CAS: 1013101-36-4; 2-Amino-8-(Rel-(1R,4R)-4-(2-Hydroxyethoxy)Cyclohexyl)-6-(6-Methoxypyridin-3-yl)-4-Methylpyrido[2,3-D]Pyrimidin-7(8H)-One

该化合物是其潜在的治疗应用,被归类为小分子,并被公认为某些蛋白性动脉的选择性抑制器,这些蛋白性酶在细胞生长和分裂等各种细胞过程中至关重要.该化合物的结构具有有助于其生物活动和选择性的特定功能组.在临床前研究中,PF-04691502在调控与癌症和其他疾病相关的途径方面显示出希望,使其成为药物开发的进一步调查的候选对象.其溶性,稳定性和药用植物特性是影响其功效和安全特征的基本要素.随着研究的继续进行,了解该化合物的行动机制和潜在副作用对于其在临床环境中的进步至关重要.

结构式图片

上下游产品

2-methoxy-pyridine-5-boronic acid

合成工艺路线路线简述

    ,2-甲氧基-5-吡啶硼酸置于2-甲氧基-5-吡啶硼酸体系中,用93的收率获得2-氨基-8-[反式-4-(2-羟基乙氧基)环己基]-6-(6-甲氧基-3-吡啶基)-4-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮
    参考文献:4-Methylpyridopyrimidinone Compounds
    标题:4-Methylpyridopyrimidinone Compounds
    摘要:本发明涉及公式(i)的新型4-甲基吡啶嘧啶酮化合物及其盐,它们的合成以及它们作为磷脂酰肌醇3-激酶α(pi3-Kα)抑制剂的用途.

    海关参考信息

    专利信息


    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:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    专利号:US-12180228-B2
    优先权日:2019-06-05
    标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
    发明人:MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

    专利号:US-2022047711-A1
    优先权日:2018-12-10
    标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
    发明人:SADOWSKY JACK; ZACHARIAS NEELIE TYANA
    权利人:GENENTECH INC
    摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.

    专利号:CN-118922420-A
    优先权日:2022-03-25
    标题 :Synthesis of TYK2 inhibitors and their intermediates
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    主要参考文献


    1: Fan Z, Tong Y, Yang Z, Wang S, Huang T, Yang D, Ni Q, Zhang M, Li D, Yang M, Fan X. Inhibitor PF-04691502 works as a senolytic to regulate cellular senescence. Exp Gerontol. 2024 Feb;186:112359. doi: 10.1016/j.exger.2024.112359. Epub 2024 Jan 7. 23(1):157. doi: 10.1186/s12876-023-02815-2.
    3: Li Z, Zhou H, Xia Z, Xia T, Du G, Franziska SD, Li X, Zhai X, Jin B. HMGA1 augments palbociclib efficacy via PI3K/mTOR signaling in intrahepatic cholangiocarcinoma. Biomark Res. 2023 Mar 29;11(1):33. doi: 10.1186/s40364-023-00473-w. Erratum in: Biomark Res. 2024 Feb 16;12(1):27. doi: 10.1186/s40364-024-00574-0.
    4: Yang Q, Ma X, Xiao Y, Zhang T, Yang L, Yang S, Liang M, Wang S, Wu Z, Xu Z, Sun Z. Engineering prodrug nanomicelles as pyroptosis inducer for codelivery of PI3K/mTOR and CDK inhibitors to enhance antitumor immunity. Acta Pharm Sin B. 2022 Jul;12(7):3139-3155. doi: 10.1016/j.apsb.2022.02.024. Epub 2022 Feb 26.

    合成参考文献


    参考文献:10.1158/1535-7163.mct-11-0185
    摘要:Yuan J, Mehta PP, Yin MJ, Sun S, Zou A, Chen J, Rafidi K, Feng Z, Nickel J, Engebretsen J, Hallin J, Blasina A, Zhang E, Nguyen L, Sun M, Vogt PK, McHarg A, Cheng H, Christensen JG, Kan JL, Bagrodia S. PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity. Mol Cancer Ther. 2011 Nov;10(11):2189–99. doi: 10.1158/1535-7163.mct-11-0185.
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