CAS: 867160-71-2; Cis-3-(8-Amino-1-(2-Phenylquinolin-7-yl)Imidazo[1,5-A]Pyrazin-3-yl)-1-Methylcyclobutan-1-Ol

该化合物是一个小分子抑制剂,主要针对胰岛素型生长因子1受体(IGF-1R)和胰岛素受体(IR),被归类为抗抑郁剂,并因其在肿瘤学中的潜在治疗应用而引人注目,特别是在治疗各种癌症,包括抗常规疗法的癌症方面.Linsitinib展示了独特的行动机制,干扰细胞扩散和生存的信号路径,这些路径往往在癌症细胞中受到高度管制.该化合物通常通过口服管理,并在临床试验中评估其功效和安全性.就其化学结构而言,Linsitinib含有多种功能性组,有助于其生物活动和可溶性特征.与许多制药剂一样,其药代科学,包括吸收,分布,代谢和排泄,对于确定其治疗潜力和施药疗法至关重要.

结构式图片

上下游产品

CAS号867164-54-3 2-苯基喹啉-7-频哪醇硼酸酯 | CAS号936901-75-6 顺式-3-(8-氨基-1-溴咪... | CAS号936901-73-4 3-(1-BROMO-8-CH...

合成工艺路线路线简述

    3-(8-Bromo-1-Chloroh-Pyrrolo[1,2-A]Pyrazin-6-yl)Cyclobutanone无结构图 在 三苯基膦 氨,Caesium Carbonate体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺,异丙醇作为反应溶剂,反应 18.0H,获得 3-[8-Amino-1-(2-Phenylquinolin-7-yl)Imidazo[1,5-A]Pyrazin-3-Yl]-1-Methylcyclobutan-1-Ol
    参考文献:[En] Process For The Preparation Of The Compound Osi-906[Fr] Pr°Cédé De Préparation Du Composé Osi-906
    标题:[En] Process For The Preparation Of The Compound Osi-906[Fr] Pr°Cédé De Préparation Du Composé Osi-906

    海关参考信息

    专利信息


    专利号:US-2024342244-A1
    优先权日:2021-07-28
    标 题:Isthmin Protein Therapeutics for the Treatment of Non-Alcoholic Fatty Liver Disease
    发明人:SVENSSON KATRIN JENNIFER; VOILQUIN LAETITIA
    权利人:UNIV LELAND STANFORD JUNIOR
    摘要:Compositions and methods are provided for the treatment of one or both of type 2 diabetes and fatty liver disease, e.g. non-alcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH). The adipokine Isthmin-1 (ISM1) protein increases adipose glucose uptake while suppressing hepatic lipid synthesis.

    专利号:US-2017107577-A1
    优先权日:2014-03-11
    标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
    发明人:AL-EJEH FARES
    权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
    摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

    专利号:US-2012220595-A1
    优先权日:2009-11-12
    标题:Deuterated Tyrosine Kinase Inhibitors
    发明人:EPSTEIN DAVID M; JIN MEIZHONG; MULVIHILL MARK J
    权利人:EPSTEIN DAVID M; JIN MEIZHONG; MULVIHILL MARK J; OSI PHARMACEUTICALS LLC
    摘要:Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1R and/or IR.
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    主要参考文献


    1: Zhang H, Kathawala RJ, Wang YJ, Zhang YK, Patel A, Shukla S, Robey RW, Talele TT, Ashby CR Jr, Ambudkar SV, Bates SE, Fu LW, Chen ZS. Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance. Int J Biochem Cell Biol. 2014 Jun;51:111-9. doi: 10.1016/j.biocel.2014.03.026. Epub 2014 Apr 12. doi: 10.1210/en.2013-2032. Epub 2014 Apr 8. doi: 10.3892/or.2013.2819. Epub 2013 Oct 25.
    4: Zhao H, Desai V, Wang J, Epstein DM, Miglarese M, Buck E. Epithelial-mesenchymal transition predicts sensitivity to the dual IGF-1R/IR inhibitor OSI-906 in hepatocellular carcinoma cell lines. Mol Cancer Ther. 2012 Feb;11(2):503-13. doi: 10.1158/1535-7163.MCT-11-0327. Epub 2011 Dec 9. doi: 10.1158/1078-0432.CCR-10-2274. Epub 2011 Jan 21.
    6: Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, O'Connor M, Pirritt C, Sun Y, Yao Y, Arnold LD, Gibson NW, Ji QS. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med Chem. 2009 Sep;1(6):1153-71. doi: 10.4155/fmc.09.89.

    合成参考文献


    参考文献:10.1186/1476-4598-13-136
    摘要:Li H, Xu L, Li C, Zhao L, Ma Y, Zheng H, Li Z, Zhang Y, Wang R, Liu Y, Qu X. Ubiquitin ligase Cbl-b represses IGF-I-induced epithelial mesenchymal transition via ZEB2 and microRNA-200c regulation in gastric cancer cells. Molecular Cancer. 2014 Jun 02;13(1):136. doi: 10.1186/1476-4598-13-136.
    参考文献:10.1186/s12885-015-1670-6
    摘要:Jaillardon L, Abadie J, Godard T, Campone M, Loussouarn D, Siliart B, Nguyen F. The dog as a naturally-occurring model for insulin-like growth factor type 1 receptor-overexpressing breast cancer: an observational cohort study. BMC Cancer. 2015 Oct 08;15():664.
    参考文献:10.1038/s12276-020-0479-9
    摘要:Ciechomska IA, Gielniewski B, Wojtas B, Kaminska B, Mieczkowski J. EGFR/FOXO3a/BIM signaling pathway determines chemosensitivity of BMP4-differentiated glioma stem cells to temozolomide. Experimental & Molecular Medicine. 2020 Aug 12;52(8):1326–40. doi: 10.1038/s12276-020-0479-9.
    参考文献:10.1186/s43046-022-00106-7
    摘要:The annual conference of National Cancer Institute - Cairo University "Bridging Gaps in Oncology" : InterContinental Citystars Cairo hotel. 3 - 5 November, 2021. J Egypt Natl Canc Inst. 2022 Mar 21;34(Suppl 1):15.
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