专利号:US-6919382-B2 优先权日:2000-08-31 标 题 :Preparation and uses of conjugated solid supports for boronic acids 发明人:HALL DENNIS G 权利人:UNIV ALBERTA 摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.
专利号:EP-3560934-A1 优先权日:2018-04-26 标题:Process for the preparation of pure 2-cyanophenylboronic acid and esters thereof, intermediates of perampanel or of e2040 发明人:FONTANA FRANCESCO; DI PIETRO FEDERICO; NALIN ARNALDO 权利人:FIS FABBRICA ITALIANA SINTETICI SPA 摘要:The present invention relates to a process for the synthesis of 2-cyanophenylboronic acid and the esters and salts thereof, which are intermediates of the synthesis of active pharmaceutical ingredients such as Perampanel or E2040, wherein impurity formation, in particular the formation of DBBN iPrketone, is reduced.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:US-7153960-B2 优先权日:2001-12-10 标 题:Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones 发明人:ZHOU JIACHENG; OH LYNETTE M; MA PHILIP; LI HUI-YIN; CONFALONE PASQUALE 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. n nThese compounds are useful as factor Xa inhibitors.
专利号:WO-2012059568-A1 优先权日:2010-11-05 标 题:Novel water-soluble indolobenzazepine molecules demonstrating antimitotic, antivascular, and antitumor activities in vivo 发明人:DODD ROBERT; BAKALA JOANNA; LIU JIANMIAO; BIGNON JEROME; PONS VALERIE; BEAUMONT STEPHANE 权利人:CENTRE NAT RECH SCIENT; DODD ROBERT; BAKALA JOANNA; LIU JIANMIAO; BIGNON JEROME; PONS VALERIE; BEAUMONT STEPHANE 摘要:The present patent application relates to indolobenzazepine derivatives having an antitumor activity, to the synthesis thereof, and to the use thereof. In particular, the present patent application relates to the stereocontrolled synthesis of C5-substituted indolobenzazepinones enabling only one of the two possible C5 isomers to be obtained, as well as water-soluble analogs making it possible to demonstrate the very high effectiveness of said molecules in reducing the size of tumors in vivo .
专利号:US-2024002405-A1 优先权日:2022-06-01 标题 :Antimicrobial compounds, synthesis methods, and uses thereof 发明人:VERMA RAJNI; DONAVALLI KRISHNA MOHAN; ZAID GENE H 权利人:ANKH LIFE SCIENCES LTD 摘要:Fused tricyclic compounds and novel methods of synthesizing, using, and/or administering the same. Methods of inhibiting microbial activity and/or treating a microbial infection with fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds. The treatment of subjects suffering from a microbial infection comprises the step of administering to the subject one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds or a composition comprising one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds.
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