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1. 发明授权

US06251858B1 Derivatives of oligosides, their process of preparation and their applications 失效
标题翻译：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
申请人： Michel Monsigny , Annie-Claude Roche , Nadia Sdiqui , Roger Mayer
发明人： Michel Monsigny , Annie-Claude Roche , Nadia Sdiqui , Roger Mayer
IPC分类号： A61K3816
CPC分类号： C07H15/12 , A61K47/61 , C07H3/06 , C07H19/044 , C07H19/048 , C07H21/00
摘要： 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).
摘要翻译：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。

2. 发明授权

US5595897A Polylysine conjugates 失效
标题翻译：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
申请人： Patrick Midoux , Patrick Erbacher , Annie-Claude Roche-Degremont , Michel Monsigny
发明人： Patrick Midoux , Patrick Erbacher , Annie-Claude Roche-Degremont , Michel Monsigny
IPC分类号： A61K47/48 , C12N15/87 , C07K1/00 , C07K1/107 , C12N15/00 , C12N15/88
CPC分类号： C12N15/87 , A61K47/48315
摘要： 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.
摘要翻译：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。

3. 发明授权

US5332575A Method of targeting melanocytes with a compound containing a fucose residue 失效
标题翻译：用含有岩藻糖残基的化合物靶向黑素细胞的方法
公开(公告)号：US5332575A
公开(公告)日：1994-07-26
申请号：US861780
申请日：1992-04-02
申请人： Gerard Redziniak , Dominique Cerdan , Claudine Kieda , Michel Monsigny
发明人： Gerard Redziniak , Dominique Cerdan , Claudine Kieda , Michel Monsigny
IPC分类号： A61K8/14 , A61K8/60 , A61K9/127 , A61K9/51 , A61K47/48 , A61Q5/08 , A61Q19/02 , A61Q19/04
CPC分类号： A61Q19/04 , A61K47/48815 , A61K8/14 , A61K8/60 , A61K9/1271 , A61Q19/02 , A61Q5/08 , Y10S514/844
摘要： The invention concerns a method of binding a product to the membrane of a melanocyte by means of a ligand-receptor bond, which comprises using a product consisting of a basic structure coupled to at least one ligand consisting of an oside residue accessible to the membrane receptors, said oside residue being a fucose residue, notably an Alpha-L-fucose residue.
摘要翻译：本发明涉及通过配体 - 受体键将产物与黑素细胞膜结合的方法，该方法包括使用由至少一种配体组成的产物，所述碱性结构与至少一种由膜受体可接近的残基组成的配体所述残留物是岩藻糖残基，特别是α-L-岩藻糖残基。

4. 发明授权

US06372499B1 Polymeric complexes for the transfection of nucleic acids, with residues causing the destabilisation of cell membranes 失效
标题翻译：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
申请人： Patrick Midoux , Michel Monsigny
发明人： Patrick Midoux , Michel Monsigny
IPC分类号： C12N1588
CPC分类号： C12N15/88 , A61K47/645 , A61K48/00
摘要： 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.
摘要翻译：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。

5. 发明授权

US4753984A Water soluble macromolecular prodrugs, their preparation and their use as antitumor and antiparasite medicines 失效
标题翻译：水溶性大分子前药，其制备及其作为抗肿瘤和抗寄生虫药物的用途
公开(公告)号：US4753984A
公开(公告)日：1988-06-28
申请号：US871883
申请日：1986-06-09
申请人： Francis Delmotte , Michel Monsigny , Pierre-Jean Lescanne , Francois Daussin
发明人： Francis Delmotte , Michel Monsigny , Pierre-Jean Lescanne , Francois Daussin
IPC分类号： A61K38/00 , A61K47/48 , A61P35/00 , A61P43/00 , A61K37/20 , A61K9/00 , A61K31/765
CPC分类号： A61K47/48246 , A61K47/48176 , A61K47/48192 , Y10S930/28
摘要： A prodrug comprises a polyhydroxylated polyamine to which a drug is linked by the intermediary of a peptidyl group. The prodrug is useful as an antitumor or antiparasite medicine.
摘要翻译：前药包括多羟基化多胺，其中药物通过肽基的中间连接。前药可用作抗肿瘤药或抗寄生虫药。

6. 发明授权

US5733762A Complexes of nucleic acid and polymer, their process of preparation and their use for the transfection of cells 失效
标题翻译：核酸和聚合物的复合物，其制备方法及其用于细胞转染的用途
公开(公告)号：US5733762A
公开(公告)日：1998-03-31
申请号：US741678
申请日：1996-10-31
申请人： Patrick Midoux , Patrick Erbacher , Annie-Claude Roche-Degremont , Michel Monsigny
发明人： Patrick Midoux , Patrick Erbacher , Annie-Claude Roche-Degremont , Michel Monsigny
IPC分类号： A61K47/48 , C12N15/87 , C07K1/00 , C07K1/107 , C12N15/00 , C12N15/88
CPC分类号： A61K47/48238 , A61K47/48315 , C12N15/87
摘要： A compound consisting essentially of polylysine conjugated to non-charged residues and recognition signals wherein the free amino functions of said polylysine are substituted with non-charged residues and said recognition signals, which non-charged residues consist of gluconalactone and which recognition signals are at least one member of the group consisting of galactoside, mannoside, fucoside, Lewis.sup.x, Lewis.sup.b, oligomannoside, oligolactosamine saccharides and peptide ANP and said conjugated polylysine contains at least 30% unsubstituted free amino functions and a method of transfecting cultured cells.
摘要翻译：基本上由缀合有非荷电残基的聚赖氨酸组成的化合物和识别信号，其中所述聚赖氨酸的游离氨基官能团被无电荷残基和所述识别信号所取代，所述非带电残基由葡萄糖酸内酯组成，哪些识别信号至少为由半乳糖苷，甘露糖苷，岩藻糖苷，Lewisx，Lewisb，寡聚半乳糖苷，寡聚乳糖糖和肽ANP组成的组中的一个成员和所述共轭聚赖氨酸含有至少30％的未取代的游离氨基功能和转染培养细胞的方法。

7. 发明授权

US4801578A Muramylpeptide-glycoprotein immunostimulant derivatives, their preparation and their use in medication 失效
标题翻译：胰蛋白酶 - 糖蛋白免疫刺激衍生物，其制备及其在药物中的应用
公开(公告)号：US4801578A
公开(公告)日：1989-01-31
申请号：US617176
申请日：1984-06-04
申请人： Michel Monsigny , Annie-Claude Roche
发明人： Michel Monsigny , Annie-Claude Roche
IPC分类号： C07K14/76 , A61K35/74 , A61K36/06 , A61K36/07 , A61K38/00 , A61K38/16 , A61K38/55 , A61K39/395 , A61P37/04 , C07K1/113 , C07K9/00 , C07K14/00 , C07K14/765 , C07K14/81 , C07K16/00 , C07K16/30 , C07K19/00 , C07K15/14 , A61K37/02 , A61K45/05
CPC分类号： C07K14/765 , C07K16/30 , C07K9/005 , A61K38/00
摘要： Macromolecular conjugates of muramylpeptides useful as a stimulant of the cellular immune systems have the formula (R--X).sub.m --(LAM) wherein R is an N-acetylmuramylpeptidyl group or a derivative thereof; (LAM) is a neoglycoprotein having affinity for macrophages or monocytes, consisting of a protein covalently substituted by more than five glycidic chains, each having at least five osidic units, X is a covalent bond between a functional group of the peptidic part of R and a functional group of (LAM) or X is the residue of a conventional bifunctional coupling agent capable of bonding to R and (LAM) by formation of covalent bonds; and m is a number greater than or equal to 1.
摘要翻译：可用作细胞免疫系统兴奋剂的胞壁酰胺的大分子缀合物具有式（R-X）m-（LAM），其中R是N-乙酰胞壁酰基肽基或其衍生物; （LAM）是对巨噬细胞或单核细胞具有亲和力的新糖蛋白，由由多于五个的糖苷链共价取代的蛋白组成，每个具有至少五个奥昔单位，X是R的肽部分的官能团之间的共价键，（LAM）或X的官能团是通过形成共价键与R和（LAM）键合的常规双功能偶联剂的残基; m是大于或等于1的数。

8. 发明授权

US4576745A Method for the fluorimetric determination of endotoxins, new peptides carrying a fluorophorous substance usable in said method and method for its preparation 失效
标题翻译：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
申请人： Michel Monsigny
发明人： Michel Monsigny
IPC分类号： C07K1/113 , C07K5/083 , C07K5/103 , C07K14/00 , C07K14/195 , C07K14/41 , C12Q1/34 , G01N33/52 , G01N33/579 , F25B29/00
CPC分类号： C07K5/1005 , C07K5/0808 , C12Q1/34 , G01N33/52 , G01N33/579 , C12Q2337/00 , G01N2333/948
摘要： 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.
摘要翻译： 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。

9. 发明授权

US5686103A Liposomal product with a ligand having fucose as a terminal moiety 失效
标题翻译：具有岩藻糖作为末端部分的配体的脂质体产物
公开(公告)号：US5686103A
公开(公告)日：1997-11-11
申请号：US717976
申请日：1996-09-23
申请人： Gerard Redziniak , Dominique Cerdan , Claudine Kieda , Michel Monsigny
发明人： Gerard Redziniak , Dominique Cerdan , Claudine Kieda , Michel Monsigny
IPC分类号： A61K8/14 , A61K8/60 , A61K9/127 , A61K9/51 , A61K47/48 , A61Q5/08 , A61Q19/02 , A61Q19/04
CPC分类号： A61Q19/04 , A61K47/48815 , A61K8/14 , A61K8/60 , A61K9/1271 , A61Q19/02 , A61Q5/08 , Y10S514/844
摘要： The invention concerns a method of binding a product to the membrane of a melanocyte by means of a ligand-receptor bond, which comprises using a product consisting of a basic structure coupled to at least one ligand consisting of an oside residue accessible to the membrane receptors, said oside residue being a fucose residue, notably an Alpha-L-fucose residue.
摘要翻译：本发明涉及通过配体 - 受体键将产物与黑素细胞膜结合的方法，该方法包括使用由至少一种配体组成的产物，所述碱性结构与至少一种由膜受体可接近的残基组成的配体所述残留物是岩藻糖残基，特别是α-L-岩藻糖残基。

10. 发明授权

US5286629A Method of binding a product to the membrane of a keratinocyte by means of a ligand-receptor bond, method of preparing such a product, product obtained, cosmetic or pharmaceutical composition in which it is present and its method of preparation 失效
标题翻译：通过配体 - 受体键将产物与角质形成细胞的膜结合的方法，制备这种产物的方法，获得的产物，其存在的化妆品或药物组合物及其制备方法
公开(公告)号：US5286629A
公开(公告)日：1994-02-15
申请号：US761809
申请日：1991-11-04
申请人： Alain Denis , Claudine Kieda , Michel Monsigny , Pierre Perrier , Gerard Redziniak
发明人： Alain Denis , Claudine Kieda , Michel Monsigny , Pierre Perrier , Gerard Redziniak
IPC分类号： A61K8/00 , A61K8/04 , A61K8/14 , A61K8/60 , A61K8/64 , A61K8/73 , A61K9/127 , A61K9/51 , A61K47/36 , A61K47/42 , A61Q7/00 , A61Q19/00 , A61Q90/00 , A61K47/48
CPC分类号： A61Q19/08 , A61K8/0241 , A61K8/11 , A61K8/14 , A61K8/60 , A61K9/127 , A61K9/1271 , A61Q19/00 , A61Q7/00 , B82Y5/00 , A61K2800/413 , A61K2800/434 , A61K2800/57 , A61K2800/612 , A61K2800/654 , Y10S514/844
摘要： The invention relates to products which are to be bound specifically to the membrane of a keratinocyte by means of a ligand-receptor bond.These products carry at least one ligand consisting of an oside residue selected from .alpha.-L-rhamnose, .alpha.-D-galactose and .alpha.-D-galactose-6-phosphate.By virtue of this specificity, it is possible to prepare cosmetic or pharmaceutical compositions having an improved efficacy in particular, for example for regeneration of the epidermis, for the treatment of psoriasis or for renewed hair growth.
摘要翻译：本发明涉及通过配体 - 受体键特异性固定在角质形成细胞膜上的产品。所述产物是至少一种配体，其由选自α-L-鼠李糖，α-D-半乳糖和α-D-半乳糖-6-磷酸的oside残基组成。由于其具体特征，可以制备具有特别是提高的效率的化妆品或药物组合物，例如用于表皮再生，用于治疗牛皮癣和用于头发再生长。

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