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    COMPOUNDS FOR TREATMENT OF HEPACI VIRUS INFECTION AND METHOD FOR DETERMINING THERAPY OF HEPACI VIRUS INFECTION, IN PARTICULAR, HCV INFECTION
    1.
    发明公开
    COMPOUNDS FOR TREATMENT OF HEPACI VIRUS INFECTION AND METHOD FOR DETERMINING THERAPY OF HEPACI VIRUS INFECTION, IN PARTICULAR, HCV INFECTION 审中-公开

    公开(公告)号：EP3670498A1

    公开(公告)日：2020-06-24

    申请号：EP18212936.1

    申请日：2018-12-17

    申请人： Gottfried Wilhelm Leibniz Universität Hannover ,  Twincore Zentrum für Experimentelle und Klinische Infektionsforschung GmbH

    发明人： PIETSCHMANN, Thomas ,  BANDA, Dominic ,  KIRSCHNING, Andreas ,  SOLODENKO, Wladimir

    IPC分类号： C07D229/02 ,  C07D249/06 ,  C07D295/096 ,  C07D295/135 ,  A61P31/14

    摘要： In a first aspect, the present invention relates to new compounds based on diphenylpiperazine and diphenylpiperidine structures. In particular, the present invention provides new flunarizine derivatives having improved hepaci virus infection inhibitory activity. In a further aspect, the present invention relates to a pharmaceutical composition containing said compound as well as the use of said pharmaceutical composition and the compounds according to the present invention in preventing or treating hepaci virus infection, in particular, HCV virus infection, like HCV of genotype 2. Moreover, a method for determining effectiveness of prophylactic or therapeutic treatment of hepaci virus, like HCV infection as well as a method for determining the therapy regimen of an individual afflicted with hepaci virus infection including HCV infection is provided. Said method is based on determining the sequence or interfacial hydrophobicity of the hepaci virus E1 protein. This may include determining the presence of mutations at predetermined positions of the E1 sequence. Based on determining the interfacial hydrophobicity of the E1 protein, the sensitivity to a diphenylpiperazine or diphenylpiperidine based hepaci virus inhibitor as well as a phenothiazine and cycloheptenepiperidine based hepaci virus inhibitor can be determined. When the central hydrophobicity region is disrupted or the hydrophobicity is below zero applying the Wimley-White hydropathy plot, or the mutations at positions 290, 299, 301 and 310 of SEQ ID No. 1 are present, it is submitted that the sensitivity against said compounds is reduced. Hence, it is possible to determine the therapy regimen of an individual afflicted with hepaci virus infection or being a risk of being afflicted with hepaci virus infection, in particular HCV infection like HCV genotype 2 infection.

    Perfluorodiaziridines and process for preparing them
    8.
    发明公开
    Perfluorodiaziridines and process for preparing them 失效
    Perfluordiaziridine和Verfahren zu ihrer Herstellung。

    公开(公告)号：EP0347885A1

    公开(公告)日：1989-12-27

    申请号：EP89111305.2

    申请日：1989-06-21

    申请人： AUSIMONT S.p.A.

    发明人： Navarrini, Walter, Dr. ,  Desmarteau, Darryl D., Dr.

    IPC分类号： C07D229/02

    CPC分类号： C07D229/00

    摘要： The present invention relates to novel perfluorodiaziridines having the formula:
    wherein:
    R₁ and R₂, the same or different from each other, represent a perfluoroalkyl group of from 1 to 10 carbon atoms, and
    R₃ represents a fluorine atom or a perfluoroalkyl group of from 1 to 9 carbon atoms.
    These perfluorodiaziridines are obtained by reacting perfluoro­aminooxaziridines with a source of fluoride ions.

    摘要翻译： 本发明涉及具有下式的新型全氟二氮吡啶：＆lt; CHEM＆gt;其中：R1和R2彼此相同或不同，表示1-10个碳原子的全氟烷基，R3表示氟原子或全氟烷基 1至9个碳原子。 这些全氟二氮杂是通过使全氟氨基吖唑啉与氟离子源反应得到的。