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29 条记录 (耗时 0.025 秒)

    (&agr;-aminophosphino) peptide derivatives, method for making same and therapeutic applications thereof
    5.
    发明授权
    (&agr;-aminophosphino) peptide derivatives, method for making same and therapeutic applications thereof 失效
    （α-氨基膦基）肽衍生物，其制备方法和治疗应用

    公开(公告)号：US06518260B1

    公开(公告)日：2003-02-11

    申请号：US09284882

    申请日：1999-04-22

    申请人： Marie-Claude Fournie-Zaluski ,  Huixiong Chen ,  Bernard Pierre Roques

    发明人： Marie-Claude Fournie-Zaluski ,  Huixiong Chen ,  Bernard Pierre Roques

    IPC分类号： A61K3166

    CPC分类号： C07F9/301 ,  C07F9/3211

    摘要： The invention concerns compounds derived from (&agr;-aminophosphino) peptides, of general formula (I), in which R1 and R2 each represents a hydrogen atom or taken together form an imine with the adjacent nitrogen atom; R3 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl group, a cycloalkylmethyl group or finally, a methyl group substituted by a heterocyclic, aromatic or saturated group; R4 represents a phenyl group, a benzyl group, these groups capable of being substituted or not, a hydrogen atom, an alkyl group, analkenyl group or a cycloalkyl group; R5 represents an alkyl group, an alkenyl group, a phenyl group, a benzyl group, all these groups capable of being substituted or not, a hydrogen atom, a cycloalkyl, cycloalkylmethyl group or finally a methyl group substituted by a heterocyclic, aromatic or saturated group; R6, R7 and R8 can in particular represent a hydrogen atom, an alkyl group, a phenyl group substituted or not . . . n is equal to 0 or 1, in the form of enantiomers, diastereoisomers or racemic mixtures, their salts, their method of preparation and their therapeutic applications.

    摘要翻译： 本发明涉及衍生自通式（I）的（α-氨基膦基）肽的化合物，其中R 1和R 2各自代表氢原子或与其相邻的氮原子一起形成亚胺; R3表示烷基，烯基，苯基，苄基，所有这些能够被取代的基团，氢原子，环烷基，环烷基甲基或最后被杂环取代的甲基， 芳族或饱和基团; R4表示苯基，苄基，这些能够被取代的基团，氢原子，烷基，断链基或环烷基; R5表示烷基，烯基，苯基，苄基，所有这些能够被取代的基团，氢原子，环烷基，环烷基甲基或最后被杂环，芳族或饱和的取代的甲基 组; R6，R7和R8可以特别表示氢原子，烷基，被取代的苯基。 。 。 n等于0或1，以对映异构体，非对映异构体或外消旋混合物，其盐，其制备方法及其治疗应用的形式。

    Peptide substrates recognisable by a botulinum toxin a, bont/a and the use thereof
    10.
    发明申请
    Peptide substrates recognisable by a botulinum toxin a, bont/a and the use thereof 有权
    由肉毒杆菌毒素a，bont / a可识别的肽底物及其用途

    公开(公告)号：US20090208993A1

    公开(公告)日：2009-08-20

    申请号：US11579491

    申请日：2005-05-04

    申请人： Marie-Claude Fournie-Zaluski ,  Bernard Pierre Roques

    发明人： Marie-Claude Fournie-Zaluski ,  Bernard Pierre Roques

    IPC分类号： C12Q1/37 ,  C07K7/06 ,  C07K5/10 ,  C07K7/08

    CPC分类号： C07K14/705 ,  C07K5/0812 ,  C07K5/1016 ,  C12Q1/37 ,  G01N2333/96486

    摘要： The present invention relates to a peptide substrate selectively recognized by botulinum toxin type A, BoNT/A, comprising a Nop-(Z)-Pya fragment in the peptide structure thereof, wherein Z represents an amino acids chain, preferably RA, said fragment being cleaved by said toxin. Said invention also relates to the substrate use, in particular for carrying out methods for detecting, identifying and/or dosing botulinum toxin type A, at very low concentrations (of the order of 20 pg), or inhibitors and/or activators of the metallopeptidase activity of said toxin and thereby making it possible to quantify the power thereof.

    摘要翻译： 本发明涉及由A型肉毒杆菌毒素BoNT / A选择性识别的肽底物，其包含其肽结构中的Nop-（Z）-Pya片段，其中Z表示氨基酸链，优选RA，所述片段为 被毒素切断。 所述发明还涉及底物用途，特别是用于进行检测，鉴定和/或给予A型非常低浓度（约20pg量级）的肉毒杆菌毒素或金属肽酶抑制剂和/或活化剂的方法 所述毒素的活性，从而可以量化其功率。