CAS: 1025065-69-3; N-((1-Methylpiperidin-4-yl)Methyl)-3-(3-(Trifluoromethoxy)Phenyl)Imidazo[1,2-B]Pyridazin-6-Amine

该化合物是一个小分子抑制器,主要以其作为蛋白质活性细胞PIM(Moloney murine Leukemia病毒的活性融合站点)的选择性抑制器而闻名;它有可能干扰细胞扩散和生存途径,特别是血友恶性肿瘤和固态肿瘤;SGI-1776展示了一种独特的行动机制,针对具有ATP约束力的PIM动性细胞站点,从而抑制了它们的活动,导致癌症细胞中出现聚变;该复合体的特点是其分子重量相对较低,而且具有具体的结构特征,从而增强了其对目标群细胞的结合性;此外,在临床研究中,对SGI-1776进行了关于其功效和安全性简介的评估,显示它作为治疗剂的前景;然而,有必要开展进一步的研究,以充分了解其药理遗传学,潜在副作用和临床环境中的总体治疗潜力.

结构式图片

上下游产品

1-(1-methylpiperidin-4-yl)methanamine 6-chloro-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazine

合成工艺路线路线简述

    📜(1-甲基-4-哌啶-)甲胺,6-Chloro-3-(3-(Trifluoromethoxy)Phenyl)Imidazo[1,2-B]Pyridazine置于苄基三乙基氯化铵,Cesium Fluoride体系中,用 二甲基亚砜 用作溶剂,以91 %的收率获得化合物sgi-1776Freebase
    参考文献:C-6 胺化 3-溴咪唑并[1,2-B]哒嗪的高效合成
    标题:C-6 胺化 3-溴咪唑并[1,2-B]哒嗪的高效合成
    摘要:在 Dmso 中于 100 ° 下用各种 1° 或 2° 烷基胺(2.0 当量),Csf(1.0 当量)和 Bnnet3Cl(10 Mol%)处理 3-溴-6-氯咪唑并[1,2-B]哒嗪c(24小时)给出了对应的...
    Doi:10.1080/00397911.2023.2284350

    专利信息


    专利号:US-11319320-B2
    优先权日:2017-11-06
    标题:PIM kinase inhibitor compositions, methods, and uses thereof
    发明人:BURK MARK J; CHEN BRANDON; LI JINGYI; BACHAN SHAWN
    权利人:SNAP BIO INC
    摘要:This application relates to compounds of formulae (I) and (II) and compositions thereof useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.

    专利号:WO-2022162606-A1
    优先权日:2021-01-30
    标 题:Heterocyclic compounds as kinase inhibitor and uses thereof
    发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK
    权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD
    摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)

    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


    1: Siu A, Virtanen C, Jongstra J. PIM kinase isoform specific regulation of MIG6 expression and EGFR signaling in prostate cancer cells. Oncotarget. 2011 Dec 22. [Epub ahead of print] doi: 10.1038/bjc.2011.426. Epub 2011 Oct 20.
    4: Chen LS, Redkar S, Taverna P, Cortes JE, Gandhi V. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood. 2011 Jul 21;118(3):693-702. Epub 2011 May 31.
    5: Chang M, Kanwar N, Feng E, Siu A, Liu X, Ma D, Jongstra J. PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation. Mol Cancer Ther. 2010 Sep;9(9):2478-87. Epub 2010 Jul 28.

    合成参考文献


    参考文献:10.1007/s00109-011-0788-5
    摘要:Paulin R, Courboulin A, Barrier M, Bonnet S. From oncoproteins/tumor suppressors to microRNAs, the newest therapeutic targets for pulmonary arterial hypertension. J Mol Med (Berl). 2011 Nov;89(11):1089–101. doi: 10.1007/s00109-011-0788-5.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知