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    ANALOGS OF TERPENE TRILACTONES FROM GINKGO BILOBA AND RELATED COMPOUNDS AND USES THEREOF
    5.
    发明申请
    ANALOGS OF TERPENE TRILACTONES FROM GINKGO BILOBA AND RELATED COMPOUNDS AND USES THEREOF 审中-公开

    公开(公告)号：WO2003082185A3

    公开(公告)日：2003-10-09

    申请号：PCT/US2003/012651

    申请日：2003-03-28

    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK

    Inventor： STROMGAARD, Kristian ,  SUEHIRO, Makiko ,  NAKANISHI, Koji ,  VOGENSEN, Stine, B.

    IPC: C07D229/02

    Abstract: The subject invention provides compounds having the structure Formula (I): wherein R 1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R 2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R 3 is H or OH; R 4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R 1 , R 2 , R 3 , or R 4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C 1 -C 5 ) alkyl group, (C 2 -C 5 ) alkenyl, or a (C 2 -C 5 ) alkynyl, (C 1 -C 5 ) alkoxy, (C 2 -C 5 ) alkenyloxy, or (C 2 -C 5 ) alkynyloxy, -N3, -COR5, -CONR5R6, -CO2R5, -OCOR5, -NH(OH), -NR5R6, -NHCOR5, .N(OH)COR5, -CH2OR5, -OCH2CO2R5, -CH2SR5, -CH2NR5R6, -SR5, -OSR5, or -NR5SO2R6, where R5 and R6 are each independently hydrogen substituted or unsubstituted (C 1 -C 5 ) alkyl, (C 2 -C 5 ) alkenyl, or (C 2 -C 5 ) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1-C10) alkyl, (C1-C10) alkenyl, (C1-C10) alkynyl, -A-Ar, -A-Z-Ar, -SO 2 -Ar, or -A-NR 5 , or -R 7 , where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject.

    COMPOUNDS FOR TREATMENT OF HEPACI VIRUS INFECTION AND METHOD FOR DETERMINING THERAPY OF HEPACI VIRUS INFECTION, IN PARTICULAR, HCV INFECTION
    6.
    发明申请
    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：WO2020127211A2

    公开(公告)日：2020-06-25

    申请号：PCT/EP2019/085576

    申请日：2019-12-17

    Applicant: GOTTFRIED WILHELM LEIBNIZ UNIVERSITÄT HANNOVER ,  TWINCORE ZENTRUM FÜR EXPERIMENTELLE UND KLINISCHE INFEKTIONSFORSCHUNG GMBH

    Inventor： PIETSCHMANN, Thomas ,  BANDA, Dominic ,  KIRSCHNING, Andreas ,  SOLODENKO, Wladimir

    IPC: C07D229/02

    Abstract: 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 Wim ley-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.

    DETERMINING SMALL MOLECULE-PROTEIN AND PROTEIN-PROTEIN INTERACTIONS
    7.
    发明申请
    DETERMINING SMALL MOLECULE-PROTEIN AND PROTEIN-PROTEIN INTERACTIONS 审中-公开

    公开(公告)号：WO2018226828A2

    公开(公告)日：2018-12-13

    申请号：PCT/US2018/036256

    申请日：2018-06-06

    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE

    Inventor： WOO, Christina, M. ,  GAO, Jinxu

    IPC: C07D229/02 ,  A61K31/396

    Abstract: Provided herein are methods, systems, kits, and compositions useful for determining small molecule-protein interactions and protein-protein interactions. The photo-click tags provided herein can be conjugated to a small molecule or amino acid analog to provide compounds that can be integrated into a protein through photo-conjugation, allowing for identification of a small molecule-protein interaction or protein-protein interaction to elucidate the small molecules mechanism of action or the protein targeted by the small molecule. In some embodiments, the photo-click tags comprise a photo-conjugation moiety and a click chemistry handle, allowing for the attachment of various functional groups (e.g., affinity tags) to the small molecule or amino acid analog.

    AMIDOPHENOXYPROPANOLAMINES
    9.
    发明申请
    AMIDOPHENOXYPROPANOLAMINES 审中-公开

    公开(公告)号：WO2013186153A2

    公开(公告)日：2013-12-19

    申请号：PCT/EP2013/061880

    申请日：2013-06-10

    Applicant: MEDIZINISCHE UNIVERSITÄT WIEN

    Inventor： GSTACH, Hubert ,  CHIBA, Peter ,  MASTALIR, Matthias

    IPC: C07D211/14 ,  C07D229/02 ,  C07C235/46 ,  C07C235/60 ,  C07D295/088 ,  A61K31/166 ,  A61K31/396 ,  A61K31/445

    CPC classification number: C07D295/088 ,  C07C235/60 ,  C07C235/64 ,  C07C235/66 ,  C07C237/28 ,  C07C2601/02 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2603/74 ,  C07D211/14 ,  C07D211/18 ,  C07D229/02

    Abstract: The use of compounds of formula wherein R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.

    Abstract translation: 使用其中R 2，R 3，R 4，R 5，R 6和R 7具有几个含义的化合物用于治疗由原生动物生物介导的病症，上式的新化合物和用于制备这些化合物的中间体，药物组合物包含 这样的新化合物，一种治疗由原生动物生物介导的病症的方法，其包括向有需要的受试者施用任选与第二药物物质的这类化合物，以及每当包含光亲和标签时，使用这些化合物来鉴定 芳基氨基醇抗疟药的分子靶标。

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