CAS: 1032568-63-0; 2-Amino-N-(7-Methoxy-8-(3-Morpholinopropoxy)-2,3-Dihydroimidazo[1,2-C]Quinazolin-5-yl)Pyrimidine-5-Carboxamide

该化合物是一种选择性磷酸丁酯3-kinase(PI3K)抑制剂,具体针对PI3K的α和三角洲异形.主要用于治疗复发或耐腐性淋巴瘤.该化合物显示出对PI3K-α和PI3K-的强烈抑制活动,它们经常在肝脏恶性疾病中受到控制.Copanlisib是静脉注射,允许有控制的药用植物和减少药物接触的变异性.其行动机制破坏了细胞扩散和存活的关键信号路径.临床研究表明,该物质在诱发肿瘤回归方面的效力,特别是对PI3K-α和PI3K-病人.该药物的选择性作用有助于与更广泛的血管抑制剂相比,形成可控的安全特征.

结构式图片

上下游产品

2-amino-pyrimidine-5-carboxylic acid 7-methoxy-8-[3-(morpholin-4-yl)propoxy]-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine 4-(benzyloxy)-3-methoxy-2-nitrobenzaldehyde 3-(benzyloxy)-6-(4,5-dihydro-1H-imidazol-2-yl)-2-methoxyaniline

合成工艺路线路线简述

    📜3-Methoxy-4-[3-(Morpholin-4-yl)Propoxy]-2-Nitrobenzaldehyde置于4-二甲氨基吡啶,C9H19N3*clh,5% Pd-1%fe/c,氢气,Potassium Carbonate,三乙胺体系中,用 乙醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,-5.0~75.0 °C,10.0 Mpa 条件下,反应 47.92H,反应生成库潘尼西
    参考文献: Synthesis Of Copanlisib And Its Dihydrochloride Salt[fr] Synthèse De Copanlisib Et De Son Sel Dichlorhydrate
    标题: Synthesis Of Copanlisib And Its Dihydrochloride Salt[fr] Synthèse De Copanlisib Et De Son Sel Dichlorhydrate
    摘要:本发明涉及一种制备科帕利西布和科帕利西布盐酸二水合物的新方法,涉及新的中间化合物,以及利用这些新的中间化合物制备科帕利西布的用途.

    专利信息


    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-10494372-B2
    优先权日:2014-11-07
    标 题 :Synthesis of copanlisib and its dihydrochloride salt
    发明人:PETERS JAN-GEORG; RUBENBAUER PHILIPP; GÖTZ DANIEL; GROSSBACH DANJA; MAIS FRANZ-JOSEF; SCHIRMER HEIKO; STIEHL JUERGEN; LOVIS KAI; LENDER ANDREAS; SEYFRIED MARTIN; ZWEIFEL THEODOR; MARTY MAURUS; WEINGÄRTNER GÜNTER
    权利人:Bayer Pharma AG
    摘要:The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.

    专利号:US-10035803-B2
    优先权日:2014-11-07
    标 题:Synthesis of copanlisib and its dihydrochloride salt
    发明人:PETERS JAN-GEORG; STIEHL JÜRGEN; LOVIS KAI
    权利人:Bayer Pharma AG
    摘要:The present invention relates to a novel method of preparing copanlisib, and copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib.

    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-2022118123-A1
    优先权日:2019-02-22
    标 题 :Combination of ar antagonists and targeted thorium conjugates
    发明人:HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
    权利人:BAYER AG; BAYER AS
    摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

    专利号:US-12390420-B1
    优先权日:2024-10-22
    标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
    发明人:EGUCHI MASAKATSU
    权利人:BRYET US INC
    摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

    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: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548413/ doi: 10.1038/s41420-019-0165-7. eCollection 2019.
    4: Eltantawy A, Vallejos X, Sebea E, Evans K. Copanlisib: An Intravenous Phosphatidylinositol 3-Kinase (PI3K) Inhibitor for the Treatment of Relapsed Follicular Lymphoma. Ann Pharmacother. 2019 Sep;53(9):954-958. doi: 10.1177/1060028019833992. Epub 2019 Feb 27. doi: 10.1016/j.clml.2018.11.021. Epub 2018 Nov 29.
    7: Dittakavi S, Mullangi R. LC-ESI-MS/MS determination of copanlisib, a novel PI3K inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice. Biomed Chromatogr. 2019 Apr;33(4):e4460. doi: 10.1002/bmc.4460. Epub 2019 Jan 7. doi: 10.1007/s00277-018-3547-7. Epub 2018 Nov 15. doi: 10.2147/DDDT.S142406. eCollection 2018. Review.

    合成参考文献


    摘要:Preliminary results of a phase II study of single agent Bay 80-6946, a Novel PI3K inhibitor, in patients with relapsed/refractory, indolent or aggressive lymphoma. Clin Adv Hematol Oncol. 2014 Feb;12(2 Suppl 5):14–6.
    参考文献:10.1007/s40487-021-00161-5
    摘要:Rodgers TD, Casulo C, Boissard F, Launonen A, Parreira J, Cartron G. Early Relapse in First-Line Follicular Lymphoma: A Review of the Clinical Implications and Available Mitigation and Management Strategies. Oncology and Therapy. 2021 Jul 28;9(2):329–46. doi: 10.1007/s40487-021-00161-5.
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