CAS: 1334298-90-6; 2-(3-(4-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-yl)-1-(1-(3-Fluoro-2-(Trifluoromethyl)Isonicotinoyl)Piperidin-4-yl)Azetidin-3-yl)Acetonitrile

该化合物是麻风素1(JAK1)的选择性抑制剂,它在各种细胞细胞和生长因素的信号路径中发挥着关键作用;该化合物主要因其治疗自体免疫疾病和某些血友恶性肿瘤的治疗潜力而受到调查;该化合物具有一种有利的药用动因特征,其特点是口服生物利用率高,可控半衰期方便剂量治疗;该物质通常以平板形式施用,并在对诸如溃化性脊髓炎和风湿性关节炎等疾病的临床试验中进行了研究;其行动机制包括抑制JAK1的中间信号,这可以减少免疫反应的炎度和调控;与许多药剂一样,该物质的安全性和功效简介不断得到评估,关注潜在的副作用,包括感染和血液细胞数的变化;

结构式图片

上下游产品

2-(1-(1-(3-Fluoro-2-(Trifluoromethyl)Isonicotinoyl)Piperidin-4-yl)-3-(4-(7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-yl)Azetidin-3-yl)Acetonitrile 1334303-20-6
Tert-Butyl 4-{3-(Cyanomethyl)-3-[4-(7-{[2-(Trimethylsilyl) Ethoxy]Methyl}-7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-Yl]Azetidin-1-Yl}Piperidine-1-Carboxylate 1334303-18-2
2-(1-(1-(3-Fluoro-2-(Trifluoromethyl)Isonicotinoyl)Piperidin-4-yl)-3-(4-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)-1H-Pyrazol-1-yl)Azetidin-3-yl)Acetonitrile
Tert-Butyl 3-(4-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-yl)-3-(Cyanomethyl)Azetidine-1-Carboxylate
Tert-Butyl 3-(Cyanomethyl)-3-(4-(7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)-1H-Pyrazol-1-yl)Azetidine-1-Carboxylate 1187594-11-1
2-(1-(1-(3-Fluoro-2-(Trifluoromethyl)Isonicotinoyl)Piperidin-4-yl)Azetidin-3-Ylidene)Acetonitrile
4-(1-(1-乙氧基乙基)-1H-吡唑-4-基)-7-(2-(三甲基硅基)乙氧基)甲基)-7H-吡咯并[2,3-D]嘧啶 4-(1-(1-Ethoxyethyl)-1H-Pyrazol-4-yl)-7-((2-(Trimethylsilyl)Ethoxy)Methyl)-7H-Pyrrolo[2,3-D]Pyrimidine 1187595-88-5
(3-Fluoro-2-(Trifluoromethyl)Pyridin-4-yl)(1,4-Dioxa-8-Azaspiro[4,5]Decan-8-yl)Methanone 1426436-72-7 1-(3-Fluoro-2-(Trifluoromethyl)Isonicotinoyl)Piperidin-4-One 1334303-99-9

合成工艺路线路线简述

    📜(3-Fluoro-2-(Trifluoromethyl)Pyridin-4-yl)(1,4-Dioxa-8-Azaspiro[4,5]Decan-8-yl)Methanone置于盐酸,水,三乙胺体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 10.58H,反应生成Hy-16997 (Incb3911)
    参考文献:Processes And Intermediates For Making A Jak Inhibitor
    标题:Processes And Intermediates For Making A Jak Inhibitor
    摘要:这项发明涉及制备{1-{1-[3-氟-2-(三氟甲基)异烟肼基]哌啶-4-基}-3-[4-(7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-基]氮杂环丙烯基}乙腈的过程和中间体,用于治疗与janus激酶(jak)活性相关的疾病,包括炎症性疾病,自身免疫性疾病,癌症和其他疾病.

    海关参考信息

    专利信息


    专利号:US-9732097-B2
    优先权日:2015-05-11
    标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor
    发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI
    权利人:INCYTE CORP
    摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.

    专利号:US-2022259212-A1
    优先权日:2019-07-11
    标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
    发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
    权利人:IDORSIA PHARMACEUTICALS LTD
    摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.

    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-11267824-B2
    优先权日:2017-08-17
    标 题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
    发明人:BOSS CHRISTOPH; BUR DANIEL; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
    权利人:IDORSIA PHARMACEUTICALS LTD
    摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.

    专利号:US-2016362426-A1
    优先权日:2015-05-11
    标题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor

    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: Yiu ZZ, Warren RB. Novel Oral Therapies for Psoriasis and Psoriatic Arthritis. Am J Clin Dermatol. 2016 Jun;17(3):191-200. doi: 10.1007/s40257-016-0179-3. doi: 10.1124/dmd.114.060673. Epub 2015 Jan 20. doi: 10.1517/14656566.2014.913024. Epub 2014 Apr 25. Review. A process for the preparation of key intermediates towards the synthesis of fluorotrifluoromethylisonicotinoylpiperi​dinylpyrrolopyrimidinylpyrazolylazetidin​ylacetonitrile for use as a JAK inhibitor. U.S. Pat. Appl. Publ. (2014), US 20140256941 A1 20140911.

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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