for preparing recombinant DAC acetyltransferase polypeptide useful for host cell synthesis of, as well as cell-free synthesis of natural and synthetic cephalosporin antibiotics.
专利号:US-9458188-B2 优先权日:2010-12-22 标 题 :Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; CHOUBAL MILIND D; DALZIEL SEAN MARK; JACKS THOMAS ELLIOTT; THOMPSON ANDREW S; ZELLER JAMES ROBERT; BTG INT LTD 摘要:A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
专利号:US-2008031812-A1 优先权日:1999-06-02 标 题:Redox-stable, non-phosphorylated cyclic peptide inhibitors of sh2 domain binding to target protein, conjugates, thereof, compositions and methods of synthesis and use 发明人:ROLLER PETER P; LONG YA-QIU; LUNG FENG-DI T; KING C RICHTER; YANG DAJUN; VOIGT JOHANNES H 权利人:GOVERNMENT OF THE USA REPRESEN; UNIV GEORGETOWN 摘要:A compound of formula: n n nin which (i) aa 1 is Adi and aa 4 is Glu or (ii) each of aa 1 and aa 4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC 50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.
专利号:US-2008131925-A1 优先权日:2004-12-10 标题 :Production of Beta-Lactams in Single Cells 发明人:BERG MARCO ALEXANDER VAN DEN; BOVENBERG ROELOF ARY LANS; NOORMAN HENDRIK JAN; ROMEIN BASTIAAN 权利人:BERG MARCO ALEXANDER VAN DEN; BOVENBERG ROELOF ARY LANS; NOORMAN HENDRIK JAN; ROMEIN BASTIAAN 摘要:The present invention describes the transformation of a microorganism that does not naturally produce a β-lactam compound with polynucleotides involved in the biosynthesis of β-lactam compounds and the use of such transformed microorganisms in the production of β-lactam compounds or in the identification of genes or factors involved in the synthesis of a β-lactam compound.
专利号:US-2022243244-A1 优先权日:2019-10-10 标 题 :Compositions and methods for in vivo synthesis of unnatural polypeptides 发明人:ROMESBERG FLOYD E; FISCHER EMIL C; HASHIMOTO KOJI; FELDMAN AARON W; DIEN VIVIAN T; ZHANG YORKE 权利人:SCRIPPS RESEARCH INST 摘要:Disclosed herein are compositions, methods, and kits for a cell incorporating unnatural amino acids into an unnatural polypeptide. Also disclosed herein are compositions, methods, and kits for increasing activity and yield of the unnatural polypeptide synthesized by the cell.
摘要:A3343: Wu HQ, Ungerstedt U, Schwarcz R: L-alpha-aminoadipic acid as a regulator of kynurenic acid production in the hippocampus: a microdialysis study in freely moving rats. Eur J Pharmacol. 1995 Jul 25;281(1):55-61. 参考文献:10.1007/s13361-016-1591-x 摘要:Yan X, Li X, Zhang C, Xu Y, Cooks RG. Ambient Ionization Mass Spectrometry Measurement of Aminotransferase Activity. Journal of The American Society for Mass Spectrometry. 2017 Jan 31;28(6):1175–81. doi: 10.1007/s13361-016-1591-x. 参考文献:10.1094/mpmi-19-0998 摘要:Barsch A, Tellström V, Patschkowski T, Küster H, Niehaus K. Metabolite profiles of nodulated alfalfa plants indicate that distinct stages of nodule organogenesis are accompanied by global physiological adaptations. Mol Plant Microbe Interact. 2006 Sep;19(9):998–1013. doi: 10.1094/mpmi-19-0998.