CAS: 937174-76-0; (S)-4-(2-(4-Amino-1,2,5-Oxadiazol-3-yl)-1-Ethyl-7-(Piperidin-3-Ylmethoxy)-1H-Imidazo[4,5-C]Pyridin-4-yl)-2-Methylbut-3-Yn-2-Ol

该化合物是一个小分子抑制器,主要以其作为蛋白质顺质AKT(又称蛋白顺质顺质顺质B)选择性抑制器的作用而闻名.它是一组化合物的一部分,它针对细胞生长,生存和新陈代谢过程中涉及的途径,使其对癌症研究和治疗感兴趣.该化合物展示了AKT等形形的特殊亲近性,在包括食道和葡萄糖新陈代谢在内的各种细胞过程中发挥着关键作用.GSK 690693已经研究过它可能用于各种恶性肿瘤的治疗用途,特别是以异常顺质AKT信号为特征的.就其化学特性而言,GSK 690693的特征是分子结构,其中包括有助于其生物活动和选择性的特定功能组.和许多动脉抑制剂,其功效和安全特征是正在进行的研究的主题,特别是在癌症治疗的组合疗法和抗药机制方面.

结构式图片

欧盟法规

C&L通报

上下游产品

1,1-dimethylethyl (3S)-3-({[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-4-(3-hydroxy-3-methyl-1-butyn-1-yl)-1H-imidazo[4,5-c]pyridin-7-yl]oxy}methyl)-1-piperidinecarboxylate ethyl-(3-bromo-5-nitropyridin-4-yl)amine 4-ethylpyridine-3,4-diamine5-bromo-2-chloro-N4-ethylpyridine-3,4-diamine (7-bromo-4-chloro-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)acetonitrile

合成工艺路线路线简述

  • 937174-75-9 = 937174-76-0
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 2.5 H,Rt
    标题:Identification Of 4-(2-(4-Amino-1,2,5-Oxadiazol-3-Yl)-1-Ethyl-7-{[(3S)-3-Piperidinylmethyl]Oxy}-1H-Imidazo[4,5-C]Pyridin-4-Yl)-2-Methyl-3-Butyn-2-Ol (Gsk690693),A Novel Inhibitor Of Akt Kinase
    作者:Heerding,Dirk A.; Rhodes,Nelson; Leber,Jack D.; Clark,Tammy J.; Keenan,Richard M.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2008 卷标:51(18) 页码:5663-5679]

    = 937174-76-0 [标题:Reaction Conditions
    标题:Selectively Nonselective Kinase Inhibition: Striking The Right Balance
    作者:Morphy,Richard
    参考文献:Journal Of Medicinal Chemistry 日期:2010 卷标:53(4) 页码:1413-1437]

    = 937174-76-0 [标题:Reaction Conditions
    标题:Targeted Small-Molecule Inhibitors Of Protein Kinase B As Anticancer Agents
    作者:Collins,Ian
    参考文献:Anti-Cancer Agents In Medicinal Chemistry 日期:2009 卷标:9(1) 页码:32-50]

    937174-75-9 = 937174-76-0
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 2.5 H,Rt
    标题:1H-Imidazo[4,5-C]Pyridin-2-Yl Derivatives As Inhibitors Of Akt Activity And Their Therapeutic Uses
    参考文献:World Intellectual Property Organization]

    = 937174-76-0 [标题:Reaction Conditions
    标题:Methods Of Use For Inhibitors Of Akt Activity
    参考文献:World Intellectual Property Organization]

    = 937174-76-0 [标题:Reaction Conditions
    标题:Erb Family Inhibitor Combination With Pi3 Kinase Inhibitor Or Akt Inhibitor For Cancer Treatment
    参考文献:World Intellectual Property Organization
(3-溴-5-硝基-吡啶-4-基)-乙基-胺置于四(三苯基膦)钯 N-甲基吗啉,盐酸,Sodium Nitrate,盐酸羟胺,水,Caesium Carbonate,Isopropyl Magnesium Chloride,1,8-二氮杂双环[5.4.0]十一碳-7-烯,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,三氟乙酸,Sodium Iodide,Tin(Ll) Chloride,锌体系中,用 四氢呋喃,1,4-二氧六环,甲醇,乙醚,二氯甲烷,水,溶剂黄146,二甲基亚砜,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 79.34H,反应生成 土大黄甙
参考文献:Wo2008/121685
标题:Wo2008/121685

海关参考信息

专利信息


专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12054508-B1
优先权日:2019-04-16
标 题 :Compositions and methods for sulfation of carbohydrates and peptides via electron-deficient aryl sulfate diesters
发明人:NIU JIA; LIU CHAO; YANG CANGJIE
权利人:THE TRUSTEES OF BOSTON COLLEGE
摘要:In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

专利号:US-9908846-B2
优先权日:2014-02-21
标题:Composition, synthesis, and use of new arylsulfonyl isonitriles
发明人:FLEMING FRASER FERGUSSON; LUJAN MONTELONGO JESUS ARMANDO
权利人:DUQUESNE UNIV OF THE HOLY GHOST; UNIV HOLY GHOST DUQUESNE
摘要:This invention relates to novel isonitriles, including arylsulfonyl isonitriles, and methods for their synthesis. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.

专利号:WO-2010062846-A1
优先权日:2008-11-26
标题 :Synthesis of stable organogold compounds and methods of use thereof
发明人:HAMMOND GERALD B; BATES PAULA J; VAISBERG ABRAHAM J; LIU LEPING; XU BO
权利人:HAMMOND GERALD B; BATES PAULA J; VAISBERG ABRAHAM J; LIU LEPING; XU BO
摘要:Disclosed herein are novel gold containing compounds and methods of synthesis and use thereof. The novel compounds are very stable. The stability of the compounds allows for their use in methods of treating cancer cells. Disclosed herein are examples of the use of the compounds to inhibit growth of cancer cell lines. The utility of the compounds disclosed herein is a method of treating cancer cells in which a therapeutically effective amount of a compound is administered.

专利号:US-8193360-B2
优先权日:2003-07-31
标 题:Radiolabelled fluorobenzamide analogues, their synthesis and use in diagnostic imaging
发明人:MACH ROBERT H; TU ZHUDE
权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON
摘要:Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18 F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.

专利号:US-9949970-B2
优先权日:2010-09-14
标题 :Synthesis of new benzothiazole derivatives as potential anti-tubercular agents
发明人:KAMAL AHMED; SHETTI RAJESH VCRNC; SWAPNA PONNAMPALLI; AZEEZA SHAIK; REDDY A MALLA; KHAN INSHAD ALI; ABDULLAH SHEIKH TASDUQ; SHARMA SANDEEP; KALIA NITIN PAL
权利人:COUNCIL SCIENT IND RES
摘要:Disclosed are compounds of general formula A useful as potential anti-tubercular agents. The general formula A is
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主要参考文献


1: Carol H, Morton CL, Gorlick R, Kolb EA, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups C, Smith MA, Houghton PJ, Lock RB. Initial testing (stage 1) of the Akt inhibitor GSK690693 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2010 Dec 15;55(7):1329-37. doi: 10.1002/pbc.22710. Epub 2010 Aug 25.
2: Kumar R, Blakemore SJ, Ellis CE, Petricoin EF 3rd, Pratt D, Macoritto M, Matthews AL, Loureiro JJ, Elliston K. Causal reasoning identifies mechanisms of sensitivity for a novel AKT kinase inhibitor, GSK690693. BMC Genomics. 2010 Jul 6;11:419.
3: Altomare DA, Zhang L, Deng J, Di Cristofano A, Klein-Szanto AJ, Kumar R, Testa JR. GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt. Clin Cancer Res. 2010 Jan 15;16(2):486-96.

合成参考文献


参考文献:10.1158/0008-5472.can-07-5783
摘要:Rhodes N, Heerding DA, Duckett DR, Eberwein DJ, Knick VB, Lansing TJ, McConnell RT, Gilmer TM, Zhang SY, Robell K, Kahana JA, Geske RS, Kleymenova EV, Choudhry AE, Lai Z, Leber JD, Minthorn EA, Strum SL, Wood ER, Huang PS, Copeland RA, Kumar R. Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity. Cancer Res. 2008 Apr 01;68(7):2366–74. doi: 10.1158/0008-5472.can-07-5783.
参考文献:10.1021/ml500088x
摘要:Nguyen T, Coover RA, Verghese J, Moran RG, Ellis KC. Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation. ACS Med Chem Lett. 2014 May 08;5(5):462–7.
参考文献:10.18632/oncotarget.6126
摘要:Vétillard A, Jonchère B, Moreau M, Toutain B, Henry C, Fontanel S, Bernard AC, Campone M, Guette C, Coqueret O. Akt inhibition improves irinotecan treatment and prevents cell emergence by switching the senescence response to apoptosis. Oncotarget. 2015 Dec 22;6(41):43342–62.
摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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