CAS: 935888-69-0; N-((S)-3-Methoxy-1-(((S)-3-Methoxy-1-(((S)-1-((R)-2-Methyloxiran-2-yl)-1-Oxo-3-Phenylpropan-2-yl)Amino)-1-Oxopropan-2-yl)Amino)-1-Oxopropan-2-yl)-2-Methylthiazole-5-Carboxamide

该化合物是一个小分子抑制剂,主要以其在治疗多种间皮瘤和其他恶性肿瘤方面的作用而闻名.它作为一个蛋白质抑制剂,它破坏蛋白质降解无处不在的蛋白质的能力,导致亲食性因素积累并最终导致癌症细胞死亡.Oprozomib的特点是它能够有效渗透组织,并口服生物利用率,使它成为病人的方便选择.该化合物有一个具体的化学结构,其中包括一种典型的蛋白质抑制剂核心结构,有助于其行动机制.此外,它还被研究过它克服对其他蛋白抑制剂的抗药性的潜力,表明它在治疗战略中的重要性.同许多药剂一样,Oprozomib的功效和安全状况是通过临床试验来评估的,这些药剂评估其对肿瘤反应和总体患者结果的影响.它的开发反映了目前为加强癌症治疗方式和改善患者生活质量而作的努力.

结构式图片

物理性质

MSDS等安全信息

上下游产品

CAS号1148157-29-2 (S)-2-amino-1-(... | CAS号40004-69-1 2-甲基-1,3噻唑-5-羧酸 | CAS号1148157-34-9 (S)-2-amino-3-m... | CAS号79836-78-5 2-甲基噻唑-5-羧酸乙酯

合成工艺路线路线简述

  • 1010136-49-8 + 935888-16-7 = 935888-69-0
    反应条件:1.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: N-Methyl-2-Pyrrolidone; 15 Min,< 0 °C; 12 H,0 °C
    标题:Gastro-Retentive Modified Release Dosage Forms For Oprozomib And Process To Make Thereof
    参考文献:United States]

    2005490-80-0 = 935888-69-0
    反应条件:1.1 Reagents: Diisopropylethylamine Catalysts: 1-Hydroxybenzotriazole,1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: Tetrahydrofuran; Cooled; 4 H,Rt
    标题:Process For Preparation Of Oprozomib And Analogs Thereof
    参考文献:China]

    1010136-49-8 + 935888-16-7 = 935888-69-0
    反应条件:1.1 Reagents: 1-Hydroxybenzotriazole Solvents: Dichloromethane; 10 Min,-5 °C1.2 Reagents: 1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride; 30 Min,-5 °C1.3 10 Min,-5 °C1.4 Reagents: Diisopropylethylamine; -5 °C; 30 Min,-5 °C; -5 °C -> Rt; 6 H,Rt
    标题:Method For Efficiently Preparing Opzomib
    参考文献:China]

    1010136-49-8 + 935888-16-7 = 935888-69-0
    反应条件:1.1 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: Dimethylformamide,N-Methyl-2-Pyrrolidone; 23 °C -> 0 °C1.2 Reagents: Diisopropylethylamine; 15 Min,< 0 °C; 12 H,0 °C
    标题:Modified Release Formulations For Oprozomib
    参考文献:United States]

    1010136-49-8 + 935888-16-7 = 935888-69-0
    反应条件:1.1 Reagents: 1-Hydroxybenzotriazole,1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: N-Methyl-2-Pyrrolidone; 23 °C -> 0 °C; -5 - 0 °C1.2 Reagents: Diisopropylethylamine; 15 Min,< 0 °C; 12 H,0 °C
    标题:Preparation And Thermal Properties Of Crystalline Tripeptide Epoxy Ketone Protease Inhibitors
    参考文献:United States]

    1083069-64-0 + 40004-69-1 = 935888-69-0
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane; 0 °C; 2 H,0 °C1.2 Reagents: 1-Hydroxybenzotriazole,Diisopropylethylamine,1-[bis(Dimethylamino)Methylene]-1H-Benzotriazolium Hexafluorophosphate(1-) 3-Oxi... Solvents: Tetrahydrofuran; -5 °C; 4 H,-5 °C
    标题:Design And Synthesis Of An Orally Bioavailable And Selective Peptide Epoxyketone Proteasome Inhibitor (Pr-047)
    作者:Zhou,Han-Jie; Aujay,Monette A.; Bennett,Mark K.; Dajee,Maya; Demo,Susan D.; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2009 卷标:52(9) 页码:3028-3038
📜2-甲基噻唑-5-羧酸乙酯置于palladium 10% On Activated Carbon,水,氢气,1-羟基苯并三唑,O-(1H-Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Hexafluorophosphate,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 四氢呋喃,N-甲基吡咯烷酮,甲醇,水 作为反应溶剂,化学反应 55.17H,反应生成 Oprozomib(onx-0912)抑制剂
参考文献:Immediate Release Formulations For Oprozomib
标题:Immediate Release Formulations For Oprozomib
摘要:本公开涉及即时释放的药物制剂(例如,固体剂型,例如,片剂),其对于口服给予oprozomib或其药学上可接受的盐给人类或动物主体是有用的,以及制备和使用该制剂的方法.

海关参考信息

专利信息


专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-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:US-11623929-B2
优先权日:2018-06-04
标 题 :Spirocyclic compounds
发明人：NASVESCHUK CHRISTOPHER G; DEY FABIAN; GOERGLER ANNICK; NORCROSS ROGER; SCHMID PHILIPP
权利人:C4 THERAPEUTICS INC
摘要:The present invention provides compounds and intermediates. The present invention also provides compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation. The present invention also provides compounds that may be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

其他信息查阅

供应商参考报价(招募中)

品牌试剂参考报价(招募中)

实用工具

⚠️全国化工行业净网倡议书
📋制造商识别码
📖 海关编码查询
📝MSDS生成器

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

主要参考文献

1. Use of peptide epoxyketone proteasome inhibitors for metastasis suppression By Kirk, Christopher J.; Jiang, Jing From PCT Int. Appl. (2011), WO 2011060179 A1 20110519. 2. Combination of proteasome inhibitors and anti-hepatitis medication for treating hepatitis By Schubert, Ulrich From PCT Int. Appl. (2011), WO 2011009961 A1 20110127. 3. A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma By Chauhan, Dharminder; Singh, Ajita V.; Aujay, Monette; Kirk, Christopher J.; Bandi, Madhavi; Ciccarelli, Bryan; Raje, Noopur; Richardson, Paul; Anderson, Kenneth C. From Blood (2010), 116(23), 4906-4915. 4. Preparation and thermal properties of crystalline tripeptide epoxy ketone protease inhibitors By Phiasivongsa, Pasit; Sehl, Louis C. From PCT Int. Appl. (2010), WO 2010108172 A1 20100923. 5. Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia By Roccaro, Aldo M.; Sacco, Antonio; Aujay, Monette; Ngo, Hai T.; Azab, Abdel Kareem; Azab, Feda; Quang, Phong; Maiso, Patricia; Runnels, Judith; Anderson, Kenneth C.; et al From Blood (2010), 115(20), 4051-4060. 6. Use of quinazoline derivatives for the treatment of hematologic malignancies, inflammatory and autoimmune disorders By Gallatin, Michael W.; Ulrich, Roger G.; Giese, Neill From PCT Int. Appl. (2010), WO 2010057048 A1 20100520. 7. Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy By Dick, Lawrence R.; Fleming, Paul E. From Drug Discovery Today (2010), 15(5/6), 243-249. 8. Design and Synthesis of an Orally Bioavailable and Selective Peptide Epoxyketone Proteasome Inhibitor (PR-047) By Zhou, Han-Jie; Aujay, Monette A.; Bennett, Mark K.; Dajee, Maya; Demo, Susan D.; Fang, Ying; Ho, Mark N.; Jiang, Jing; Kirk, Christopher J.; Laidig, Guy J.; et al From Journal of Medicinal Chemistry (2009), 52(9), 3028-3038. 9. Preparation of peptide epoxides and peptide aziridines as enzyme inhibitors, especially N-terminal nucleophile hydrolase inhibitors, for treating diseases By Zhou, Han-Jie; Laidig, Guy J.; Shenk, Kevin D.; Sun, Congcong M. From PCT Int. Appl. (2008), WO 2008140782 A2 20081120. 10. Compounds for enzyme inhibition By Zhou, Han-Jie; Sun, Congcong M.; Shenk, Kevin D.; Laidig, Guy J. From U.S. Pat. Appl. Publ. (2007), US 20070105786 A1 20070510.

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:10.1038/s41408-022-00636-2
摘要:Kumar H, Mazumder S, Chakravarti S, Sharma N, Mukherjee UK, Kumar S, Baughn LB, Van Ness BG, Mitra AK. secDrug: a pipeline to discover novel drug combinations to kill drug-resistant multiple myeloma cells using a greedy set cover algorithm and single-cell multi-omics. Blood Cancer Journal. 2022 Mar 09;12(3):39. doi: 10.1038/s41408-022-00636-2.
参考文献:10.1186/s12964-022-00834-2
摘要:Gong R, Chen M, Huang C, Wong HLX, Kwan HY, Bian Z. Combination of artesunate and WNT974 induces KRAS protein degradation by upregulating E3 ligase ANACP2 and β-TrCP in the ubiquitin–proteasome pathway. Cell Communication and Signaling. 2022 Mar 19;20(1):34. doi: 10.1186/s12964-022-00834-2.
📝 需求与反馈
尽可能描述清楚需求与问题信息
×

通知