CAS: 644-62-2; 2-((2,6-Dichloro-3-Methylphenyl)Amino)Benzoic Acid

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2,6-dichloro-3-methylaniline Diphenyliodonium-2-carboxylate potassium o-bromobenzoate H-quinazoline-2,4-dione1,3-bis-(2,6-dichloro-3-methyl-phenyl)-1H-quinazoline-2,4-dione2-[(2,6-dichloro-3-methylphenyl)amino]benzoic acid,methyl ester 2-(2,6-Dichloro-3-methyl-phenylamino)-benzoic acid acetoxymethyl ester 2-(2,6-Dichloro-3-methyl-phenylamino)-benzoic acid benzoyloxymethyl ester ethoxymethyl N-(2,6-dichloro-m-tolyl)-anthranilate

合成工艺路线路线简述

    📜2-[(2,6-二氯-3-甲基苯基)氨基]苯甲酸甲酯置于一水合肼体系中,用 甲醇 作为反应溶剂,化学反应生成 甲氯芬那酸
    参考文献:Triazole Derivatives Of Fenamates As Antiinflammatory Agents
    标题:Triazole Derivatives Of Fenamates As Antiinflammatory Agents
    摘要:本发明涉及新颖的化合物,它们是1,2,4-三唑类化合物,芬酸酯衍生物以及其药学上可接受的补充物和碱盐,以及其药物组合物和使用方法.发明的化合物现已发现具有作为5-脂氧合酶和/或环氧合酶抑制剂的活性,可用于治疗受到这种抑制有利影响的疾病,包括炎症,关节炎,疼痛,发热等.

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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-8546532-B2
    优先权日:2008-04-17
    标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders
    发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS
    权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC
    摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.

    专利号:US-12264143-B2
    优先权日:2020-12-17
    标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
    发明人:SAMMIS GLENN M; ROGGEN MARKUS
    权利人:NALU BIO INC
    摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.

    专利号:US-10975069-B2
    优先权日:2014-04-01
    标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
    发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
    权利人:UNIV WASHINGTON
    摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

    专利号:US-2008287407-A1
    优先权日:2003-12-10
    标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
    发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
    权利人:NITROMED INC
    摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

    专利号:US-8304409-B2
    优先权日:2002-07-03
    标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use
    发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
    权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA
    摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

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    主要参考文献


    1: Soriano-Hernandez AD, Madrigal-Pérez D, Galvan-Salazar HR, Martinez-Fierro ML, Valdez-Velazquez LL, Espinoza-Gómez F, Vazquez-Vuelvas OF, Olmedo-Buenrostro BA, Guzman-Esquivel J, Rodriguez-Sanchez IP, Lara-Esqueda A, Montes-Galindo DA, Delgado-Enciso I. Anti-inflammatory drugs and uterine cervical cancer cells: Antineoplastic effect of meclofenamic acid. Oncol Lett. 2015 Oct;10(4):2574-2578. Epub 2015 Aug 7.
    2: Delgado-Enciso I, Soriano-Hernández AD, Rodriguez-Hernandez A, Galvan-Salazar HR, Montes-Galindo DA, Martinez-Martinez R, Valdez-Velazquez LL, Gonzalez-Alvarez R, Espinoza-Gómez F, Newton-Sanchez OA, Lara-Esqueda A, Guzman-Esquivel J. Histological changes caused by meclofenamic acid in androgen-independent prostate cancer tumors: evaluation in a mouse model. Int Braz J Urol. 2015 Sep-Oct;41(5):1002-7. doi: 10.1590/S1677-5538.IBJU.2013.00186. doi: 10.1093/nar/gku1276. Epub 2014 Dec 1.
    4: Sun H, Wen Y, Ning N, An J, Li J. Retinal toxicity associated with high dose of meclofenamic acid. Drug Chem Toxicol. 2013 Oct;36(4):461-5. doi: 10.3109/01480545.2013.776582. Epub 2013 Mar 27. doi: 10.1177/0960327112472997. Epub 2013 Apr 12. doi: 10.1016/j.neulet.2013.03.029. Epub 2013 Apr 6. doi: 10.1007/s11255-011-0012-0. Epub 2011 Jun 10. doi: 10.1016/j.jinorgbio.2011.05.025. Epub 2011 Jun 13. doi: 10.1016/j.jvir.2010.12.015. Epub 2011 Mar 17. doi: 10.1016/j.ijpharm.2010.11.043. Epub 2010 Dec 1. doi: 10.1016/j.jinorgbio.2009.01.014. Epub 2009 Jan 27. doi: 10.1152/jn.00112.2009. Epub 2009 Mar 11.

    合成参考文献


    参考文献:10.1124/jpet.111.183020
    摘要:Chi Y, Li K, Yan Q, Koizumi S, Shi L, Takahashi S, Zhu Y, Matsue H, Takeda M, Kitamura M, Yao J. Nonsteroidal Anti-Inflammatory Drug Flufenamic Acid Is a Potent Activator of AMP-Activated Protein Kinase. The Journal of Pharmacology and Experimental Therapeutics. 2011 Oct;339(1):257–66. doi: 10.1124/jpet.111.183020.
    参考文献:10.1007/s10549-005-9102-y
    摘要:Kato I, Chen G, Djuric Z. Non-steroidal anti-inflammatory drug (NSAID) use and levels of a lipid oxidation marker in plasma and nipple aspirate fluids. Breast Cancer Res Treat. 2006 May;97(2):145–8. doi: 10.1007/s10549-005-9102-y.
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