专利号:US-2024076303-A1 优先权日:2022-09-07 标 题:Green Synthesis of Salicylaldehydate-Metal-Organic Frameworks and Applications Thereof 发明人:SHETTY DINESH; MOHAMMED ABDUL KHAYUM 权利人:UNIV KHALIFA SCIENCE & TECHNOLOGY 摘要:Embodiments of the present disclosure generally describe two-dimensional/three-dimensional conjugated salicylaldehydate metal organic framework (2D/3D-c-SA MOF) compositions, method for green synthesis of the two-dimensional/three-dimensional conjugated salicylaldehydate metal organic framework (2D/3D-c-SA MOF) compositions, applications of the said compositions in supercapacitors, lithium-ion batteries, electrocatalytic conversion reactions, photocatalytic reduction of CO 2 and other uses.
专利号:US-11447454-B2 优先权日:2015-08-07 标题:Synthesis of benzodiazepine derivatives 发明人:BOYCE MALCOLM JAMES; THOMSEN LIV; GILBERT DONALD ALAN; WOOD DAVID 权利人:TRIO MEDICINES LTD 摘要:The invention relates to processes for the synthesis of benzodiazepine derivatives of Formula I:
专利号:US-2004053355-A1 优先权日:2000-05-26 标题:Modular approach to on-line synthesis, drug discovery and biochemical transformations using immobilized enzyme reactors 发明人:WAINER IRVING; MARKOGLOU NEKTARIA 摘要:A coupled system using extremely different enzymes with incompatible cofactors and reaction conditions has been constructed using standard liquid chromatographic formats and open tubular formats. One of the significant aspects of the present invention lies in the development of the liquid chromatographic on-line enzyme cascade. This has been illustrated by the biosynthetic pathway involving dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase which encompass the synthesis of the key neurotransmitters, norepinephrine and epinephrine. The results demonstrate for the first time the immobilization of dopamine beta-hydroxylase and phenylethanolamine N-methyltransferase. The IMERs are active and can be used in a liquid chromatographic format for qualitative and quantitative determinations. The IMER-HPLC system can be used to carry out standard Michaelis-Menten enzyme kinetic studies and to quantitatively determine enzyme kinetic constants, identify specific enzyme inhibitors, provide information regarding the mode of inhibition and the inhibitor constants (K i ). A second significant aspect of the present invention lies in the ability of the immobilized enzyme reactors to be used independently or as a combination, thus providing a unique opportunity to explore the interrelationships between these enzymes, to investigate the source of diseases and to design new drug entities for identified clinical syndromes.
专利号:US-11845970-B2 优先权日:2016-01-15 标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins 发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN 权利人:UNIV MARYLAND 摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.
专利号:US-12043612-B2 优先权日:2020-05-09 标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same 发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY 权利人:ARVINAS OPERATIONS INC 摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-2003147958-A1 优先权日:2002-01-29 标题 :Biodegradable multi-block copolymers of poly(amino acid)s and poly(ethylene glycol) for the delivery of bioactive agents 发明人:AHN CHEOL-HEE; CHAE SU YOUNG 摘要:This patent discloses the synthesis of a multi-block copolymer containing poly(amino acids) (PAA) and a hydrophilic polymer which are degradable under physiological conditions. Control over the degradation rate of the obtained copolymers is achieved by introducing ester, amide or urethane groups as a biodegradable linkage connecting the PAA and the hydrophilic polymer. The biodegradable multi-block copolymers display high transfection efficiency in plasmid delivery with low cytotoxicity.
1: Namikawa K, Björnsson ES. Rebound Acid Hypersecretion after Withdrawal of Long-Term Proton Pump Inhibitor (PPI) Treatment-Are PPIs Addictive? Int J Mol Sci. 2024 May 17;25(10):5459. doi: 10.3390/ijms25105459. 2: Choi J, Lee H, Cho S, Choi Y, Pham TX, Huynh TTX, Lim YS, Hwang SB. Polygalic acid inhibits african swine fever virus polymerase activity: findings from machine learning and in vitro testing. J Comput Aided Mol Des. 2023 Sep;37(9):453-461. doi: 10.1007/s10822-023-00520-6. Epub 2023 Jul 15. 13:1054575. doi: 10.3389/fphar.2022.1054575.
合成参考文献
摘要:Matov V, Dimitrov B, Bozhiianov V. [Intragastric pH electrometry and gastric secretion in duodenal ulcer (proceedings)]. Vutr Boles. 1980;19(1):55–8. 摘要:British Medical Journal., 289(470), 1984 摘要:ECKARDT V, WERGAND H; SUPERSENSITIVITY TO PENTAGASTRIN IN DIFFUSE ESOPHAGEAL SPASM; GUT 15 (SEP) 706-709 (1974) 参考文献:10.1007/bf01308136 摘要:Smout AJPM, Van Der Schee EJ, Grashuis JL. What is measured in electrogastrography Digestive Diseases and Sciences. 1980 Mar;25(3):179–87. doi: 10.1007/bf01308136. 参考文献:10.1007/bf01308140 摘要:Faichney A, Kim MS, Lee KY, Chey WY. A simplified procedure for preparing innervated gastric pouches. Digestive Diseases and Sciences. 1980 Mar;25(3):205–8. doi: 10.1007/bf01308140.