Methyl 3-<<(Ethoxycarbonyl)Methyl>-N-Methylamino>Sulfonyl>-2-Thiophenecarboxylate置于sodium Methylate体系中,用 甲醇,Xylene 作为反应溶剂,化学反应 7.67H,反应生成 替诺昔康 参考文献:Analogs And Derivatives Of Tenoxicam. 1. Synthesis And Antiinflammatory Activities Of Analogs With Different Residues On The Ring Nitrogen And The Amide Nitrogen 标题:Analogs And Derivatives Of Tenoxicam. 1. Synthesis And Antiinflammatory Activities Of Analogs With Different Residues On The Ring Nitrogen And The Amide Nitrogen 摘要:The Synthesis Of Tenoxicam,4-Hydroxy-2-Methyl-N-2-Pyridyl-2H-Thieno[2,3-E]-1,2-Thiazine-3-Carboxami De 1,1-Dioxide (1E),And Of The Analogues With Various Residues On The Ring Nitrogen And The Amide Nitrogen Is Described. This New Class Of "Oxicams" Has Pronounced Antiinflammatory And Analgesic Properties. The Very Specific Structure-Activity Relationship Of Isomeric And Isosteric Groups At The Amide Nitrogen Has Been Evaluated. The Substituent In Position 2 Also Has A Great Influence On The Pharmacological Properties. Tenoxicam Is Presently Undergoing Clinical Trials. DOI:10.1021/jm00387A017
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-2017132357-A1 优先权日:2015-11-10 标 题 :Platform for visual synthesis of genomic, microbiome, and metabolome data 发明人:BREWERTON SUZANNE; COON BRYAN; XIE CHAO; Zuniga Rafael; DE CASTRO JHALLEY; Yooseph Shibu; LI WEIZHONG; ULASZEK RYAN; KLITGORD NIELS; YEO ZHENXUAN; Mulawadi Fabi; FRIEDMAN AARON; TERRELL STEPHEN; WIRAWAN ADRIANTO; Gule Korkut; Saygi Erhan; HADIMULYONO ANDREAS; Tan Yong Heng; Sisk Thomas; VOLOCHENKO ALEXEY; BLAIR SEAN; ANG AIK MENG; LIM KIAN YONG; ZHANG DANIEL; Bezyazychnyy Dmitry; WANG QIANG; LIU XIAOHUI; Lim Ream; Veshkurtsev Nikita; Wong Marie; PIPER JASON; SUN MIAO; CLONEY MATTHEW; PHAM BAO; TURPAZ YARON 权利人:HUMAN LONGEVITY INC 摘要:Described are platforms, systems, media, and methods for providing a biologic information visual synthesis application, the biologic information including one or more of: genome data, microbiome data, and metabolome data.
专利号:US-7332505-B2 优先权日:1999-02-26 标 题 :Nitrosated and nitrosylated proton pump inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; LETTS L GORDON; RICHARDSON STEWART K; TAM SANG WILLIAM; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or NO 2 group, and, optionally, at least one compound that donates, transfers, or releases nitric oxide, induces the production of endogenous nitric oxide or endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one nonsteroidal antiinflammatory drug, selective COX-2 inhibitor, antacid, bismuth-containing reagent, acid-degradable antibacterial compound, and mixtures thereof. The present invention also provides methods for treating and/or preventing gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti- Helicobacter pylon properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating Helicobacter pylori and viral infections. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
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合成参考文献
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