CAS: 1361951-15-6; 2-(Trans-4-((3-(3-(Trifluoromethyl)Phenyl)Imidazo[1,2-B]Pyridazin-6-yl)Amino)Cyclohexyl)Propan-2-Ol

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6-Chloro-3-(3-(Trifluoromethyl)Phenyl)Imidazo[1,2-B]Pyridazine 928336-97-4

合成工艺路线路线简述

    📜3-溴-6-氯咪唑并[1,2-B]哒嗪置于四(三苯基膦)钯,Potassium Carbonate,N,N-二异丙基乙胺,Cesium Fluoride体系中,用 1,4-二氧六环,水,二甲基亚砜 用作溶剂,化学反应 28.0H,反应生成反式-A,A-二甲基-4-[[3-[3-(三氟甲基)苯基]咪唑[1,2-B]哒嗪-6-基]氨基]环己醇
    参考文献:Substituted Imidazo[1,2-B]Pyridazines As Protein Kinase Inhibitors
    标题:Substituted Imidazo[1,2-B]Pyridazines As Protein Kinase Inhibitors
    摘要:本发明提供具有以下结构之一的蛋白激酶(i),(II)或(III):或其立体异构体,前药,互变异构体或药用可接受盐,其中r,R1,R2和x如本文所定义.还公开了在治疗癌症,自身免疫,炎症和其他pim激酶相关疾病中使用这些组合物和方法.

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    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.

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    主要参考文献


    1: Foulks JM, Carpenter KJ, Luo B, Xu Y, Senina A, Nix R, Chan A, Clifford A, Wilkes M, Vollmer D, Brenning B, Merx S, Lai S, McCullar MV, Ho KK, Albertson DJ, Call LT, Bearss JJ, Tripp S, Liu T, Stephens BJ, Mollard A, Warner SL, Bearss DJ, Kanner SB. A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas. Neoplasia. 2014 May;16(5):403-12. doi: 10.1016/j.neo.2014.05.004.
    2: Thakur ML, Marcus CS, Saeed S, Pallela V, Minami C, Diggles L, Le Pham H, Ahdoot R, Kalinowski EA. 99mTc-labeled vasoactive intestinal peptide analog for rapid localization of tumors in humans. J Nucl Med. 2000 Jan;41(1):107-10.

    合成参考文献


    参考文献:10.1021/acs.jmedchem.3c01802
    摘要:Chen L, Mao W, Ren C, Li J, Zhang J. Comprehensive Insights that Targeting PIM for Cancer Therapy: Prospects and Obstacles. J Med Chem. 2024 Jan 11;67(1):38–64. doi: 10.1021/acs.jmedchem.3c01802.
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