CAS: 1201438-56-3; (S)-3-(1-((9H-Purin-6-yl)Amino)Ethyl)-8-Chloro-2-Phenylisoquinolin-1(2H)-One

该化合物是一种小分子抑制剂,它针对磷酰三基酶(PI3K)路径,特别是三角形和伽马色异形,主要调查其在血友恶性肿瘤中的潜在治疗应用,包括某些类型的淋巴瘤和白血病;IPI-145通过干扰促进细胞扩散和癌症细胞生存的信号路径,表明抗扰动活动;该化合物通常通过口述方式进行,并在临床试验中评估其功效和安全性能;其行动机制包括抑制PI3K,它在各种细胞过程,包括新陈代谢,生长和存活过程中起着关键作用;与许多有针对性的疗法一样,其副作用可能包括免疫反应,胃肠紊乱和血液学变化;持续的研究继续探索其充分潜力,并优化其利用,同时结合其他疗法,加强肿瘤治疗结果.

结构式图片

欧盟法规

C&L通报

上下游产品

aniline 2-chloro-6-methylbenzoic acid (S)-3-(1-aminoethyl)-8-chloro-2-phenylisoquinoline-1(2H)-one 8-chloro-2-phenyl-3-((1S)-1-(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-ylamino)ethyl)isoquinolin-1(2H)-one(S)-3-(1-((9H-purin-6-yl)amino)ethyl)-2-phenyl-8-(pyrrolidin-1-yl)isoquinolin-1(2H)-one (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-2-phenyl-8-(1H-pyrazol-4-yl)isoquinolin-1(2H)-one (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-1-oxo-2-phenyl-1,2-dihydroisoquinoline-8-carbaldehyde (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-1-oxo-2-phenyl-1,2-dihydroisoquinoline-8-carbonitrile

合成工艺路线路线简述

    苯胺置于n,N-二甲基甲酰胺 盐酸,正丁基锂,草酰氯,水,三乙胺体系中,用 四氢呋喃,乙醇,正己烷,二氯甲烷,正丁醇 用作溶剂,化学反应 24.0H,反应生成(S)-3-(1-((9H-嘌呤-6-基)氨基)乙基)-8-氯-2-苯基-1(2H)-异喹啉酮
    参考文献: Chemical Compounds,Compositions And Methods For Kinase Modulation[fr] Composés Chimiques,Compositions Et Procédés Pour Modulation De Kinases
    标题: Chemical Compounds,Compositions And Methods For Kinase Modulation[fr] Composés Chimiques,Compositions Et Procédés Pour Modulation De Kinases
    摘要:本文描述了调节激酶活性的化合物,包括pi3激酶活性,以及与激酶活性相关的疾病和病况的化合物,药物组合物和治疗方法,包括pi3激酶活性.

    海关参考信息

    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    专利号:US-12441733-B2
    优先权日:2018-03-26
    标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
    发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
    权利人:NOVARTIS AG
    摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

    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-10370455-B2
    优先权日:2014-12-05
    标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists
    发明人:MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL
    权利人:IMMUNEXT INC
    摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
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    主要参考文献


    1: Ford J, Koh MJ, Lenart AW, MacVicar CT, Chopra K, Meharwal A, Sorial MN, Merrill MH, Rider AB, Sohani A, McCabe SM, Nemec RA, Iwasaki M, Mistry D, Kariya KM, Chen S, Barnes JA, McAfee S, Chen YB, Wong CY, Nasto K, Jacobsen ED, Jain S. Real-world Evidence of Duvelisib and Romidepsin in Relapsed/Refractory Peripheral and Cutaneous T-cell Lymphomas. Blood Adv. 2025 Jun
    17:bloodadvances.2025016347. doi: 10.1182/bloodadvances.2025016347. Epub ahead of print.
    32:100222. doi: 10.1016/j.slasd.2025.100222. Epub 2025 Feb 23.
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