CAS: 22204-24-6; (E)-1-Methyl-2-(2-(Thiophen-2-yl)Vinyl)-1,4,5,6-Tetrahydropyrimidine 4,4'-Methylenebis(3-Hydroxy-2-Naphthoate)

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    专利信息


    专利号:US-2004110228-A1
    优先权日:2002-04-01
    标 题:Combinatorial organic synthesis of unique biologically active compounds
    发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
    摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

    专利号:WO-2025056767-A1
    优先权日:2023-09-15
    标题 :Process for the preparation of enantiomerically enriched aliphatic amines
    发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.

    专利号:WO-2021074309-A1
    优先权日:2019-10-16
    标 题:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives as fungicides for combating specific phytopathogens
    发明人:WEISS MATTHIAS; QUARANTA LAURA; BOU HAMDAN FARHAN; MAHAJAN ATUL; WILLIAMS SIMON; KILARU JAGADEESH; SEN INDIRA; BIERI STEPHANE; DIGGELMANN MARTIN
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:1-(3-quinolyl)-3,4-dihydroisoquinoline derivatives of formula (I) as well as a method of combating, preventing or controlling the phytopathogens Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale), which comprises applying to the phytopathogen, to the locus of the phytopathogen, or to a plant susceptible to attack by the phytopathogen, or to propagation material thereof, a fungicidally effective amount of a 1-(3-quinolyl)-3,4-dihydroisoquinoline derivative of formula (I). The present description discloses the synthesis of exemplary compounds, formulation examples, relevant biological data (antifungal activity against Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale) when spayed on plants), as well as comparative data against three prior art compounds (e.g. pages 52 to 85; formulation examples; examples A1 to A3; table E; compounds E.01 to E.187; biological examples). Exemplary compounds are e.g.: 5-bromo-1-(8-fluoro-3-quinolyl)spiro[4H-isoquinoline-3,1'- cyclopropane] (example A1) 5-bromo-1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline (example A2) 1-(8-fluoro-3-quinolyl)-3,3-dimethyl-4H-isoquinoline-5-carbonitrile (example A3)

    专利号:WO-2021074311-A1
    优先权日:2019-10-16
    标题:1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives as fungicides for combating specific phytopathogens
    发明人:WEISS MATTHIAS; QUARANTA LAURA; BOU HAMDAN FARHAN; MAHAJAN ATUL; WILLIAMS SIMON; KILARU JAGADEESH; BIERI STEPHANE; DIGGELMANN MARTIN
    权利人:SYNGENTA CROP PROTECTION AG
    摘要:1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) as well as a method of combating, preventing or controlling the phytopathogens Mycosphaerella graminicola (Septoria tritici), Fusarium culmorum, Gibberella zeae (Fusarium graminearum) and Monographella nivalis (Microdochium nivale), which comprises applying to the phytopathogen, to the locus of the phytopathogen, or to a plant susceptible to attack by the phytopathogen, or to propagation material thereof, a fungicidally effective amount of a 1-(3-quinolyl)-1,2,3,4-tetrahydroisoquinoline derivatives of formula (I). The present description discloses the synthesis of exemplary compounds, formulation examples, relevant biological data (antifungal activity against Mycosphaerella graminicola, Monographella nivalis, Fusarium culmorum and/or Gibberella zeae when spayed on plants) (e.g. pages 47 to 55; examples A1 and A2; compounds E.01 to E.17; table E). An exemplary compounds is e.g.: 3-(5-bromo-3,3-dimethyl-2,4-dihydro-1 H-isoquinolin-1-yl)-8-fluoro- quinoline (example A1)

    专利号:US-9907753-B2
    优先权日:2010-03-19
    标 题 :Lipid vesicle compositions and methods of use
    发明人:IRVINE DARRELL J; MOON JAEHYUN
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

    专利号:US-2007148246-A1
    优先权日:2005-08-11
    标题:Nucleic Acid-Based Matrixes
    发明人:LUO DAN; LI YOUGEN
    权利人:LUO DAN; LI YOUGEN
    摘要:Various nucleic acid-based matrixes are provided, comprising nucleic acid monomers as building blocks, as well as nucleic acids encoding proteins, so as to produce novel biomaterials. Methods of utilizing such biomaterials include delivery of biologically active agents, cell and tissue culture, and cell-free protein synthesis.
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    主要参考文献


    1: Moser W, Sayasone S, Xayavong S, Bounheuang B, Puchkov M, Huwyler J, Hattendorf J, Keiser J. Efficacy and tolerability of triple drug therapy with albendazole, pyrantel pamoate, and oxantel pamoate compared with albendazole plus oxantel pamoate, pyrantel pamoate plus oxantel pamoate, and mebendazole plus pyrantel pamoate and oxantel pamoate against hookworm infections in school-aged children in Laos: a randomised, single-blind trial. Lancet Infect Dis. 2018 Jul;18(7):729-737. doi: 10.1016/S1473-3099(18)30220-2. Epub 2018 Apr 16. Available from http://www.ncbi.nlm.nih.gov/books/NBK501733/ doi: 10.1371/journal.pntd.0006506. eCollection 2018 May.
    4: Arion A, Fernández-Varón E, Cárceles CM, Gagyi L, Ognean L. Pharmacokinetics of praziquantel and pyrantel pamoate combination following oral administration in cats. J Feline Med Surg. 2018 Oct;20(10):900-904. doi: 10.1177/1098612X17734065. Epub 2017 Oct 11. doi: 10.2460/javma.251.10.1188.

    合成参考文献


    参考文献:10.1097/inf.0b013e31821e52e9
    摘要:Messina AF, Wehle FJ, Intravichit S, Washington K. Moniliformis moniliformis infection in two Florida toddlers. Pediatr Infect Dis J. 2011 Aug;30(8):726–7. doi: 10.1097/inf.0b013e31821e52e9.
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