CAS: 153168-05-9; 3-(3,5-Dimethyl-4-(3-(3-Methylisoxazol-5-yl)Propoxy)Phenyl)-5-(Trifluoromethyl)-1,2,4-Oxadiazole

该化合物是一种抗病毒化合物,主要以其针对造成各种呼吸道感染的肠道病毒和犀牛病毒的活动而闻名;它通过抑制病毒复制,特别是针对病毒的粘合,防止病毒进入宿主细胞所需的松动过程;Pleconaril的特点是水溶性相对较低,这可能影响其生物利用率和药物应用中的配方;该化合物的分子重量将它归类为小分子,并表现出温和的亲脂性,允许可能的口服生物利用率;其化学结构包括一条和环丙烷混合物,有助于其独特的药理特性;虽然在治疗病毒感染的临床试验中,胸膜显示出希望,但其使用有限,原因是对抗药性的关切和需要进一步研究,以确定其在更广泛的病人人口中的效率和安全状况.

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2-(2,2,2-trifluoroethylidene)-1,3-dithiane oxy>benzenecarboxamide imineN-hydroxy-3,5-dimethyl-4-3-(3-methyl-5-isoxazolyl)propyloxybenzenecarboxamide imine trifluoroacetic anhydride

合成工艺路线路线简述

    N-Hydroxy-3,5-Dimethyl-4-<<3-(3-Methyl-5-Isoxazolyl)Propyl>Oxy>Benzenecarboxamide Imine 反应生成普可那利
    参考文献:1,2,4-Oxadiazolyl-Phenoxyalkylisoxazoles And Their Use As Antiviral
    标题:1,2,4-Oxadiazolyl-Phenoxyalkylisoxazoles And Their Use As Antiviral
    摘要:式为##str1##的化合物,其中:R.Sub.1是烷基,烷氧基,羟基,环烷基,羟基烷基,烷氧基烷基或羟基烷氧基;Y是3至9个碳原子的脂肪基;R.Sub.2和r.Sub.3独立地是氢,烷基,烷氧基,卤素,三氟甲基和硝基;R.Sub.4是烷氧基,羟基,卤代甲基,二卤代甲基,三卤代甲基,环烷基,烷氧羰基,羟基烷基,烷氧基烷基,烷基羧酸酯氧基烷基,氰基,2,2,2-三氟乙基,(4-甲基苯基)磺酰氧甲基,N.Dbd.Q或con.Dbd.Q,其中n.Dbd.Q是氨基,烷基氨基或二烷基氨基;或其药学上可接受的酸加成盐可用作抗病毒剂.

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    专利信息


    专利号:US-2016185745-A1
    优先权日:2013-08-07
    标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
    发明人:SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
    权利人:UNIV TEXAS
    摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

    专利号:WO-9964032-A1
    优先权日:1998-06-08
    标题 :Combinatorial synthesis of multibinding libraries
    发明人:CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
    权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
    摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

    专利号:WO-2016202721-A1
    优先权日:2015-06-16
    标 题:Salts of (s)-4-[(r)-6-(2-chloro-4-fluoro-phenyl)-5-methoxycarbonyl-2-thiazol-2-yl-3,6- dihydro-pyrimidin-4-ylmethyl]-morpholine-3-carboxylic acid, salt former and methods for preparing and using the same
    发明人:EGLI ANDRé; DIODONE RALPH; WUITSCHIK GEORG
    权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE
    摘要:The present invention relates to salts of (S)-4-[(R)-6-(2-Chloro-4-fluoro-phenyl)-5- methoxycarbonyl-2-thiazol-2-yl-3,6-dihydro-pyrimidin-4-ylmethyl]-morpholine-3-carboxylic acid and an acid, the synthesis of the acid salts, and their use for the treatment of pathological disorders, particularly hepatitis B (HBV) infection.

    专利号:US-9994558-B2
    优先权日:2013-09-20
    标题 :Multicyclic compounds and methods of using same
    发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
    权利人:KARYOPHARM THERAPEUTICS INC
    摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

    专利号:US-10736911-B2
    优先权日:2015-12-29
    标题 :Use of a DHODH inhibitor in combination with an inhibitor of pyrimidine salvage
    发明人:DEANS RICHARD; OKESLI AYSE; MORGENS DAVID; KHOSLA CHAITAN; BASSIK MICHAEL C
    权利人:UNIV LELAND STANFORD JUNIOR
    摘要:Compounds and methods are provided for the treatment of pathogenic virus infections or cancer. The formulations combine an inhibitor of de novo pyrimidine synthesis, and an inhibitor of a pyrimidine salvage pathway enzyme.

    专利号:US-10065924-B2
    优先权日:2014-07-22
    标 题 :Preparation and biological evaluation of viridicatumtoxin analogs
    发明人:NICOLAOU KYRIACOS C; HALE CHRISTOPHER R H; NILEWSKI CHRISTIAN; IOANNIDOU HERAKLIDIA; EL MARROUNI ABDELLATIF
    权利人:UNIV RICE WILLIAM M
    摘要:In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.
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    主要参考文献


    1: Billich A. Pleconaril Sanofi Synthélabo/ViroPharma. Curr Opin Investig Drugs. 2000 Nov;1(3):303-7. 29(11):2902-2908. doi: 10.1038/s41591-023-02576-1. Epub 2023 Oct 4.
    3: Florea NR, Maglio D, Nicolau DP. Pleconaril, a novel antipicornaviral agent. Pharmacotherapy. 2003 Mar;23(3):339-48. doi: 10.1592/phco.23.3.339.32099.
    4: Ianevski A, Frøysa IT, Lysvand H, Calitz C, Smura T, Schjelderup Nilsen HJ, Høyer E, Afset JE, Sridhar A, Wolthers KC, Zusinaite E, Tenson T, Kurg R, Oksenych V, Galabov AS, Stoyanova A, Bjørås M, Kainov DE. The combination of pleconaril, rupintrivir, and remdesivir efficiently inhibits enterovirus infections in vitro, delaying the development of drug-resistant virus variants. Antiviral Res. 2024 Apr;224:105842. doi: 10.1016/j.antiviral.2024.105842. Epub 2024 Feb 26. 21(1):127. doi: 10.1186/s12887-021-02599-y.

    合成参考文献


    参考文献:10.1007/s13312-012-0216-0
    摘要:Sharma S, Mishra D, Aneja S, Kumar R, Jain A, Vashishtha VM; Expert Group on Encephalitis, Indian Academy of Pediatrics. Consensus guidelines on evaluation and management of suspected acute viral encephalitis in children in India. Indian Pediatr. 2012 Nov;49(11):897–910. doi: 10.1007/s13312-012-0216-0.
    参考文献:10.1053/spid.2002.29756
    摘要:Sawyer MH. Enterovirus infections: Diagnosis and treatment. Seminars in Pediatric Infectious Diseases. 2002 Jan;13(1):40–7. doi: 10.1053/spid.2002.29756.
    参考文献:10.1007/s11908-002-0023-1
    摘要:Romero JR. Diagnosis and Management of Enteroviral Infections of the Central Nervous System. Curr Infect Dis Rep. 2002 Aug;4(4):309–16. doi: 10.1007/s11908-002-0023-1.
    参考文献:10.1007/s11908-002-0027-x
    摘要:Lu HZ, Bloch KC, Tang YW. Molecular Techniques in the Diagnosis of Central Nervous System Infections. Curr Infect Dis Rep. 2002 Aug;4(4):339–50. doi: 10.1007/s11908-002-0027-x.
    参考文献:10.1016/s1473-3099(02)00326-2
    摘要:The Lancet Infectious Diseases. Cold comfort. The Lancet Infectious Diseases. 2002 Jul;2(7):385. doi: 10.1016/s1473-3099(02)00326-2.
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