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    Derivatives of oligosides, their process of preparation and their applications
    1.
    发明授权
    Derivatives of oligosides, their process of preparation and their applications 失效
    寡核苷酸的衍生物，其制备过程及其应用

    公开(公告)号：US06251858B1

    公开(公告)日：2001-06-26

    申请号：US08591481

    申请日：1996-02-21

    Applicant: Michel Monsigny ,  Annie-Claude Roche ,  Nadia Sdiqui ,  Roger Mayer

    Inventor： Michel Monsigny ,  Annie-Claude Roche ,  Nadia Sdiqui ,  Roger Mayer

    IPC: A61K3816

    CPC classification number: C07H15/12 ,  A61K47/61 ,  C07H3/06 ,  C07H19/044 ,  C07H19/048 ,  C07H21/00

    Abstract: The invention relates to compounds comprising one or several oligosides, each of said oligosides being fixed in a covalent manner on one or many molecules, matrixs or particles, specifically one, two or three, via an intermediary molecule possessing a nitrogen atom carried by a carbon in &agr; of a C═O group and one or many functional groups, specifically one, two or three, the covalent bond between said intermediary molecule and the oligoside being done by the intermediary of said nitrogen atom, and the covalent bond between said intermediary molecule and said molecule, said matrix, said particle, or said molecules, said matrixs, said particles being done by the intermediary of the said functional groups of said intermediary molecule and appropriate functional groups to the molecule(s), the matrix(ces) or the particle(s).

    Abstract translation: 本发明涉及包含一种或几种寡糖的化合物，每种所述寡聚体通过具有碳原子携带的氮原子的中间分子以共价方式固定在一个或多个分子，基质或颗粒上，特别是一个，两个或三个 在C = O基团和一个或多个官能团的α，特别是一个，两个或三个，所述中间分​​子和寡核苷酸之间的共价键由所述氮原子的中间体进行，所述中间分​​子之间的共价键 所述基质，所述颗粒或所述分子，所述基质，所述颗粒通过所述中间分​​子的所述官能团和所述分子的适当官能团，所述基质（ces）或 颗粒。

    Polylysine conjugates
    3.
    发明授权
    Polylysine conjugates 失效
    聚赖氨酸共轭物

    公开(公告)号：US5595897A

    公开(公告)日：1997-01-21

    申请号：US288681

    申请日：1994-08-10

    Applicant: Patrick Midoux ,  Patrick Erbacher ,  Annie-Claude Roche-Degremont ,  Michel Monsigny

    Inventor： Patrick Midoux ,  Patrick Erbacher ,  Annie-Claude Roche-Degremont ,  Michel Monsigny

    IPC: A61K47/48 ,  C12N15/87 ,  C07K1/00 ,  C07K1/107 ,  C12N15/00 ,  C12N15/88

    CPC classification number: C12N15/87 ,  A61K47/48315

    Abstract: The invention concerns a complex between at least one negatively charged nucleic acid and at least one positively charged polymeric conjugate, the link between the nucleic acid and the polymeric conjugate being electrostatic in nature, the polymeric conjugate containing a polymer formed from monomer components having free NH.sub.3.sup.+ functions of the aforementioned components and being as follows:--the free NH.sub.3.sup.+ functions from the aforementioned components are substituted in a ratio of at least 10%, advantageously from 45% to 70%, particularly 60%, by noncharged residues leading to a reduction of positive charges in comparison to the same nonsubstituted polymeric conjugate, facilitating the release of nucleic acid by the dissociation of the complex,--the aforementioned residues possess in addition the following properties:.fwdarw.they contain at least one hydroxyl group,.fwdarw.they do not correspond to a recognition signal recognized by a cellular membrane receptor,--the free NH.sub.3.sup.+ functions from the above mentioned components and/or the hydroxyl groups of the above mentioned residues are also able to be substituted by at least one molecule which constitutes a recognition signal recognized by a cellular membrane receptor, under the condition that the polymeric conjugate contains at least 30% free NH.sub.3.sup.+ functions.

    Abstract translation: 本发明涉及至少一个带负电荷的核酸和至少一个带正电荷的聚合物缀合物之间的复合物，核酸和聚合物缀合物之间的连接本质上是静电的，所述聚合物缀合物含有由具有游离NH 3+的单体组分形成的聚合物， 上述组分的功能如下： - 上述组分的游离NH 3+官能团以至少10％，有利地为45％至70％，特别是60％的比例被非电荷残基取代，导致降低 与相同的非取代的聚合物缀合物相比，正电荷有利于通过络合物的解离释放核酸，上述残基另外具有以下性质： - >它们含有至少一个羟基， - >它们不 对应于由细胞膜受体识别的识别信号， - 来自a的游离NH 3+功能 所述提及的组分和/或上述残基的羟基也能够被至少一种构成由细胞膜受体识别的识别信号的分子取代，条件是聚合物缀合物含有至少30％的游离 NH3 +功能。

    Polymeric complexes for the transfection of nucleic acids, with residues causing the destabilisation of cell membranes
    5.
    发明授权
    Polymeric complexes for the transfection of nucleic acids, with residues causing the destabilisation of cell membranes 失效
    用于转染核酸的聚合物复合物，其残留物导致细胞膜的不稳定

    公开(公告)号：US06372499B1

    公开(公告)日：2002-04-16

    申请号：US09297519

    申请日：1999-05-03

    Applicant: Patrick Midoux ,  Michel Monsigny

    Inventor： Patrick Midoux ,  Michel Monsigny

    IPC: C12N1588

    CPC classification number: C12N15/88 ,  A61K47/645 ,  A61K48/00

    Abstract: The complex has at least one negatively charged nucleic acid bonded to at least one positively charged polymeric conjugate The conjugate containing a polylysine formed from monomers having free NH3+ groups, and having at least 10% of the free NH3+ groups substituted by residues which can be protonated in a weakly acid medium causing destabilization of cell membranes. Optionally, some of the free NH3+ groups can be substituted by a molecule with a recognition signal by a cell membrane receptor. The free NH3+ groups of the said polylysine make up at least 30% of the monomers of the polymeric conjugate. The residue that causes the destabilization of cell membrane in weak acid of quinolines of the formula: where R1 is hydrogen, R2 is —(CH2)n13 CO2—H, X is hydrogen or chlorine and n is an integer from 1 to 10. The signal is a simple oside or a disaccharide or peptide.

    Abstract translation: 所述复合物具有至少一个与至少一个带正电荷的聚合物缀合物连接的带负电荷的核酸。所述缀合物含有由具有游离NH 3 +基团的单体形成的聚赖氨酸，并且具有至少10％的可被质子化的残基取代的游离NH 3 +基团 弱酸介质导致细胞膜的不稳定。可选地，一些游离的NH 3 +基团可以被具有细胞膜受体的识别信号的分子取代。所述聚赖氨酸的游离NH 3+组成至少30％ 导致聚合物缀合物的单体的残留物，其导致下式喹啉的弱酸中细胞膜的不稳定性：其中R1是氢，R2是 - （CH2）n13CO2-H，X是氢或氯，n是整数 信号是一种简单的oside或二糖或肽。

    Method for the fluorimetric determination of endotoxins, new peptides carrying a fluorophorous substance usable in said method and method for its preparation
    9.
    发明授权
    Method for the fluorimetric determination of endotoxins, new peptides carrying a fluorophorous substance usable in said method and method for its preparation 失效
    内毒素荧光测定方法，可用于所述方法的携带荧光物质的新肽及其制备方法

    公开(公告)号：US4576745A

    公开(公告)日：1986-03-18

    申请号：US422976

    申请日：1982-09-09

    Applicant: Michel Monsigny

    Inventor： Michel Monsigny

    IPC: C07K1/113 ,  C07K5/083 ,  C07K5/103 ,  C07K14/00 ,  C07K14/195 ,  C07K14/41 ,  C12Q1/34 ,  G01N33/52 ,  G01N33/579 ,  F25B29/00

    CPC classification number: C07K5/1005 ,  C07K5/0808 ,  C12Q1/34 ,  G01N33/52 ,  G01N33/579 ,  C12Q2337/00 ,  G01N2333/948

    Abstract: Method for determining endotoxins in a liquid, wherein said liquid is contacted, at 20.degree.-40.degree. C., with a lysate of limule amebocytes and an aqueous solution of a peptide having the following formula: ##STR1## in which [Pept-- is a peptidic hydrophobic chain, n is 1, 2, 3, 4, or 5, B is ##STR2## being H or CH.sub.3, --NH--Ar] is the residue of a fluorescent heteroaromatic amine and X.sup..crclbar. is an anion, the pH of the thus obtained medium is adjusted at 5 to 10 and the heteroaromatic amine thus formed is determined by fluorimetry, and new peptides according to formula (I) usable in said method.

    Abstract translation: PCT No.PCT / FR82 / 00003 Sec。 371日期1982年9月9日 102（e）1982年9月9日PCT PCT卷号1982年1月6日PCT公布。 出版物WO82 / 02382 日本1982年7月22日。用于测定液体中的内毒素的方法，其中所述液体在20℃-40℃下与角质形成细胞的裂解物和具有下式的肽的水溶液接触：（I）其中[肽是肽疏水链，n为1,2,3,4或5，B为H或CH 3，-NH-Ar]为荧光杂芳族化合物的残基 胺和X（ - ））是阴离子，将所得介质的pH调节至5至10，并通过荧光测定法测定所形成的杂芳族胺，根据式（I）的新肽可用于所述方法。

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