847494-64-8 = 847499-27-8 反应条件:1.1 Reagents: Hydrochloric Acid,2-Methylpropylboronic Acid Solvents: Methanol,Hexane,Water; 16 H,Rt 标题:Discovery Of A Potent,Selective,And Orally Active Proteasome Inhibitor For The Treatment Of Cancer 作者:Dorsey,Bruce D.; Iqbal,Mohamed; Chatterjee,Sankar; Menta,Ernesto; Bernardini,Raffaella; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2008 卷标:51(4) 页码:1068-1072
2-羧基-6-苯基吡啶置于盐酸,氯化亚砜,异丁基硼酸,Sodium Carbonate,N,N-二异丙基乙胺,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 甲醇,正庚烷,水,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 16.0H,反应生成 地兰佐米 参考文献:Proteasome Inhibitor Delanzomib For Use In The Treatment Of Lupus 标题:Proteasome Inhibitor Delanzomib For Use In The Treatment Of Lupus 摘要:本发明提供了一种治疗狼疮的方法,包括向受试者施用化合物a的步骤.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
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-12441733-B2 优先权日:2018-03-26 标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors 发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS 权利人:NOVARTIS AG 摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
专利号:AU-2020409711-A1 优先权日:2019-12-20 标题 :Synthesis of lactone derivatives and their use in the modification of proteins
专利号:EP-4076533-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins
专利号:CA-3164962-A1 优先权日:2019-12-20 标题 :Synthesis of lactone derivatives and their use in the modification of proteins
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合成参考文献
参考文献:10.1093/jnci/djr160 摘要:Ruschak AM, Slassi M, Kay LE, Schimmer AD. Novel proteasome inhibitors to overcome bortezomib resistance. J Natl Cancer Inst. 2011 Jul 06;103(13):1007–17. doi: 10.1093/jnci/djr160. 参考文献:10.1080/10428194.2016.1263842 摘要:Vogl DT, Martin TG, Vij R, Hari P, Mikhael JR, Siegel D, Wu KL, Delforge M, Gasparetto C. Phase I/II study of the novel proteasome inhibitor delanzomib (CEP-18770) for relapsed and refractory multiple myeloma. Leuk Lymphoma. 2017 Aug;58(8):1872–9. doi: 10.1080/10428194.2016.1263842.