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21. 发明授权

US08114863B2 Compounds comprising short aminoalcohol chains and metal complexes for medical imaging 有权
标题翻译：包含用于医学成像的短氨基醇链和金属络合物的化合物
公开(公告)号：US08114863B2
公开(公告)日：2012-02-14
申请号：US12083092
申请日：2006-10-09
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K31/33 , C07D257/02
CPC分类号： A61K49/085 , A61K49/10 , A61K49/103 , A61K49/106 , A61K49/14 , A61K51/0402 , A61K51/0478 , A61K51/0482 , C07D257/02 , C07D471/08 , C07D487/04
摘要： The present invention relates to a compound of formula (II) chosen from (IIa) and (IIb) or of formula (VI) chosen from (VIa) and (VIb) of following general formulae: in which: X1, X2, X3, X4 and X5 represent, independently of one another, L-Y in which L represents a C1-C3 alkyl group, preferably (CH2)n with n=1 to 3, Y represents —CONH2, —CO—NR7R8 or —NR8-CO—R8, or an isomer, an enantiomer or a diastereoisomer of these or their mixtures or a pharmaceutically acceptable salt of the compounds of formulae (VIa) and (VIb). It also relates to a complex of these compounds with a paramagnetic metal or a radionuclide and their use in diagnostic methods.
摘要翻译：本发明涉及选自（IIa）和（IIb）或式（VI）的选自（VIa）和（VIb））下列通式的式（II）化合物：其中：X1，X2，X3， X4和X5彼此独立地表示LY，其中L表示C1-C3烷基，优选（CH2）n，n = 1至3，Y表示-CONH2，-CO-NR7R8或-NR8-CO-R8 ，或这些或它们的混合物的异构体，对映体或非对映异构体或式（VIa）和（VIb）化合物的药学上可接受的盐。它还涉及这些化合物与顺磁金属或放射性核素的复合物及其在诊断方法中的用途。

22. 发明授权

US09770520B2 Chelate nanoemulsion for MRI 有权
公开(公告)号：US09770520B2
公开(公告)日：2017-09-26
申请号：US13995732
申请日：2011-12-20
申请人： Marc Port , Caroline Robic , Fernando Leal Calderon , Samy Chadel
发明人： Marc Port , Caroline Robic , Fernando Leal Calderon , Samy Chadel
IPC分类号： A61K49/18
CPC分类号： A61K49/1809 , A61K49/1806
摘要： The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising: an aqueous phase, representing 70% to 90% by weight of the composition, advantageously 75% to 85% and more advantageously from 78% to 82% a lipid phase comprising an oil, representing 9.5% to 29.5% by weight of the composition, advantageously 14% to 25% and more advantageously 17% to 21%, a surfactant at the interface between the aqueous and lipid phases, the surfactant comprising at least one amphiphilic paramagnetic metal chelate and optionally an amphiphilic lipid; the total content of surfactant by weight relative to the oil being between 4% and 10% and advantageously between 5% and 8%; the total content of surfactant by weight relative to the composition being between 0.35% and 2.95% and advantageously between 0.5% and 2%; the oil comprising at least 70%, advantageously at least 80%, advantageously at least 95% by weight and especially at least 97% of saturated C6-C18, advantageously C6-C14 and more advantageously C6-C10 fatty acids.

23. 发明授权

US06440956B1 Bicyclic polyaminoacid metal complexes, their process of preparation and their application in medical imaging 有权
标题翻译：双环聚氨基酸金属络合物，其制备方法及其在医学成像中的应用
公开(公告)号：US06440956B1
公开(公告)日：2002-08-27
申请号：US09589345
申请日：2000-06-08
申请人： Marc Port
发明人： Marc Port
IPC分类号： C07D48708
CPC分类号： C07D471/08
摘要： Metal chelates of the amides of formula in which R has the formula Use in medical imaging.
摘要翻译：在医学成像中具有式用途的甲醛酰胺的金属螯合物

24. 发明授权

US09352056B2 Method for preparing a pharmaceutical formulation of lanthanide chelate in powder form 有权
标题翻译：制备粉末状镧系螯合物药物制剂的方法
公开(公告)号：US09352056B2
公开(公告)日：2016-05-31
申请号：US13319901
申请日：2010-05-12
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K51/00 , A61M36/14 , A61K49/06
CPC分类号： A61K49/108 , A61K9/08 , A61K49/06
摘要： The present invention relates to a method for preparing a pharmaceutical formulation of lanthanide chelate in powder form, wherein the powder constitutes a mol/mol excess of free chelate of between 0.002 and 0.4%.
摘要翻译：本发明涉及一种制备粉末状镧系螯合物的药物制剂的方法，其中该粉末构成0.002至0.4％之间的摩尔/摩尔过量游离螯合物。

25. 发明申请

US20130309176A1 CHELATE NANOEMULSION FOR MRI 有权
标题翻译：用于MRI的CHELATE NANOEMULSION
公开(公告)号：US20130309176A1
公开(公告)日：2013-11-21
申请号：US13995732
申请日：2011-12-20
申请人： Marc Port , Caroline Robic , Fernando Leal Calderon , Samy Chadel
发明人： Marc Port , Caroline Robic , Fernando Leal Calderon , Samy Chadel
IPC分类号： A61K49/18
CPC分类号： A61K49/1809 , A61K49/1806
摘要： The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising: an aqueous phase, representing 70% to 90% by weight of the composition, advantageously 75% to 85% and more advantageously from 78% to 82% a lipid phase comprising an oil, representing 9.5% to 29.5% by weight of the composition, advantageously 14% to 25% and more advantageously 17% to 21%, a surfactant at the interface between the aqueous and lipid phases, the surfactant comprising at least one amphiphilic paramagnetic metal chelate and optionally an amphiphilic lipid; the total content of surfactant by weight relative to the oil being between 4% and 10% and advantageously between 5% and 8%; the total content of surfactant by weight relative to the composition being between 0.35% and 2.95% and advantageously between 0.5% and 2%; the oil comprising at least 70%, advantageously at least 80%, advantageously at least 95% by weight and especially at least 97% of saturated C6-C18, advantageously C6-C14 and more advantageously C6-C10 fatty acids.
摘要翻译：本发明涉及用于MRI的水包油纳米乳液组合物，其包含：水相，占组合物重量的70％至90％，有利地为75％至85％，更有利地为78％至82％在水相和脂质相之间的界面处的表面活性剂占组合物重量的9.5％至29.5％，优选为14％至25％，更优选为17％至21％的脂质相，表面活性剂至少包含一种两亲顺磁金属螯合物和任选的两亲性脂质; 相对于油的重量比的表面活性剂的总含量在4％至10％之间，有利地在5％和8％之间; 表面活性剂的总含量相对于组合物的总含量在0.35％至2.95％之间，有利地在0.5％和2％之间; 该油包含至少70％，有利地至少80％，有利地至少95％重量，特别是至少97％的饱和C 6 -C 18，有利地是C 6 -C 14，更有利地是C 6 -C 10脂肪酸。

26. 发明申请

US20110243859A1 ENCAPSULATING SYSTEM FOR CEST IMAGING WITH CHELATE Q GREATER THAN OR EQUAL TO 2 审中-公开
标题翻译：用于CES成像的包封系统大于或等于2
公开(公告)号：US20110243859A1
公开(公告)日：2011-10-06
申请号：US13133902
申请日：2009-12-09
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K49/18 , A61P43/00
CPC分类号： A61K49/1812
摘要： The present invention relates to the use of a CEST contrast agent in a method of CEST imaging, wherein the contrast agent is a composition comprising an encapsulating system ES encapsulating at least one CEST agent, wherein the at least one CEST agent is constituted of a monomeric chelate of a chelate of q≧2 type, or of a multimer of monomeric chelates of q≧2 type, and wherein said chelate is free inside the encapsulating system.
摘要翻译：本发明涉及CEST造影剂在CEST成像方法中的用途，其中造影剂是包含封装系统ES的组合物，其包封至少一种CEST试剂，其中至少一种CEST试剂由单体 q≥2型的螯合物的螯合物，或q≥2型的单体螯合物的多聚体，并且其中所述螯合物在封装体系内游离。

27. 发明授权

US09402924B2 Diagnostic compounds for targeting a chemokine receptors 有权
公开(公告)号：US09402924B2
公开(公告)日：2016-08-02
申请号：US11663548
申请日：2005-09-23
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K51/04 , A61K49/00 , C07K7/64 , A61K49/18 , A61K49/08 , B82Y5/00
CPC分类号： A61K49/1866 , A61K49/085 , A61K49/186 , A61K51/0446 , A61K51/0455 , A61K51/0459 , A61K51/0497 , B82Y5/00
摘要： The present invention relates to a compound comprising, firstly a component for targeting at least one chemokine receptor and, secondly, a detection component capable of being identified by a medical imaging method.

28. 发明申请

US20120082624A1 METHOD FOR PREPARING A PHARMACEUTICAL FORMULATION OF LANTHANIDE CHELATE IN POWDER FORM 有权
标题翻译：制备粉末形态中的柠檬酸盐的药物制剂的方法
公开(公告)号：US20120082624A1
公开(公告)日：2012-04-05
申请号：US13319901
申请日：2010-05-12
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K49/10
CPC分类号： A61K49/108 , A61K9/08 , A61K49/06
摘要： The present invention relates to a method for preparing a pharmaceutical formulation of lanthanide chelate in powder form, this powder comprising a mol/mol excess of free chelate of between 0.002 and 0.4%, said method comprising the following successive steps: 1) step 1: mixing the chelate and the lanthanide so as to obtain complexation of the lanthanide by the chelate, the complexation solution obtained comprising, in addition to the chelate-lanthanide complex, an excess amount X1 of free chelate; 2) step 2: preferably measuring X1; 3) step 3: precipitating the complexation solution obtained in step 1) from an organic solvent so as to obtain a powder of chelate-lanthanide complex, the powder containing an excess amount X2 of free chelate; 4) step 4: optionally adjusting X2 so as to obtain: 4.a) X2 is between 0.002 and 0.4%, and more especially between 0.02 and 0.3% mol/mol, very advantageously between 0.025 and 0.25% mol/mol, 4.b) X2 corresponds to between 0.2 and 2 times X1, in particular between 0.5 and 1.5 times X1, X2 advantageously belonging to the range: [0.5-0.95]×X1, or to the range [1.05-1.3]×X1; 5) step 5: preferably measuring X2.
摘要翻译：本发明涉及一种制备粉末形式的镧系元素螯合物的药物制剂的方法，该粉末包含0.002至0.4％的摩尔/摩尔过量的游离螯合物，所述方法包括以下连续步骤：1）步骤1：混合螯合物和镧系元素，以便通过螯合物使镧系元素络合，得到的配合溶液除了螯合镧系元素络合物外还含有过量的游离螯合物X1; 2）步骤2：优选测量X1; 3）步骤3：从有机溶剂中沉淀步骤1）中得到的络合溶液，得到螯合镧系配合物的粉末，该粉末含有过量的游离螯合物X2; 4）步骤4：任选地调整X2以获得：4.a）X2为0.002至0.4％，更特别为0.02至0.3％mol / mol，非常有利地为0.025至0.25％mol / mol，4。 b）X2对应于X1的0.2和2倍之间，特别是X1和X2的0.5和1.5之间，X2有利地属于[0.5-0.95]×X1或范围[1.05-1.3]×X1; 5）步骤5：优选测量X2。

29. 发明申请

US20090214441A1 Lipophilic Chelates and Their Use in Imaging 有权
标题翻译：亲脂性螯合剂及其在成像中的应用
公开(公告)号：US20090214441A1
公开(公告)日：2009-08-27
申请号：US11886911
申请日：2006-03-24
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61B5/055 , C07D487/00
CPC分类号： C07D471/08 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/1854 , C07F9/6561
摘要： The invention relates to chelate compounds which can be used in MRI, the chelates being intended to be conveyed by lipophilic transporters, such as lipid nanoparticles or liposomes. The invention also relates to compounds comprising, in association, these chelates and these transporters, if appropriate connected via chemical bonding groups, and to their use in diagnostic imaging, it being possible for this association additionally to comprise biological targeting markers, denoted biovectors.
摘要翻译：本发明涉及可用于MRI中的螯合物，螯合物旨在由脂质转运蛋白（例如脂质纳米颗粒或脂质体）输送。本发明还涉及包括这些螯合物和这些转运蛋白的化合物，如果适当地通过化学键合基团连接，以及它们在诊断成像中的用途，则该结合可能另外包含生物靶向标记物，表示为生物医学。

30. 发明申请

US20090202435A1 Diagnostic compounds for targeting a chemokine receptors 有权
标题翻译：用于靶向趋化因子受体的诊断化合物
公开(公告)号：US20090202435A1
公开(公告)日：2009-08-13
申请号：US11663548
申请日：2005-09-23
申请人： Marc Port
发明人： Marc Port
IPC分类号： A61K51/04 , C07K7/64 , C07F19/00 , A61K49/00 , A61K49/06
CPC分类号： A61K49/1866 , A61K49/085 , A61K49/186 , A61K51/0446 , A61K51/0455 , A61K51/0459 , A61K51/0497 , B82Y5/00
摘要： The present invention relates to a compound comprising, firstly a component for targeting at least one chemokine receptor and, secondly, a detection component capable of being identified by a medical imaging method.
摘要翻译：本发明涉及一种化合物，其包含首先是用于靶向至少一种趋化因子受体的成分，其次，能够通过医学成像方法鉴定的检测成分。

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