CAS: 120685-11-2; N-((5S,6R,7R,9R)-6-Methoxy-5-Methyl-14-Oxo-6,7,8,9,15,16-Hexahydro-5H,14H-17-Oxa-4B,9A,15-Triaza-5,9-Methanodibenzo[b,H]Cyclonona[jkl]Cyclopenta[e]-As-Indacen-7-yl)-N-Methylbenzamide

该化合物是一种小分子性细胞抑制剂,针对多种受体性强效激素性动脉,包括FLT3,KIT和PDGFR,主要用于治疗急性流血性白血病(AML),使用FLT3突变和先进的系统性囊肿症(SM);Midostaurin通过抑制诱发恶性细胞扩散和存活的异常信号路径而进行工作,其主要优势包括显示其与FLT3变异的AML标准化疗相结合的功效,提高了总体存活率;该化合物还展示了打击KIT D816V突变的活动,使其对SM治疗具有价值;Midostaurin是口服的,为病人提供方便,并具有精密的药用植物基因特征,支持其在定向治疗疗法中的临床效用.

结构式图片

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    专利信息


    专利号:WO-2025038767-A1
    优先权日:2023-08-14
    标 题:Cell-free synthesis platform for synthetically dimierized, clickable fragment antigen-binding (fab) fragments
    发明人:THAMES ARIEL; RISCHE CLAYTON; JEWETT MICHAEL; BOCHNER BRUCE
    权利人:UNIV NORTHWESTERN
    摘要:Disclosed are components, systems, methods, and kits for synthesis of diamerized, clickable antigen binding fragments, such as Fab fragments, and uses thereof. The components, systems, methods, and kits disclosed herein utilize cell-free protein synthesis (CFPS) systems and methods to produce clickable antigen binding fragments.

    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:US-2025049791-A1
    优先权日:2023-08-03
    标题:Synthesis of MEK7 Inhibitors and methods of Use Thereof
    发明人:SCHEIDT KARL A; KIM DALTON ROBERT; ORR MEGHAN JO
    权利人:UNIV NORTHWESTERN
    摘要:Disclosed herein are 4-phenoxypyrimidine compounds and derivatives thereof for use as inhibitors of mitogen-activated protein kinase 7 (MEK7). The disclosed compounds and pharmaceutical compositions thereof may be used in methods for treating a disease or disorder associated with MEK7 activity, including cell proliferative diseases and disorders associated with MEK7 activity, such as cancer.

    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Wang ES. Beyond midostaurin: Which are the most promising FLT3 inhibitors in AML? Best Pract Res Clin Haematol. 2019 Dec;32(4):101103. doi: 10.1016/j.beha.2019.101103. Epub 2019 Oct 18. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK548874/ doi: 10.18773/austprescr.2019.017. Epub 2019 Feb 28. Review.
    4: Sly N, Gaspar K. Midostaurin for the management of FLT3-mutated acute myeloid leukemia and advanced systemic mastocytosis. Am J Health Syst Pharm. 2019 Feb 9;76(5):268-274. doi: 10.1093/ajhp/zxy050. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK500909/ doi: 10.1182/bloodadvances.2017011080. Review. Erratum in: Blood Adv. 2018 Apr 10;2(7):787.
    7: Weisberg E, Sattler M, Manley PW, Griffin JD. Spotlight on midostaurin in the treatment of FLT3-mutated acute myeloid leukemia and systemic mastocytosis: design, development, and potential place in therapy. Onco Targets Ther. 2017 Dec 29;11:175-182. doi: 10.2147/OTT.S127679. eCollection 2018. Review.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
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