CAS: 56741-95-8; 2-Amino-5-Bromo-4-Hydroxy-6-Phenylpyrimidine

该化合物是一种主要因其免疫细胞特性而得到承认的合成化学化合物,它属于火药衍生物类别,其特点是能够加强免疫反应,使其在免疫治疗领域引起兴趣;该化合物在治疗各种情况,包括某些类型的癌症和病毒感染方面的潜在应用已经进行了研究;溴蛋白在水中表现出相对较低的溶解性,这可能会影响其生物利用率和药用植物;其行动机制包括刺激免疫细胞,特别是T淋巴细胞,从而促进增强免疫反应;此外,溴蛋白因的安全特征和潜在副作用已经受到调查,这是治疗用途的重要考虑因素;

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2-amino-6-phenyl-3H-pyrimidin-4-one ethyl 3-oxo-3-phenylpropionate benzoyl chloride methyl 3-oxo-3-phenylpropionate 2-succinimido-5-bromo-6-phenyl-4(3H)-pyrimidinone 2-(acetylamino)-5-bromo-6-phenyl-4(3H)-pyrimidinone pyrimidine7-bromo-4,6-dioxo-8-phenyl-2,3,4,6-tetrahydro-1H-pyrimido1,2-apyrimidine 2-amino-6-phenyl-3H-pyrimidin-4-one

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    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-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.

    专利号:US-9220714-B2
    优先权日:2006-03-16
    标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
    发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
    权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
    摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

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    主要参考文献


    1: Suzuki H, Mochizuki A, Yoshimura K, Miyamoto Y, Kaneko K, Inoue T, Chikazu D, Takami M, Kamijo R. Bropirimine inhibits osteoclast differentiation through production of interferon-β. Biochem Biophys Res Commun. 2015 Nov 6;467(1):146-51. doi: 10.1016/j.bbrc.2015.09.092. Epub 2015 Sep 21. doi: 10.1016/j.jim.2014.10.011. Epub 2014 Oct 30. doi: 10.1016/j.jim.2013.08.004. Epub 2013 Aug 15.
    5: Kassouf W, Kamat AM. Current state of immunotherapy for bladder cancer. Expert Rev Anticancer Ther. 2004 Dec;4(6):1037-46. Review. Review. Review. Review. Review. Review. Spanish. Review. Review. Japanese.

    合成参考文献


    摘要:Drugs of the Future., 9(567), 1984
    参考文献:10.1021/jm00150a018
    摘要:Skulnick HI, Weed SD, Eidson EE, Renis HE, Wierenga W, Stringfellow DA. Pyrimidinones. 1. 2-Amino-5-halo-6-aryl-4(3H)-pyrimidinones. Interferon-inducing antiviral agents. J Med Chem. 1985 Dec;28(12):1864–9. doi: 10.1021/jm00150a018.
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