CAS: 72732-56-0; 6-(2,5-Dimethoxybenzyl)-5-Methylpyrido[2,3-D]Pyrimidine-2,4-Diamine

该化合物是一种合成化合物,被归类为抗蛋白,主要用于治疗某些类型的癌症和抗微生物剂,以其结构上与叶酸相似而著称,允许它通过抑制二氢氟酸还原酶(一种对DNA复制和细胞分解至关重要的酶)干扰核酸合成.这一机制使Piritrexim对迅速分裂的细胞(如肿瘤和某些病原体中发现的细胞)有效.该化合物通常在临床环境中施用,其药理植物因施用方式和途径不同而不同.已经研究过它治疗各种恶性病和感染的潜力,尽管其使用可能受到副作用和某些情况下抗药性发展的限制.和许多甲虫一样,对病人进行仔细监测对于管理毒性和确保治疗效果至关重要.

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CAS号72676-85-8 2,4-diamino-5-m... | CAS号93-02-7 2,5-二甲氧基苯甲醛 | CAS号72676-82-5 ethyl α-(2,5-di... | CAS号72676-83-6 ethyl α-acetyl-... | CAS号72676-84-7 2,4-diamino-5-m... | CAS号847234-66-6 2-amino-3-cyano... | CAS号71493-76-0 2-氨基-3-氰基-4-甲基吡啶 | CAS号410547-37-4 2-(4,4-dimethox... | CAS号180994-87-0 2-氨基-5-溴-4-甲基烟腈

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    专利信息


    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:US-7256197-B2
    优先权日:2001-10-12
    标 题 :Methods for synthesis of diarylmethanes
    发明人:ROSOWSKY ANDRE; CHEN HAN
    权利人:DANA FARBER CANCER INST INC
    摘要:The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; methods of preparation of dihydrofolate reductase inhibitors that include metal mediated cross coupling of an aromatic halide or heteroaromatic halide with an organozinc reagent; and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such dihydrofolate reductase inhibitors.

    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-5612217-A
    优先权日:1994-10-25
    标 题 :Streptomyces sp. MA 7074 (ATCC 55605) used for microbial synthesis of HIV protease inhibitors
    发明人:SHAFIEE ALI; CHEN SHIEH-SHUNG T; ARISON BYRON H; MILLER RANDALL R; GARRITY GEORGE M; HEIMBUCH BRIAN
    权利人:MERCK & CO INC
    摘要:Biotransformation products of a fermentation with culture MA7074 are potent HIV protease inhibitors. These products are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are 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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    主要参考文献


    1: Sigel CW, Macklin AW, Woolley JL Jr, Johnson NW, Collier MA, Blum MR, Clendeninn NJ, Everitt BJ, Grebe G, Mackars A, et al. Preclinical biochemical pharmacology and toxicology of piritrexim, a lipophilic inhibitor of dihydrofolate reductase. NCI Monogr. 1987;(5):111-20.
    4: Lassiter LK, Tummala MK, Hussain MH, Stadler WM, Petrylak DP, Carducci MA. Phase II open-label study of oral piritrexim in patients with advanced carcinoma of the urothelium who have experienced failure with standard chemotherapy. Clin Genitourin Cancer. 2008 Mar;6(1):31-5. doi: 10.3816/CGC.2008.n.005.
    7: Perkins W, Williams RE, Vestey JP, Tidman MJ, Layton AM, Cunliffe WJ, Saihan EM, Klaber MR, Manna VK, Baker H, et al. A multicentre 12-week open study of a lipid-soluble folate antagonist, piritrexim in severe psoriasis. Br J Dermatol. 1993 Nov;129(5):584-9.

    合成参考文献


    摘要:Proceedings of the American Association for Cancer Research., 25(310), 1984
    参考文献:10.1021/jm990079m
    摘要:Gangjee A, Adair O, Queener SF. Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase Inhibitors and Antitumor Agents: Synthesis and Biological Activities of 2,4-Diamino-5-methyl-6-[(monosubstituted anilino)methyl]- pyrido[2,3-d]pyrimidines. J. Med. Chem. 1999 Jun 09;42(13):2447–55. doi: 10.1021/jm990079m.
    参考文献:10.1007/bf00873124
    摘要:Schiesel JD, Carabasi M, Magill G, Casper E, Cheng E, Marks L, Feyzi J, Clendeninn NJ, Smalley RV. Oral piritrexim--a phase II study in patients with advanced soft tissue sarcoma. Invest New Drugs. 1992 Jul;10(2):97–8. doi: 10.1007/bf00873124.
    参考文献:10.1016/s0968-0896(02)00159-1
    摘要:Agrawal VK, Sohgaura R, Khadikar PV. QSAR studies on biological activity of piritrexim analogues against pc DHFR. Bioorganic & Medicinal Chemistry. 2002 Sep;10(9):2919–26. doi: 10.1016/s0968-0896(02)00159-1.
    参考文献:10.1007/s11030-008-9079-7
    摘要:Balalaie S, Abdolmohammadi S, Bijanzadeh HR, Amani AM. Diammonium hydrogen phosphate as a versatile and efficient catalyst for the one-pot synthesis of pyrano[2,3-d]pyrimidinone derivatives in aqueous media. Mol Divers. 2008 May;12(2):85–91. doi: 10.1007/s11030-008-9079-7.
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