CAS: 847499-27-8; ((R)-1-((2S,3R)-3-Hydroxy-2-(6-Phenylpicolinamido)Butanamido)-3-Methylbutyl)Boronic Acid

该化合物是一个小分子抑制器,主要针对蛋白质,一个细胞综合体,该细胞体是造成无源蛋白质退化的细胞体,被归类为蛋白质抑制剂,并因其潜在的治疗用途,特别是治疗各种癌症,包括多种骨髓瘤和固态肿瘤,受到调查.Delanzomib展示了一个独特的行动机制,在癌症细胞中干扰蛋白质的自闭症,导致流行性疾病和抑制肿瘤生长.其化学结构是有助于其生物活动的功能组别的具体安排.在临床前研究中,Delanzomib显示出克服其他疗法阻力的前景,使其成为综合治疗的候选.然而,与许多调查药物一样,其安全性和功效简介仍在临床试验中评估中.总的来说,Delanzomib代表了肿瘤学领域的一个重要研究领域,特别是在研制有目标的恶性疗法方面.

结构式图片

上下游产品

N-[(1S,2R)-1-[[[(1R)-1-1[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-hydroxypropyl]-6-phenyl-2-pyridinecarboxamide 6-phenyl-pyridine-2-carboxylic acid 16H16N2O4C16H16N2O4 6-phenyl-pyridine-2-carbonyl chloride

合成工艺路线路线简述

  • 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.

海关参考信息

专利信息


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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主要参考文献


1: Sanchez E, Li M, Li J, Wang C, Chen H, Jones-Bolin S, Hunter K, Ruggeri B, Berenson JR. CEP-18770 (delanzomib) in combination with dexamethasone and lenalidomide inhibits the growth of multiple myeloma. Leuk Res. 2012 Nov;36(11):1422-7. doi: 10.1016/j.leukres.2012.07.018. Epub 2012 Aug 17.
48:100663. doi: 10.1016/j.drup.2019.100663. Epub 2019 Nov 11. 111(5):2765-75. doi: 10.1182/blood-2007-07-100651. Epub 2007 Dec 5. 12(1):257-70. doi: 10.1016/j.intimp.2011.11.019. Epub 2011 Dec 13. 58(8):1872-1879. doi: 10.1080/10428194.2016.1263842. Epub 2017 Jan 31. 148(4):569-81. doi: 10.1111/j.1365-2141.2009.08008.x. Epub 2009 Dec 1. 49(2):290-6. doi: 10.1016/j.ejca.2012.09.009. Epub 2012 Oct 8.
61:101100. doi: 10.1016/j.blre.2023.101100. Epub 2023 May 27. 96(1):1-9. doi: 10.1016/j.bcp.2015.04.008. Epub 2015 Apr 29. 10(4):918-929. doi: 10.1111/1759-7714.13030. Epub 2019 Mar 18.

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.
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