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-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8129560-B2 优先权日:2005-08-15 标 题 :Process for the synthesis of mandipropamid and derivatives thereof 发明人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG 权利人:BOWDEN MARTIN CHARLES; CLARK THOMAS AITCHESON; GIORDANO FANNY; JAU BEAT; SCHNEIDER HANS-DIETER; SEIFERT GOTTFRIED; ZELLER MARTIN; FABER DOMINIK; WISS JUERG; SYNGENTA CROP PROT INC 摘要:A process for the preparation of a compound of formula (I), the process comprising: (i) the reaction of a compound of formula (III), with a compound of formula (IV) to give a compound of formula (II), and (ii) the reaction of the compound of formula (II) with a leaving group, to give the compound of formula (I).
专利号:US-3886166-A 优先权日:1972-12-22 标 题:Method for the synthesis of ({35 )-glaziovine 发明人:CASAGRANDE CESARE; CANONICA LUIGI 权利人:SIPHAR SA 摘要:A method is disclosed for synthesizing ( + OR - )-glaziovine, a naturally occurring alkaloid, useful in the therapeutics as an anxiolytic drug. The reaction pattern is the following: WHEREIN OR1 is an ether or ester group, and R2 is a diazo group. Several variants are provided for the different stages of the method and hydrogenation with catalysts and irradiation with visible and UV radiations are employed for preparing certain intermediates and for carrying out the final stage of the method.
专利号:WO-2022127321-A1 优先权日:2020-12-18 标题 :Novel intermediate, preparation method for same, and applications thereof 发明人:QIN YONG; ZHONG WU; LI SONG; XUE FEI; SONG HAO; LIU XIAOYU; ZHANG DAN; HE HUAN; Xue Fanglin; ZHANG MAOJIE; HU ZHAO; LI CHUNXIN; ZHU JIANQUAN; ZHANG YIFAN; TANG YU; WANG RUI; LI XUE; CAI YUKUN 权利人:UNIV SICHUAN 摘要:The invention relates to the field of medicament synthesis and specifically to a novel intermediate, a preparation method for same, and applications thereof. The structural formula of the novel intermediate of the present application is as represented by formula (I): in which R is a secondary amine protecting group. The present invention, based on possible biogenetic pathways of morphine derivatives, by means of a strategy for biomimetic synthesis, with an asymmetric transfer hydrogenation reaction and an intramolecular oxidative dearomatization Heck reaction in the preparation process of the intermediate serving as key reactions for total synthesis, implements the highly efficient synthesis of the morphine derivatives. The synthesis of the morphine derivatives starting from the novel intermediate provided in the present invention is characterized by significantly reduced synthesis steps, an increased yield, a reduced discharge of gaseous, liquid, and solid wastes, and inexpensive production costs.
专利号:US-2017266353-A1 优先权日:2014-05-13 标 题:Bioadhesive compounds and methods of synthesis and use 发明人:MURPHY JOHN L; RADANO CHRISTOPHER P; DALSIN JEFFREY L; KOEPSEL JUSTIN T 权利人:DSM IP ASSETS BV 摘要:Synthesis methods for creating polymeric compounds comprising phenyl derivatives (PD), or PDp i.e., polymers modified with PD, with desired surface active effects are described. The polymer backbone of PDp has structural or performance features that can be tailored to control physical properties of PDp, allowing it to be useful for different applications i.e., tissue adhesives or sealants, adhesion promoting coatings, and antifouling coatings.