CAS: 1137868-52-0; 4-((9-Cyclopentyl-7,7-Difluoro-5-Methyl-6-Oxo-6,7,8,9-Tetrahydro-5H-Pyrimido[4,5-B][1,4]Diazepin-2-yl)Amino)-2-Fluoro-5-Methoxy-N-(1-Methylpiperidin-4-yl)Benzamide

该化合物是一种化学化合物,在制药研究中引起注意,特别是其潜在的治疗用途,被归类为某些蛋白性血管的选择性抑制剂,在细胞生长,分化和新陈代谢等各种细胞过程中起着关键作用.该化合物的行动机制通常涉及与癌症和其他疾病有关的信号路径的调控,使其成为定向疗法的候选.TAK-960的特点是它与目标的血管有具体结合,这可能导致这些蛋白质的活动减少,并进而对肿瘤细胞扩散产生影响.此外,其药用植物特性,如吸收,分布,新陈代谢和排泄,对于确定其在临床环境中的功效和安全特征至关重要.正在进行的研究旨在进一步阐明其在治疗特定类型癌症或其他受动素活动影响的条件方面的生物影响和潜在应用.

结构式图片

上下游产品

4-(9-Cyclopentyl-7,7-Difluoro-5-Methyl-6-Oxo-6,7,8,9-Tetrahydro-5H-Pyrimido[4,5-B][1,4]Diazepin-2-Ylamino)-2-Fluoro-5-Methoxy-Benzoic Acid 1137867-66-3
2-Chloro-9-Cyclopentyl-7,7-Difluoro-5-Methyl-5,7,8,9-Tetrahydro-6H-Pyrimido[4,5-B][1,4]Diazepin-6-One 1062246-03-0
2-Chloro-9-Cyclopentyl-7,7-Difluoro-5,7,8,9-Tetrahydro-Pyrimido[4,5-B][1,4]Diazepin-6-One 1062246-01-8
3-[(2-Chloro-5-Nitro-Pyrimidin-4-yl)-Cyclopentyl-Amino]-2,2-Difluoro-Propanoic Acid Ethyl Ester 1062245-99-1

合成工艺路线路线简述

  • 合成目标产物 Tak-960 主要起始原料 Cyclopentylamine
  • (文献来源)合成步骤主要原料 Cyclopentylamine
📜3-Cyclopentylamino-2,2-Difluoro-Propanoic Acid Ethyl Ester置于盐酸,铁粉,碳酸氢钠,O-Benzotriazol-1-Yl-N,N,N',N'-Bis(Tetramethylene)Uronium Hexafluorophosphate,Caesium Carbonate,溶剂黄146,N,N-二异丙基乙胺体系中,用 乙醇,水,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 53.0H,反应生成Tak960抑制剂
参考文献:Identification Of Novel,Potent And Selective Inhibitors Of Polo-Like Kinase 1
标题:Identification Of Novel,Potent And Selective Inhibitors Of Polo-Like Kinase 1
摘要:A Series Of Pyrimidodiazepines Was Identified As Potent Polo-Like Kinase 1 (Plk1) Inhibitors. The Synthesis And Sar Are Discussed. The Lead Compound 7 (Ro3280) Has Potent Inhibitory Activity Against Plk1,Good Selectivity Against Other Kinases,And Excellent In Vitro Cellular Potency. It Showed Strong Antitumor Activity In Xenograft Mouse Models. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.11.052

海关参考信息

专利信息


专利号:US-8003785-B2
优先权日:2008-06-18
标 题 :Halo-substituted pyrimidodiazepines
发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL
权利人:TAKEDA PHARMACEUTICAL
摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.

专利号:EP-2878592-B1
优先权日:2013-11-27
标题 :Synthesis of amide derivatives of some nonsteroidal antiinflammatory drugs as potential pro-drugs
发明人:KÜCÜKGÜZEL ILKAY; KULABAS NECLA; SET IREM
权利人:KUECUEKGUEZEL ILKAY

专利号:EP-2878592-A1
优先权日:2013-11-27
标题 :Synthesis of amide derivatives of some nonsteroidal antiinflammatory drugs as potential pro-drugs

专利号:WO-2012100179-A1
优先权日:2011-01-21
标题:Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives

专利号:US-2012009151-A1
优先权日:2007-12-21
标题 :Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof
发明人:HAN AMY QI; COBURN GLEN A; PROVONCHA KATHLEEN P; ROTSHTEYN YAKOV
权利人:HAN AMY QI; COBURN GLEN A; PROVONCHA KATHLEEN P; ROTSHTEYN YAKOV; PROGENICS PHARM INC
摘要:Disclosed herein are novel triazines and related compounds, the synthesis thereof, and compositions, including pharmaceutical compositions, comprising the novel triazines and related compounds. Such novel triazines and related compounds function to inhibit or block entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.

专利号:US-2010160351-A1
优先权日:2008-12-19
标题:Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
发明人:JENKINS HELEN; KITT MICHAEL; PEARLMAN RODNEY; SERAFINI TITO; THORSETT EUGENE
权利人:NUON THERAPEUTICS INC
摘要:Disclosed is a pharmaceutical composition comprising (a) a first therapeutic agent, wherein the first therapeutic agent is a compound of formula II: n n n n n n n n n n n n or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , X and n are as defined herein; (b) a second therapeutic agent, wherein the second therapeutic agent is a uric acid synthesis inhibitor or a uricosuric agent; and (c) a pharmaceutically acceptable diluent or carrier.

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献

This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message Sent On: Wed Nov 11
14:13:40 2020 Search: TAK-960 8 selected items Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734.
2: Klauck PJ, Bagby SM, Capasso A, Bradshaw-Pierce EL, Selby HM, Spreafico A, Tentler JJ, Tan AC, Kim J, Arcaroli JJ, Purkey A, Messersmith WA, Kuida K, Eckhardt SG, Pitts TM. Antitumor activity of the polo-like kinase inhibitor, TAK-960, against preclinical models of colorectal cancer. BMC Cancer. 2018 Feb 5;18(1):136. doi: 10.1186/s12885-018-4036-z.
3: Talati C, Griffiths EA, Wetzler M, Wang ES. Polo-like kinase inhibitors in hematologic malignancies. Crit Rev Oncol Hematol. 2016 Feb;98:200-10. doi: 10.1016/j.critrevonc.2015.10.013. Epub 2015 Nov 4.

合成参考文献


参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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