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    PROCESS FOR PREPARING A PHARMACEUTICAL FORMULATION OF CONTRAST AGENTS
    4.
    发明申请
    PROCESS FOR PREPARING A PHARMACEUTICAL FORMULATION OF CONTRAST AGENTS 有权
    制备药物制剂的方法

    公开(公告)号：US20110129425A1

    公开(公告)日：2011-06-02

    申请号：US12918259

    申请日：2009-02-18

    申请人： Dominique Meyer ,  Claire Corot ,  Marc Port ,  Vincent Barbotin ,  Bruno Bonnemain

    发明人： Dominique Meyer ,  Claire Corot ,  Marc Port ,  Vincent Barbotin ,  Bruno Bonnemain

    IPC分类号： A61K49/12 ,  C07D257/02 ,  A61P43/00

    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 of free 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 ch1 and/or of free lanthanide C lan1; d) adjustment of C ch1 and/or of C lan1 so as to obtain C ch1=C tch1 and C lan1=0, wherein C t ch1 is the target concentration of free macrocyclic chelate in the final liquid pharmaceutical formulation.

    摘要翻译： 本发明涉及制备含有大环螯合物与镧系元素络合物和摩尔/摩尔量的游离大环螯合物的液体药物制剂的方法，其含量为0.002％至0.4％，有利地为0.02％至0.3％，非常有利地介于 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） 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，其次是游离的大环螯合物和/或游离的镧系元素; 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 lan1的浓度; d）调整C ch1和/或C lan1，以获得C ch1 = C tch1和C lan1 = 0，其中C t ch1是最终液体药物制剂中游离大环螯合物的目标浓度。

    COMPOUNDS FOR THE DIAGNOSIS OF APOPTOSIS
    5.
    发明申请
    COMPOUNDS FOR THE DIAGNOSIS OF APOPTOSIS 审中-公开
    用于诊断病毒的化合物

    公开(公告)号：US20100143250A1

    公开(公告)日：2010-06-10

    申请号：US12593495

    申请日：2008-03-21

    申请人： Marc Port ,  Olivier Rousseaux ,  Robert Muller ,  Carmen Burtea

    发明人： Marc Port ,  Olivier Rousseaux ,  Robert Muller ,  Carmen Burtea

    IPC分类号： A61K51/08 ,  C07K7/06 ,  A61K49/14 ,  A61K49/00

    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 present invention relates to a compound of general formula (I) below: Signal−Linker−Peptide (I) in which Signal represents a signal entity; Linker, which may or may not be present, represents a chemical bond and Peptide represents a peptide comprising an apoptosis-targeting peptide, the apoptosis-targeting peptide being chosen from the peptides having the formula below and the functional equivalents thereof: X1-X2-X3-X4-X5-X6 (1) (SEQ ID No 1) in which X1 and X2 represent, independently of one another, leucine or isoleucine, X3 and X4 represent lysine, X5 represents proline and X6 represents phenylalanine, 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 represents phenylalanine or leucine; P-G-D-L-X8-X9 (3) (SEQ ID No 3) in which X8 represents serine or valine and X9 represents threonine or arginine; H-G-X10-L-S-X11 (4) (SEQ ID No 4) in which X10 represents aspartic acid or histidine, and X11 represents threonine or isoleucine; V-L-G-E-R-G (5) (SEQ ID No 5); and the pharmaceutically acceptable salts of these compounds.

    摘要翻译： 本发明涉及以下通式（I）的化合物：其中Signal表示信号实体的信号连接子 - 肽（I） 可能存在或不存在的接头表示化学键，肽代表包含凋亡靶向肽的肽，所述凋亡靶向肽选自具有下式的肽及其功能等同物：X1-X2- 其中X1和X2彼此独立地表示亮氨酸或​​异亮氨酸的X3-X4-X5-X6（1）（SEQ ID No 1），X3和X4表示赖氨酸，X5表示脯氨酸，X6表示苯丙氨酸，有利地是肽LIKKPF （SEQ ID No.11）及其功能等同物; D-A-H-S-X7-S（2）（SEQ ID No 2），其中X7表示苯丙氨酸或亮氨酸; P-G-D-L-X8-X9（3）（SEQ ID No 3），其中X8表示丝氨酸或缬氨酸，X9表示苏氨酸或精氨酸; 其中X10表示天冬氨酸或组氨酸，X11表示苏氨酸或异亮氨酸的H-G-X10-L-S-X11（4）（SEQ ID No 4） V-L-G-E-R-G（5）（SEQ ID No 5）; 和这些化合物的药学上可接受的盐。

    Compounds Comprising Short Aminoalcohol Chains and Metal Complexes for Medical Imgaing
    6.
    发明申请
    Compounds Comprising Short Aminoalcohol Chains and Metal Complexes for Medical Imgaing 有权
    包含短氨基醇链和金属配合物用于医学成像的化合物

    公开(公告)号：US20090169479A1

    公开(公告)日：2009-07-02

    申请号：US12083092

    申请日：2006-10-09

    申请人： Marc Port

    发明人： Marc Port

    IPC分类号： A61K31/395 ,  C07D471/08 ,  C07D257/02 ,  C12N15/63 ,  C07F15/00 ,  A61K31/555 ,  A61K31/439 ,  A61K49/12

    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), with n=1 to 3, Y represents —CONH2, —CO—NR7R8 or —NR7-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， X 4和X 5彼此独立地表示L L，其中L表示C 1 -C 3烷基，优选（CH 2），n = 1至3，Y表示-CONH 2，-CO-NR 7 R 8或-NR 7 -CO-R 8 ，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。

    Contrast Agents Encapsulating Systems for Cest Imaging
    7.
    发明申请
    Contrast Agents Encapsulating Systems for Cest Imaging 审中-公开
    用于Cest成像的对比剂封装系统

    公开(公告)号：US20070292354A1

    公开(公告)日：2007-12-20

    申请号：US11663583

    申请日：2005-09-23

    申请人： Marc Port

    发明人： Marc Port

    IPC分类号： A61K49/18 ,  A61K49/06 ,  A61K49/16

    CPC分类号： A61K49/1812

    摘要： The present invention concerns a contrast agent compound for CEST imaging wherein said contrast agent comprises a proton pool encapsulating system that contains a pool of water mobile shifted protons.

    摘要翻译： 本发明涉及用于CEST成像的造影剂化合物，其中所述造影剂包括含有水移动移位质子池的质子池封装系统。

    Porphyrin compounds and their use in high-field MRI
    9.
    发明申请
    Porphyrin compounds and their use in high-field MRI 失效
    卟啉化合物及其在高场MRI中的应用

    公开(公告)号：US20060013774A1

    公开(公告)日：2006-01-19

    申请号：US11077033

    申请日：2005-03-11

    申请人： Marc Port

    发明人： Marc Port

    IPC分类号： A61K49/12 ,  C07F5/00

    CPC分类号： C07D487/22 ,  A61K49/085 ,  A61K49/10 ,  B24B49/003

    摘要： The present invention relates to the use, in magnetic resonance imaging employing a field greater than 1.5 Tesla, of a porphyrin compound of the following general formula I in which R0 and R′0 are such that the compound is soluble in a biological medium, and M denotes a paramagnetic metal ion, advantageously Mn3+. The present invention also relates to novel porphyrin compounds.

    摘要翻译： 本发明涉及在使用大于1.5特斯拉的磁场的磁共振成像中使用以下通式I的卟啉化合物，其中R 0和R'0 < SUB>使得化合物可溶于生物培养基，M表示顺磁金属离子，有利地为Mn 3+。 本发明还涉及新的卟啉化合物。

    Diagnostic compounds comprising a scaffold coupled to a signal entity for medical imaging diagnostic
    10.
    发明申请
    Diagnostic compounds comprising a scaffold coupled to a signal entity for medical imaging diagnostic 审中-公开
    包括与用于医学成像诊断的信号实体相连的支架的诊断化合物

    公开(公告)号：US20050260127A1

    公开(公告)日：2005-11-24

    申请号：US10833282

    申请日：2004-04-28

    申请人： Claire Corot ,  Marc Port ,  Thierry Gautheret ,  Xavier Williard

    发明人： Claire Corot ,  Marc Port ,  Thierry Gautheret ,  Xavier Williard

    IPC分类号： A61K49/00 ,  A61K49/18 ,  A61K51/00 ,  A61K51/04 ,  C07F5/00

    CPC分类号： B82Y5/00 ,  A61K49/0002 ,  A61K49/124 ,  A61K51/0497

    摘要： The present invention concerns a diagnostic compound of formula (E) (SCAFFOLD)n1-(LINKER)n3-(SIGNAL)n2-(M), wherein SCAFFOLD is chosen in table 2: namely Biphenyl; arylpiperidine; Arylpiperazine; 1,4 dyhydropyridine Dihydropyrimidone; 1,4 benzodiazepine-2-one; 1,5 benzodiazepine-2-one; 1,4-benzodiazepine-2,5 diones; pyrrolo2,1-c 1,4 benzodiazepines 5,11 diones; 1,4 benzothiazepine-5-ones; 5,11-dihydro-benzo pyrido 3,2b 1,4 diazepine-6-ones; Benzopyrane; Chromone; Benzopyranone; Coumarine, pyranocoumarine; Benzopiperazinones; Quinazolinone; Quinazolindione; Quinoxalinone; Imidazoquinoxaline; indole; Benzimidazole Benzofurane Benzothiophene; SIGNAL is a signal entity for medical imaging diagnostic, and pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及一种诊断性化合物，该化合物具有式<？in-line-formula description =“In-line Formulas”end =“lead”？>（E）（SCAFFOLD）n1 - （LINKER） SUB（n3） - （SIGNAL）n2 - （M），<？in-line-formula description =“In-line Formulas”end =“tail”？>其中选择SCAFFOLD 在表2中：即联苯; 芳基哌啶; 芳基哌嗪; 1,4-二氢吡啶二氢嘧啶酮; 1,4-苯并二氮杂-2-酮; 1,5苯并二氮杂-2-酮; 1,4-苯并二氮杂2,5二氧化es; 吡咯并[2,1-c] 1,4苯并二氮杂5,11二氢噻吩; 1,4-苯并硫氮杂-5-酮; 5,11-二氢 - 苯并吡啶并[3,2-b]二氮杂-6-酮; 苯并吡喃 色酮 苯并吡喃酮 香豆素，吡喃葡萄糖; 苯并嗪酮; 喹唑啉酮 喹唑啉酮 喹喔啉酮 咪唑喹喔啉 吲哚 苯并咪唑苯并呋喃苯并噻吩; SIGNAL是用于医学成像诊断的信号实体及其药学上可接受的盐。