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1. 发明授权

US6060040A Cross-linked polymeric compositions for increasing the MRI contrast in visualising the digestive tract of patients 失效
标题翻译：用于增加患者消化道可视化MRI对比度的交联聚合物组合物
公开(公告)号：US6060040A
公开(公告)日：2000-05-09
申请号：US997453
申请日：1997-12-23
申请人： Herve Tournier , Philippe Bussat
发明人： Herve Tournier , Philippe Bussat
IPC分类号： A61K49/00 , A61K49/06 , C07C229/16 , C07C233/20 , C07C237/08 , C07C237/10 , C07C327/06 , C07C327/10 , C07D257/02 , C08F20/00 , C08F20/36 , C08F20/38 , C08F20/52 , C08F22/10 , A61B5/055
CPC分类号： C08F22/105 , A61K49/06 , C07C229/16 , C07C237/10 , C07D257/02 , C08F20/36 , Y10S514/836
摘要： The invention provides, as contrast signal generators in MR imaging of the digestive tract, paramagnetic metal chelates of novel acrylic compounds of formula C(R.sup.1 R.sup.2).dbd.CR.sup.3 --CO--Z--A (1) and/or C(R.sup.1 R.sup.2).dbd.CR.sup.3 --O--Z--A--Z--CO--CR.sup.3 .dbd.C(R.sup.1 R.sup.2) (2) in monomer, oligomer, homopolymer and copolymer forms, in which the R.sup.1, R.sup.2 and R.sup.3 represent H or saturated or unsaturated C.sub.1-10 aliphatic radicals optionally substituted by one or more OH groups; Z is a covalent bond or a linker spacer and A is a moiety capable of fixing a paramagnetic metal by chelation. Compounds of type (1) useful in the present invention are, for instance the polyalkylene-aminopolycaboxylic acids such as NTA, EDTA, DTPA, DOTA and like structures, possibly involving additional substituents; an example is the compound BOPTA which is a DTPA derivative carrying a benzyloxypropyl group.
摘要翻译：本发明提供作为消化道MR成像中的对比信号发生器，式C（R1R2）= CR3-CO-ZA（1）和/或C（R1R2）= CR3-OZAZ-的新型丙烯酸化合物的顺磁性金属螯合物， CO-CR 3 = C（R 1 R 2）（2）在单体，低聚物，均聚物和共聚物形式中，其中R 1，R 2和R 3表示H或任选被一个或多个OH基团取代的饱和或不饱和C 1-10脂族基团; Z是共价键或连接基团，A是通过螯合固定顺磁性金属的部分。可用于本发明的（1）型化合物是例如可能涉及另外的取代基的聚亚烷基 - 氨基多羧酸如NTA，EDTA，DTPA，DOTA等结构; 作为具有苄氧基丙基的DTPA衍生物的化合物BOPTA的实例。

2. 发明授权

US5393530A Method for making liposomes of enhanced entrapping capacity toward foreign substances to be encapsulated 失效
标题翻译：制备脂质体增强包封能力的方法
公开(公告)号：US5393530A
公开(公告)日：1995-02-28
申请号：US861889
申请日：1992-06-22
申请人： Michel Schneider , Herve Tournier , Roland Hyacinthe , Christian Guillot , Bernard Lamy
发明人： Michel Schneider , Herve Tournier , Roland Hyacinthe , Christian Guillot , Bernard Lamy
IPC分类号： A61K9/00 , A61K9/127 , A61K47/48 , A61K49/04 , B01J13/02 , A61K57/22
CPC分类号： A61K49/0466 , A61K9/1278
摘要： Liposome vesicles are prepared containing water or very dilute solutions encapsulated therein. These "empty" liposomes are suspended in a carrier liquid containing, dispersed therein, substances of interest to be loaded into the vesicles and incubated for a period of time at temperatures above the lipids transition temperature, whereby loading by transmembrane permeation occurs in high yields.
摘要翻译： PCT No.PCT / EP91 / 00377。 371日期：1992年6月22日 102（e）日期1992年6月22日PCT提交1992年12月9日PCT公布。公开号WO92 / 10166 日期：1992年6月25日。制备含有水或非常稀的溶液的脂质体囊泡。将这些“空”脂质体悬浮于含有分散在其中的感兴趣物质的载体液体中，将其装载到囊泡中，并在高于脂质转变温度的温度下温育一段时间，由此通过跨膜渗透的加载以高产率发生。

3. 发明授权

US5370901A Compositions for increasing the image contrast in diagnostic investigations of the digestive tract of patients 失效
标题翻译：用于增加患者消化道诊断调查中图像对比度的组合
公开(公告)号：US5370901A
公开(公告)日：1994-12-06
申请号：US824311
申请日：1992-01-23
申请人： Herve Tournier , Roland Hyacinthe , Friedrich Cavagna
发明人： Herve Tournier , Roland Hyacinthe , Friedrich Cavagna
IPC分类号： A61K47/26 , A61K49/00 , A61K49/18 , A61K49/22 , G01R33/28 , A61K9/16 , A61B8/12
CPC分类号： G01R33/5601 , A61K49/1845 , A61K49/1854 , A61K49/1863 , A61K49/1893 , A61K49/223 , A61K49/226 , Y10S514/836 , Y10T436/24
摘要： Method of making an ingestible composition useful as a contrast enhancing agent in ultrasonic imaging of the digestive tract of humans and animals, wherein the composition has microballoons as contrast enhancing particles bound to an organic carrier phase, which when hydrated has an adhesive affinity for the gastrointestinal mucosa.Method includes grafting a silane coupler having at least two reactive functions to the microballoons through one of the reactive functions and binding the grafted microballoons to the carrier phase through another reactive function.
摘要翻译：制备可用作对比增强剂的可摄取组合物在人和动物消化道超声成像中的方法，其中所述组合物具有微球作为与有机载体相结合的对比增强颗粒，当与水合物具有对胃肠道的粘合亲和力时粘膜方法包括通过反应性功能之一将具有至少两个反应性功能的硅烷偶联剂接枝到微球上，并通过另一个反应性官能将接枝的微球结合到载体相上。

4. 发明授权

US5312615A Injectable opacifying composition containing liposomes of high encapsulation capacity for X-ray examinations 失效
标题翻译：含有X射线检查的高包封能力的脂质体的注射不透明组合物
公开(公告)号：US5312615A
公开(公告)日：1994-05-17
申请号：US302690
申请日：1989-01-19
申请人： Michel Schneider , Herve Tournier , Bernard Lamy
发明人： Michel Schneider , Herve Tournier , Bernard Lamy
IPC分类号： A61K9/127 , A61K9/50 , A61K49/04 , A61K49/00
CPC分类号： A61K49/0466
摘要： Injectable aqueous composition intended for opacifying certain organs with a view to examination by X-rays. This composition is based on liposomes containing, encapsulated therein, an aqueous solution of an iodinated opacifying agent. The ratio between the weight of iodine encapsulated by the liposomes and the weight of the lipids from which their membrane is formed is not lower than 1.5 mg/mg.
摘要翻译： PCT No.PCT / EP88 / 00447 Sec。 371日期1989年1月19日 102（e）日期1989年1月19日PCT提交1988年5月16日PCT公布。出版物WO88 / 09165 日期：1988年12月1日。用于使某些器官不透明的可注射的含水组合物，以便通过X射线检查。该组合物基于含有其中包封碘化不透明剂水溶液的脂质体。由脂质体包封的碘的重量与其膜形成的脂质的重量之比不低于1.5mg / mg。

5. 发明授权

US4267314A Process for the preparation of lactosylurea, its purification and its conversion to the corresponding N-hydroxymethylated derivative 失效
标题翻译：制备乳糖基脲的方法，其纯化及其转化为相应的N-羟甲基化衍生物
公开(公告)号：US4267314A
公开(公告)日：1981-05-12
申请号：US11133
申请日：1979-02-12
申请人： Jean-Pierre Sachetto , Alain Regnault , Sergio Cuccolo , Herve Tournier , Jean-Michel Armanet
发明人： Jean-Pierre Sachetto , Alain Regnault , Sergio Cuccolo , Herve Tournier , Jean-Michel Armanet
IPC分类号： A23K50/15 , C07H13/12 , C07H5/00
CPC分类号： C07H13/12 , A23K50/15
摘要： A process for the preparation of lactosylurea and the N-methylol derivative thereof which are usable as feed supplements for ruminants.According to this process, lactose and urea are heated to 70.degree.-110.degree. C. with a minimum of water and, if possible, this water is eliminated during the reaction. The crude reaction product can be purified by grinding with ice-water or ethanol and subsequent draining so as to eliminate by dissolution in such solvants the unreacted urea.The corresponding N-methylol derivative is obtained by the reaction with formaldehyde.
摘要翻译：一种制备可用作反刍动物饲料添加剂的乳糖基脲及其N-羟甲基衍生物的方法。根据该方法，用最少量的水将乳糖和尿素加热至70-110℃，如果可能的话，在反应期间将其除去。粗反应产物可以通过用冰水或乙醇研磨并随后排出来纯化，以便通过在这样的溶剂中溶解未反应的尿来消除。通过与甲醛的反应获得相应的N-羟甲基衍生物。

6. 发明授权

US4257818A Process and apparatus for continuous acid hydrolysis and saccharification 失效
公开(公告)号：US4257818A
公开(公告)日：1981-03-24
申请号：US032891
申请日：1979-04-24
申请人： Alain Regnault , Jean-Pierre Sachetto , Herve Tournier , Thomas Hamm , Jean-Michel Armanet
发明人： Alain Regnault , Jean-Pierre Sachetto , Herve Tournier , Thomas Hamm , Jean-Michel Armanet
IPC分类号： C13K1/02 , B01J19/08 , B01F9/02
CPC分类号： C13K1/02
摘要： Continuous hydrolysis to produce sugars is effected by cyclically immersing a solid, divided lignocellulosic material in a bath of concentrated hydrochloric acid and draining the material between successive immersions so as to dissolve the produced sugars, until the sugar concentration of the acid in the bath has attained a desired value.The solid material and the liquid acid are delivered to a tubular horizontal rotary reactor arranged to provide a bath of the acid, to produce a rotating movement for cyclical immersion of the solid material in the bath of acid and longitudinally displace the solid material undergoing hydrolysis together with the acid of the bath and to continuously discharge solid residue and acid containing dissolved sugars due to overflow by gravity at an outlet end of the reactor.

7. 发明申请

US20070196284A1 Liposomal assembly for therapeutic and/or diagnostic use 有权
标题翻译：用于治疗和/或诊断用途的脂质体组装
公开(公告)号：US20070196284A1
公开(公告)日：2007-08-23
申请号：US11596447
申请日：2005-05-31
申请人： Herve Tournier , Roland Hyacinthe , Michel Schneider
发明人： Herve Tournier , Roland Hyacinthe , Michel Schneider
IPC分类号： A61K49/10 , A61K9/127
CPC分类号： A61K9/1075 , A61K9/1271 , A61K48/0091 , A61K49/1812 , C12N15/88 , Y10S977/907 , Y10T428/2982
摘要： Composition for diagnostic or therapeutic use which comprises an assembly comprising an active agent. The assembly comprises a liposome and a plurality of micellar components associated thereto, said micellar components being associated to the outer surface of the envelope of said liposome through a substantially electrostatic interaction. When an active compound is incorporated into the micelles, a substantial amount of said active compound can be linked to a singe liposome. Furthermore, the presence of the outer micellar layer allows to increase the residence time of said liposome in the blood stream.
摘要翻译：用于诊断或治疗用途的组合物，其包含包含活性剂的组合物。组合物包含脂质体和与其相关联的多个胶束组分，所述胶束组分通过基本静电相互作用与所述脂质体的包膜的外表面相关联。当活性化合物掺入胶束中时，大量的所述活性化合物可以连接到单个脂质体。此外，外胶束层的存在允许增加所述脂质体在血流中的停留时间。

8. 发明授权

US5980937A Liposomes with enhanced entrapment capacity and their use in imaging 失效
标题翻译：具有增强的捕获能力的脂质体及其在成像中的应用
公开(公告)号：US5980937A
公开(公告)日：1999-11-09
申请号：US909827
申请日：1997-08-12
申请人： Herve Tournier , Michel Schneider , Christian Guillot
发明人： Herve Tournier , Michel Schneider , Christian Guillot
IPC分类号： A61K9/127 , A61K49/04 , B01J13/02
CPC分类号： A61K9/1277 , Y10S514/945 , Y10T428/2984
摘要： The invention relates to a dry deposit as a precursor to liposome vesicles, the precursor being a three dimensional expanded structure with bulk density between 0.01 and 0.001 g/cm.sup.3. The invention also concerns a method of making liposome vesicles with an enhanced entrapment capacity by dissolving one or more film forming lipids in at least one organic solvent to form a solution in a reaction vessel, evaporating the solvent to form an expanded three dimensional porous lipid structure, contacting the lipid deposit with an aqueous carrier phase, and producing liposome vesicles entrapping the carrier phase as well as an apparatus comprising an array of tubing or an inert packing which serves as a material support or a matrix surface for the deposition of lipids produced according to the method.
摘要翻译：本发明涉及作为脂质体囊泡前体的干沉积物，该前体是体积密度在0.01至0.001g / cm 3之间的三维膨胀结构。本发明还涉及通过将一种或多种成膜脂质溶解在至少一种有机溶剂中以形成溶液在反应容器中，使溶剂蒸发以形成扩展的三维多孔脂质结构，从而制备具有增强的捕获能力的脂质体囊泡的方法使脂质沉积物与水性载体相接触，并产生包裹载体相的脂质体囊泡，以及包含管阵列或惰性填料的装置，其用作材料载体或基质表面，用于沉积根据的方法。

9. 发明授权

US5910300A Amphiphilic linkers for coupling administrable diagnostically or physiologically active agents and bioselective targeting compounds 失效
标题翻译：用于偶联给药的诊断或生理活性剂和生物选择性靶向化合物的两亲接头
公开(公告)号：US5910300A
公开(公告)日：1999-06-08
申请号：US740620
申请日：1996-10-31
申请人： Herve Tournier , Sibylle Pochon , Bernard Lamy
发明人： Herve Tournier , Sibylle Pochon , Bernard Lamy
IPC分类号： G01R33/28 , A61B5/055 , A61K47/48 , A61K49/00 , A61K49/08 , A61K49/18 , C08G65/32 , C08G65/329 , G01N31/00
CPC分类号： A61K49/103 , A61K49/085 , A61K49/1821 , A61K49/1866 , B82Y5/00 , C08G65/329
摘要： Administrable factors or compositions to be directed to specific sites in the body of human and animal patients which comprise a medically and/or diagnostically effective moiety (I) and, coupled thereto by means of a linker (L), a substance (II) having specific affinity for specific sites in the organism.Linker "L" has a structure schematized by the formula:Y(W-Z-R).sub.m, m being 1, 2, or 4wherein the portion YW is an amphiphile, i.e. a segment comprised of a hydrophobic-lipophilic sequence "Y" and a hydrophilic-lipophobic sequence "W" connected covalently together, Z is a chemical bond or an intermediate connector sequence and R is a reactive function for effecting coupling with selected substances (II).
摘要翻译：涉及包含医学和/或诊断有效部分（I）的人和动物患者体内的特定部位的可管理因子或组合物，并通过连接体（L）与其连接，具有对生物体中特定位点的特异性亲和力。连接子“L”具有由下式表示的结构：Y（WZR）m，m为1,2或4，其中部分YW为两亲物，即由疏水亲油性序列“Y”组成的链段和亲水的 - 疏水序列“W”共价连接在一起，Z是化学键或中间连接器序列，R是用于与所选物质（II）偶联的反应性函数。

10. 发明授权

US5895661A Liposome vesicle precursors 失效
标题翻译：脂质体囊泡前体
公开(公告)号：US5895661A
公开(公告)日：1999-04-20
申请号：US909097
申请日：1997-08-12
申请人： Herve Tournier , Michel Schneider , Christian Guillot
发明人： Herve Tournier , Michel Schneider , Christian Guillot
IPC分类号： A61K9/127 , A61K49/04 , B01J13/02
CPC分类号： A61K9/1277 , Y10S514/945 , Y10T428/2984
摘要： The invention relates to a dry deposit as a precursor to liposome vesicles, the precursor being a three dimensional expanded structure with bulk density between 0.01 and 0.001 g/cm.sup.3. The invention also concerns a method of making liposome vesicles with an enhanced entrapment capacity by dissolving one or more film forming lipids in at least one organic solvent to form a solution in a reaction vessel, evaporating the solvent to form an expanded three dimensional porous lipid structure, contacting the lipid deposit with an aqueous carrier phase, and producing liposome vesicles entrapping the carrier phase as well as an apparatus comprising an array of tubing or an inert packing which serves as a material support or a matrix surface for the deposition of lipids produced according to the method.
摘要翻译：本发明涉及作为脂质体囊泡前体的干沉积物，该前体是体积密度在0.01至0.001g / cm 3之间的三维膨胀结构。本发明还涉及通过将一种或多种成膜脂质溶解在至少一种有机溶剂中以形成溶液在反应容器中，使溶剂蒸发以形成扩展的三维多孔脂质结构，从而制备具有增强的捕获能力的脂质体囊泡的方法使脂质沉积物与水性载体相接触，并产生包裹载体相的脂质体囊泡，以及包含管阵列或惰性填料的装置，其用作材料载体或基质表面，用于沉积根据的方法。

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