CAS: 52128-35-5; 5-Methyl-6-(((3,4,5-Trimethoxyphenyl)Amino)Methyl)Quinazoline-2,4-Diamine

该化合物是一种合成化合物,被归类为抗叶酸盐,主要用于治疗某些类型的癌症和自体免疫疾病,作为二氢氟酸盐还原消化酶抑制剂,破坏叶酸新陈代谢,从而抑制快速分解细胞中的DNA合成.这一机制使其对肿瘤细胞有效.三氯硝酸盐通常与其他乳胶化剂结合施用,以提高其功效.该化合物的特点是其溶性以及渗透细胞膜的能力,这有利于其在细胞内采取行动.其分子重量相对较低,并且通常由于其药用动力特性而静脉注射.副作用可能包括叶酸抑制,胃肠扰动和潜在的肝中毒,需要在治疗期间进行仔细监测.

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CAS号253-82-7 喹唑啉 | CAS号24313-88-0 3,4,5-三甲氧基苯胺 | CAS号18917-72-1 2,4-二氨基-5-甲基-6-喹唑啉甲腈

合成工艺路线路线简述

    📜2,4-二氨基-5-甲基喹唑啉-6-甲腈置于2,4-二氨基-5-甲基喹唑啉-6-甲腈体系中,用52的收率获得产物三甲曲沙
    参考文献:J. Labelled. Compd. Rad. 1991,29,415-429
    标题:J. Labelled. Compd. Rad. 1991,29,415-429

    海关参考信息

    专利信息


    专利号:US-2004242897-A1
    优先权日:2002-07-31
    标题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-2012177593-A1
    优先权日:2009-07-20
    标 题 :Synthesis of dendrimer conjugates
    发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
    权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
    摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

    专利号:WO-2004011474-A1
    优先权日:2002-07-31
    标题:Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-6653468-B1
    优先权日:2002-07-31
    标 题 :Universal support media for synthesis of oligomeric compounds
    发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH
    权利人:ISIS PHARMACEUTICALS INC
    摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Blanke CD, Chansky K, Christman KL, Hundahl SA, Issell BF, Van Veldhuizen PJ Jr, Budd GT, Abbruzzese JL, Macdonald JS. S9511: a Southwest Oncology Group phase II study of trimetrexate, 5-fluorouracil, and leucovorin in unresectable or metastatic adenocarcinoma of the stomach. Am J Clin Oncol. 2010 Apr;33(2):117-20. doi: 10.1097/COC.0b013e318199fb84.
    2: Senkovich O, Schormann N, Chattopadhyay D. Structures of dihydrofolate reductase-thymidylate synthase of Trypanosoma cruzi in the folate-free state and in complex with two antifolate drugs, trimetrexate and methotrexate. Acta Crystallogr D Biol Crystallogr. 2009 Jul;65(Pt 7):704-16. doi: 10.1107/S090744490901230X. Epub 2009 Jun 20. doi: 10.1097/QAD.0b013e32832d0792.
    7: Szabolcs P, Park KD, Marti L, Deoliveria D, Lee YA, Colvin MO, Kurzberg J. Superior depletion of alloreactive T cells from peripheral blood stem cell and umbilical cord blood grafts by the combined use of trimetrexate and interleukin-2 immunotoxin. Biol Blood Marrow Transplant. 2004 Nov;10(11):772-83.

    合成参考文献


    摘要:McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 93. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1993 (Plus Supplements, 1993)., p. 626
    摘要:US Pharmacopeial Convention; US Pharmacopeia Dispensing Information (USP DI); Drug Information for the Health Care Professional 12th ed, V.I p.V/56 (1992)
    摘要:Ellenhorn, M.J. and D.G. Barceloux. Medical Toxicology - Diagnosis and Treatment of Human Poisoning. New York, NY: Elsevier Science Publishing Co., Inc. 1988., p. 68
    摘要:HANSCH,C ET AL. (1995)
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