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1. 发明申请

WO2009103744A3 PROCESS FOR PREPARING A PHARMACEUTICAL FORMULATION OF CONTRAST AGENTS 审中-公开
标题翻译：制备药物制剂的方法
公开(公告)号：WO2009103744A3
公开(公告)日：2009-12-17
申请号：PCT/EP2009051937
申请日：2009-02-18
申请人： GUERBET SA , MEYER DOMINIQUE , COROT CLAIRE , PORT MARC , BARBOTIN VINCENT , BONNEMAIN BRUNO
发明人： MEYER DOMINIQUE , COROT CLAIRE , PORT MARC , BARBOTIN VINCENT , BONNEMAIN BRUNO
IPC分类号： A61K49/06
CPC分类号： A61K49/108 , A61K9/0019 , A61K31/28 , A61K45/06 , A61K47/18 , A61K49/106 , G01N33/15
摘要： The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount offree macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, DO3A, BT-DO3A, HP-DO3A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and/or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate C chl and/or of free lanthanide C lanl; d)adjustmentof C chl and/or of C lanl so as to obtain C chl = C tchl and C lanl = 0, wherein C t chl is the target concentration of free macrocyclic chelate in the final liquid pharmaceuticalformulation.
摘要翻译：本发明涉及一种制备液体药物制剂的方法，其含有大环螯合物与镧系元素的复合物和摩尔/摩尔量的大分子螯合物，其含量为0.002％至0.4％，有利地为0.02％至0.3％，非常有利地为0.025 ％和0.25％，大环螯合物有利地选自DOTA，NOTA，DOTAGA，DO3A，BT-DO3A，HP-DO3A和PCTA，并且优选为DOTA，所述方法包括以下连续步骤：b）制备液体药物组合物首先含有大环螯合物与镧系元素的复合物，其次，游离的大环螯合物和/或游离镧系元素; c）在步骤b）中获得的药物制剂中测量游离大环螯合物C ch1和/或游离镧系元素C lanl的浓度; d）调整C chl和/或C lanl，以获得C chl = C tchl和C lanl = 0，其中C t chl是游离大环螯合物在最终液体药物制剂中的目标浓度。

2. 发明申请

WO2009053597A3 NOVEL METHOD FOR PREPARING NANOPARTICLES COVERED WITH AN ORGANIC STABILISING LAYER COUPLED TO TARGETING LIGANDS 审中-公开
标题翻译：制备纳米颗粒的新方法，该纳米颗粒被与靶向配体偶联的有机稳定层覆盖
公开(公告)号：WO2009053597A3
公开(公告)日：2009-10-15
申请号：PCT/FR2008051803
申请日：2008-10-06
申请人： GUERBET SA , PORT MARC , ROUSSEAUX OLIVIER
发明人： PORT MARC , ROUSSEAUX OLIVIER
IPC分类号： A61K49/18
CPC分类号： A61K49/1842 , A61K49/0002 , A61K49/0032 , A61K49/0041 , A61K49/0043 , A61K49/0093 , B82Y5/00
摘要： The invention relates to a novel method for preparing nanoparticles for medical imaging, including a metal core, an organic stabilising layer and at least one ligand for targeting diseased tissue.
摘要翻译：本发明涉及用于制备用于医学成像的纳米颗粒的新型方法，其包括金属芯，有机稳定层和至少一种用于靶向患病组织的配体。

3. 发明申请

WO2009037342A2 FORMULATION COMPRISING CONTRAST AGENTS FOR MRI COMPRISING AN ORGANIC POLYBASE 审中-公开
标题翻译：包含对包含有机多核苷酸的MRI的对比剂的制剂
公开(公告)号：WO2009037342A2
公开(公告)日：2009-03-26
申请号：PCT/EP2008062550
申请日：2008-09-19
申请人： GUERBET SA , PORT MARC
发明人： PORT MARC
IPC分类号： A61K49/10 , A61K49/18
CPC分类号： A61K49/18 , A61K49/101
摘要： The invention relates to a contrast agent formulation comprising a chelate which complexes a paramagnetic metal ion and at least one organic polybase.
摘要翻译：本发明涉及包含螯合物的造影剂制剂，其螯合顺磁性金属离子和至少一种有机多基质。

4. 发明申请

WO2008125420A3 COMPOUNDS FOR DIAGNOSING APOPTOSIS 审中-公开
标题翻译：用于诊断细胞凋亡的化合物
公开(公告)号：WO2008125420A3
公开(公告)日：2008-12-11
申请号：PCT/EP2008053447
申请日：2008-03-21
申请人： GUERBET SA , PORT MARC , ROUSSEAUX OLIVIER , MULLER ROBERT , BURTEA CARMEN
发明人： PORT MARC , ROUSSEAUX OLIVIER , MULLER ROBERT , BURTEA CARMEN
IPC分类号： C07K7/06 , G01N33/68
CPC分类号： A61K49/186 , A61K49/085 , A61K49/14 , A61K49/1863 , A61K49/1866 , B82Y5/00 , C07D257/02 , C07D403/06 , C07K7/06
摘要： The invention relates to a compound of the following general formula (I): Signal-Link-Peptide (I) in which Signal is a signal entity, Link is present or absent and is a chemical bond, and Peptide is a peptide including an apoptosis targeting peptide, the apoptosis targeting peptide being selected from the peptides of the following formula and the functional equivalents thereof: - X1-X2-X3-X4-X5-X6 (1) (SEQ ID No 1) in which X1 and X2 are each independently leucine or isoleucine, X3 and X4 are lysine, X5 is proline and X6 is phenlyalanine, advantageously the peptide L-I-K-K-P-F (SEQ ID No 11) and the functional equivalents thereof; - D-A-H-S-X7-S (2) (SEQ ID No 2) in which X7 is phenlyalanine or leucine; - P-G-D-L-X8-X9 (3) (SEQ ID No 3) in which X8 is serine or valine and X9 is threonine or arginine; - H-G-X10-L-S-X11 (4) (SEQ ID No 4) in which X10 is aspartic acid or histidine and X11 is threonine or isoleucine; - V-L-G-E-R-G (5) (SEQ ID No 5); and the pharmaceutically acceptable salts of said compounds.
摘要翻译：本发明涉及下列通式（I）的化合物：其中Signal是信号实体的信号 - 连接 - 肽（I），Link存在或不存在并且是化学键，并且肽是包括细胞凋亡所述凋亡靶向肽选自下式的肽及其功能等价物：-X1-X2-X3-X4-X5-X6（1）（SEQ ID No1），其中X1和X2各自为独立的亮氨酸或异亮氨酸，X3和X4是赖氨酸，X5是脯氨酸，X6是苯丙氨酸，有利地是肽LIKKPF（SEQ ID No 11）及其功能等价物; - 其中X 7是苯丙氨酸或亮氨酸的D-A-H-S-X 7 -S（2）（SEQ ID No 2） - 其中X 8为丝氨酸或缬氨酸且X 9为苏氨酸或精氨酸的P-G-D-L-X 8 -X 9（3）（SEQ ID No 3） -H-G-X10-L-S-X11（4）（SEQ ID No 4），其中X10是天冬氨酸或组氨酸，X11是苏氨酸或异亮氨酸; - V-L-G-E-R-G（5）（SEQ ID No 5）; 和所述化合物的药学上可接受的盐。

5. 发明申请

WO2011045415A3 IMAGING AGENTS AND THEIR USE FOR THE DIAGNOSTIC IN VIVO OF NEURODEGENERATIVE DISEASES, NOTABLY ALZHEIMER'S DISEASE AND DERIVATIVE DISEASES 审中-公开
标题翻译：成像剂及其在神经病变疾病诊断中的应用，罕见的阿尔茨海默病和衍生性疾病
公开(公告)号：WO2011045415A3
公开(公告)日：2011-10-06
申请号：PCT/EP2010065526
申请日：2010-10-15
申请人： GUERBET SA , CATOEN SARAH , GAUTHERET THIERRY
发明人： CATOEN SARAH , GAUTHERET THIERRY
IPC分类号： C07D405/04 , A61K51/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04
CPC分类号： C07D409/04 , A61K51/0453 , A61K51/0455 , C07D405/04 , C07D413/04 , C07D417/04 , C07D471/04
摘要： The present invention relates to new imaging agents and their use for the in vivo diagnostic of neurodegenerative diseases, notably Alzheimer's disease and related diseases.
摘要翻译：本发明涉及新的成像剂及其用于神经变性疾病，特别是阿尔茨海默氏病和相关疾病的体内诊断的用途。

6. 发明申请

WO2004058275A3 COMPOSITIONS OF MAGNETIC PARTICLES COVERED WITH GEM-BISPHOSPHONATE DERIVATIVES 审中-公开
标题翻译：含有GEM-BISPHOSPHONATE衍生物的磁性颗粒的组成
公开(公告)号：WO2004058275A3
公开(公告)日：2004-12-09
申请号：PCT/FR0303855
申请日：2003-12-19
申请人： GUERBET SA
发明人： PORT MARC , COROT CLAIRE , RAYNAL ISABELLE , ROUSSEAUX OLIVIER
IPC分类号： A61K49/18 , A61P9/00 , A61P29/00 , A61P35/00 , C07F9/38
CPC分类号： B82Y5/00 , A61K49/1842
摘要： The invention relates to a composition comprising acid magnetic particles (p) based on an iron compound, said acid magnetic particles (p) being complexed by one or more gem-bisphosphonate compounds, having formula (I) X-L-CH (PO3H2)2, wherein: L represents an organic group connecting function X to function gem-bisphosphonate -CH(PO3H2)2; X represents a chemical function that can react with a biovector and, optionally, the X functions of the aforementioned particles are fully or partially coupled to a biovector. The invention also relates to a method of preparing said compounds and to the use of same, particularly as a contrast agent for magnetic resonance imaging (IRM).
摘要翻译：本发明涉及包含基于铁化合物的酸性磁性颗粒（p）的组合物，所述酸性磁性颗粒（p）由一种或多种具有式（I）XL-CH（PO 3 H 2）2的双膦酸化合物络合，其中：L表示连接功能X的功能偕二膦酸盐-CH（PO 3 H 2）2的有机基团; X表示可以与生物载体反应的化学功能，并且任选地，上述颗粒的X官能团完全或部分偶联于生物载体。本发明还涉及一种制备所述化合物及其用途的方法，特别是用作磁共振成像（IRM）的造影剂。

7. 发明申请

WO2009053596A2 NOVEL METHOD FOR PREPARING NANOPARTICLES COVERED WITH A GEM-BISPHOSPHONATE STABILISING LAYER COUPLED TO HYDROPHILIC BIODISTRIBUTION LIGANDS 审中-公开
标题翻译：用于制备与水解生物分布配位体偶联的GEM-二磷酸酯稳定层的纳米颗粒的新方法
公开(公告)号：WO2009053596A2
公开(公告)日：2009-04-30
申请号：PCT/FR2008051802
申请日：2008-10-06
申请人： GUERBET SA , PORT MARC , ROUSSEAUX OLIVIER
发明人： PORT MARC , ROUSSEAUX OLIVIER
IPC分类号： A61K49/18 , A61K9/51 , A61K33/24 , A61K47/02 , A61K47/48 , B82B1/00 , G01N33/553
CPC分类号： A61K49/0428 , A61K49/1842 , A61K49/186 , B82Y5/00 , C09B11/24 , C09B23/0033 , C09B23/0066 , C09B23/083
摘要： The invention relates to a novel method for preparing nanoparticles for medical imaging, including a metal core, an organic stabilising layer containing gem-bisphosphonate compounds and at least one hydrophilic biodistribution ligand.
摘要翻译：本发明涉及一种用于制备用于医学成像的纳米颗粒的新方法，包括金属芯，含有双膦酸化合物的有机稳定层和至少一种亲水性生物分布配体。

8. 发明申请

WO2007141305A3 WATER DIFFUSION IMAGING AND USPIO 审中-公开
标题翻译：水扩散成像和USPIO
公开(公告)号：WO2007141305A3
公开(公告)日：2008-03-06
申请号：PCT/EP2007055598
申请日：2007-06-06
申请人： GUERBET SA , COROT CLAIRE , PORT MARC , ROBERT PHILIPPE , SCHAEFER MICHEL , LE BIHAN DENIS , FROEHLICH JOHANNES
发明人： COROT CLAIRE , PORT MARC , ROBERT PHILIPPE , SCHAEFER MICHEL , LE BIHAN DENIS , FROEHLICH JOHANNES
IPC分类号： G01R33/563 , A61B5/055
CPC分类号： A61B5/055 , A61B5/415 , A61B5/416 , A61B5/418 , G01R33/281 , G01R33/5601 , G01R33/56341
摘要： The invention concerns a method of water diffusion imaging during Magnetic Resonance Imaging within a diagnostically relevant area, characterised in that it includes a combination of the administration of a contrast product capable of generating a signal specifically within its particular area of localisation, said zone of localisation being included in said relevant area, the application of a sequence of water diffusion imaging to the whole of the relevant area, the specific signal generated by the contrast product significantly and specifically modifying the signal within the localisation area, especially in comparison with the signal from the whole of the relevant area.
摘要翻译：本发明涉及在诊断相关区域内的磁共振成像期间的水扩散成像的方法，其特征在于，其包括能够特异性地在其特定定位区域内产生信号的造影剂的施用的组合，所述定位区包括在所述相关区域中，将一系列水扩散成像应用于整个相关区域，由对比产物产生的特定信号显着地且特异性地修改定位区域内的信号，特别是与来自整个相关领域。

9. 发明申请

WO2007042504A3 COMPOUNDS COMPRISING A BIOLOGICAL TARGET RECOGNIZING PART, COUPLED TO A SIGNAL PART CAPABLE OF COMPLEXING GALLIUM 审中-公开
标题翻译：包含生物目标识别部分的化合物，与可复制GALLIUM的信号部分相连
公开(公告)号：WO2007042504A3
公开(公告)日：2008-02-28
申请号：PCT/EP2006067211
申请日：2006-10-09
申请人： GUERBET SA , PORT MARC , COROT CLAIRE , GAUTHERET THIERRY
发明人： PORT MARC , COROT CLAIRE , GAUTHERET THIERRY
IPC分类号： C07D471/08 , A61K49/10
CPC分类号： A61K49/10 , A61K49/085 , A61K49/14 , A61K51/0497 , A61K51/088 , C07D471/08
摘要： The invention concerns compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium. The invention also concerns methods for obtaining said compounds, screening methods capable of selecting such compounds for chemical synthesis thereof and their diagnostic applications, in particular in PET, PET/IRM, PET CT imaging.
摘要翻译：本发明涉及包含与能够络合镓的信号部分耦合的生物靶识别部分的化合物。本发明还涉及获得所述化合物的方法，能够选择用于化学合成的化合物的筛选方法及其诊断应用，特别是在PET，PET / IRM，PET CT成像中。

10. 发明申请

WO2006032704A3 DIAGNOSTIC COMPOUNDS FOR TARGETING A CHEMOKINE RECEPTOR 审中-公开
标题翻译：用于靶向化疗受体的诊断化合物
公开(公告)号：WO2006032704A3
公开(公告)日：2007-04-12
申请号：PCT/EP2005054797
申请日：2005-09-23
申请人： GUERBET SA , PORT MARC
发明人： PORT MARC
IPC分类号： A61K51/12 , A61K49/18 , A61P35/02 , A61P35/04 , G01N33/574
CPC分类号： A61K49/1866 , A61K49/085 , A61K49/186 , A61K51/0446 , A61K51/0455 , A61K51/0459 , A61K51/0497 , B82Y5/00
摘要： The invention relates to a component comprising a targeting portion of at least one chemokine receptor and a detection portion identifiable by a medical imaging method.
摘要翻译：本发明涉及包含至少一种趋化因子受体的靶向部分和通过医学成像方法可识别的检测部分的组分。

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