📜4,9-Dihydro-9-[(+)-Isopinocampheyloxymethyl]-3-Methyl-4-[(4-Methyl-1-Piperazinyl)-Acetyl]-10H-Thieno[3,4-B][1,5]Benzodiazepin-10-One置于盐酸体系中,用 甲酸,水 作为反应溶剂,化学反应生成 替仑西平 参考文献:Thienotricylene For The Treatment Of Bronchial Diseases 标题:Thienotricylene For The Treatment Of Bronchial Diseases 摘要:该发明涉及使用替莫唑和(+)-替莫唑治疗支气管疾病.此外,该发明涉及(+)-替莫唑,其制备方法以及其制备中间体.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-4381301-A 优先权日:1980-05-07 标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.
专利号:US-10308615-B2 优先权日:2015-05-29 标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2025221964-A1 优先权日:2020-03-13 标题 :Substituted Isoxazoles as Selective Nav1.7 Inhibitors for Pain Treatment and Method of Pain Treatment 发明人:FRANZ DOUG; NEFF ROBYNNE; DIBRELL SARA 权利人:UNIV TEXAS 摘要:Tri-substituted isoxazole compounds and compound synthesis is disclosed. Tri-substituted isoxazole compounds having sodium gate channel Nav7 selectivity that are tunable for selectivity over Nav1.5. In particular, structure-activity relationship (SAR) studies demonstrated that subtype selectivity (Nav1.7 vs. Nav1.5) is improved with methylation of the amide nitrogen or ortho-substitution on the phenyl ring in the 5-position.
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合成参考文献
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