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1. 发明申请

US20110200533A1 COMPOUNDS FOR THE DIAGNOSIS OF DISEASES ASSOCIATED WITH VCAM EXPRESSION 有权
标题翻译：用VCAM表达相关疾病诊断的化合物
公开(公告)号：US20110200533A1
公开(公告)日：2011-08-18
申请号：US12593175
申请日：2008-03-28
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： A61K49/14 , C07K7/06 , A61K49/00 , A61K38/08 , A61P9/00
CPC分类号： A61K49/0008 , A61K49/0056 , A61K49/14 , A61K49/186 , A61K49/1866 , B82Y5/00 , C07K7/06
摘要： The present invention relates to a compound of the following general formula (I):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 a VCAM-targeting peptide, the VCAM-targeting peptide being chosen from the peptides of formula below and the functional equivalents thereof: a) X1-X2-X3-X4-X5-X6-X7-X8-X9 (1) (SEQ ID No. 1) where X1 is absent or chosen from cysteine and methionine; X2 chosen from asparagine and glutamine; X3 chosen from asparagine and glutamine; X4 chosen from serine and threonine; X5 chosen from lysine, arginine, histidine and ornithine; X6 chosen from serine and threonine; X7 chosen from histidine, arginine and lysine; X8 chosen from threonine and serine; X9 is absent or chosen from cysteine and methionine; preferably, the peptide CNNSKSHTC (SEQ ID No. 2) and the peptide NNSKSHT (SEQ ID No. 3); b) X10-X11-X12-X13-X14-X15-X16-X17-X18 (2) (SEQ ID No. 4) with X10 chosen from cysteine and methionine; X11 chosen from methionine and cysteine; X12 chosen from lysine, arginine and alanine; X13 chosen from threonine and serine; X14 chosen from aspartic acid and glutamic acid; X15 chosen from threonine and serine; X16 chosen from arginine, alanine and lysine; X17 chosen from leucine, isoleucine and valine; X18 chosen from cysteine and methionine; preferably, the peptide CMKTDTRLC (SEQ ID No. 5); and the pharmaceutically acceptable salts of these compounds of a) or of b).
摘要翻译：本发明涉及以下通式（I）的化合物：信号连接子 - 肽（I），其中： - 信号代表信号实体; 可能存在或不存在的激酶表示化学键，肽表示包含VCAM靶向肽的肽，所述VCAM靶向肽选自下式的肽及其功能等同物：a）其中X1不存在或选自半胱氨酸和甲硫氨酸的X1-X2-X3-X4-X5-X6-X7-X8-X9（1）（SEQ ID No.1） X2选自天冬酰胺和谷氨酰胺; X3选自天冬酰胺和谷氨酰胺; X4选自丝氨酸和苏氨酸; X5选自赖氨酸，精氨酸，组氨酸和鸟氨酸; X6选自丝氨酸和苏氨酸; X7选自组氨酸，精氨酸和赖氨酸; X8选自苏氨酸和丝氨酸; X9不存在或选自半胱氨酸和甲硫氨酸; 优选肽CNNSKSHTC（SEQ ID No.2）和肽NNSKSHT（SEQ ID No.3）; b）具有选自半胱氨酸和甲硫氨酸的X10的X10-X11-X12-X13-X14-X15-X16-X17-X18（2）（SEQ ID No.4） X11选自甲硫氨酸和半胱氨酸; X12选自赖氨酸，精氨酸和丙氨酸; X13选自苏氨酸和丝氨酸; X14选自天冬氨酸和谷氨酸; X15选自苏氨酸和丝氨酸; X16选自精氨酸，丙氨酸和赖氨酸; X17选自亮氨酸，异亮氨酸和缬氨酸; X18选自半胱氨酸和甲硫氨酸; 优选地，肽CMKTDTRLC（SEQ ID No.5）; 和a）或b）的这些化合物的药学上可接受的盐。

2. 发明申请

US20100143250A1 COMPOUNDS FOR THE DIAGNOSIS OF APOPTOSIS 审中-公开
标题翻译：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。

3. 发明授权

US08367039B2 Compounds for the diagnosis of diseases associated with VCAM expression 有权
标题翻译：用于诊断与VCAM表达相关的疾病的化合物
公开(公告)号：US08367039B2
公开(公告)日：2013-02-05
申请号：US12593175
申请日：2008-03-28
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： A61K49/00
CPC分类号： A61K49/0008 , A61K49/0056 , A61K49/14 , A61K49/186 , A61K49/1866 , B82Y5/00 , C07K7/06
摘要： The present invention relates to a compound of the following general formula (I): Signal-Linker-Peptide (I) in which Signal is a signal entity; Linker, is absent or is a chemical bond, and Peptide is a peptide having a VCAM-targeting peptide and pharmaceutically acceptable salts thereof. The VCAM-targeting peptide may be X10-X11-X12-X13-X14-X15-X16-X17-X18 (SEQ ID No. 4) with X10 chosen from cysteine and methionine; X11 chosen from methionine and cysteine; X12 chosen from lysine, arginine and alanine; X13 chosen from threonine and serine; X14 chosen from aspartic acid and glutamic acid; X15 chosen from threonine and serine; X16 chosen from arginine, alanine and lysine; X17 chosen from leucine, isoleucine and valine; X18 chosen from cysteine and methionine; preferably, the peptide CMKTDTRLC (SEQ ID No. 5).
摘要翻译：本发明涉及以下通式（I）的化合物：其中Signal是信号实体的信号连接子 - 肽（I）; 接头，不存在或是化学键，肽是具有VCAM靶向肽及其药学上可接受的盐的肽。 VCAM靶向肽可以是X10-X11-X12-X13-X14-X15-X16-X17-X18（SEQ ID No.4），其中X10选自半胱氨酸和甲硫氨酸; X11选自甲硫氨酸和半胱氨酸; X12选自赖氨酸，精氨酸和丙氨酸; X13选自苏氨酸和丝氨酸; X14选自天冬氨酸和谷氨酸; X15选自苏氨酸和丝氨酸; X16选自精氨酸，丙氨酸和赖氨酸; X17选自亮氨酸，异亮氨酸和缬氨酸; X18选自半胱氨酸和甲硫氨酸; 优选地，肽CMKTDTRLC（SEQ ID No.5）。

4. 发明申请

US20100215586A1 NOVEL METHOD FOR PREPARING NANOPARTICLES COVERED WITH A GEM-BISPHOSPHONATE STABILIZING LAYER COUPLED TO HYDROPHILIC BIODISTRIBUTION LIGANDS 有权
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：US20100215586A1
公开(公告)日：2010-08-26
申请号：US12681378
申请日：2008-10-06
申请人： Marc Port , Olivier Rousseaux
发明人： Marc Port , Olivier Rousseaux
IPC分类号： A61K49/18
CPC分类号： A61K49/0428 , A61K49/1842 , A61K49/186 , B82Y5/00 , C09B11/24 , C09B23/0033 , C09B23/0066 , C09B23/083
摘要： A novel method for preparing nanoparticles for medical imaging, including a metal core, an organic stabilizing layer containing gem-bisphosphonate compounds and at least one hydrophilic biodistribution ligand.
摘要翻译：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。

5. 发明授权

US07780953B2 Compositions magnetic particles covered with gem-bisphosphonate derivatives 有权
标题翻译：组合物用双 - 二膦酸衍生物覆盖的磁性颗粒
公开(公告)号：US07780953B2
公开(公告)日：2010-08-24
申请号：US10739400
申请日：2003-12-19
申请人： Marc Port , Claire Corot , Isabelle Raynal , Olivier Rousseaux
发明人： Marc Port , Claire Corot , Isabelle Raynal , Olivier Rousseaux
IPC分类号： A61B5/055 , A61B5/05 , A01N57/18
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, the acid magnetic particles (p) being complexed by one or more gem-bisphosphonate compounds, of formula I: X-L-CH(PO3H2)2 (I) in which: L represents an organic group connecting the X group to the gem-bisphosphonate group —CH(PO3H2)2; X represents a chemical group capable of reacting with a biovector; all or some of the X groups of the particles optionally being coupled to a biovector. The invention relates, also to a process for the preparation of the compositions and their use, in particular as contrast products for Magnetic Resonance Imaging (MRI).
摘要翻译：本发明涉及一种组合物，其包含基于铁化合物的酸性磁性颗粒（p），酸性磁性颗粒（p）由一种或多种式偕二膦酸盐化合物络合：式I：XL-CH（PO 3 H 2）2 ）其中：L表示连接X基团与偕 - 双膦酸基团-CH（PO3H2）2的有机基团; X表示能够与生物载体反应的化学基团; 所有或一些X组的颗粒任选地与生物载体偶联。本发明还涉及制备组合物及其用途的方法，特别是用于磁共振成像（MRI）的对比产物。

6. 发明授权

US08722018B2 Method for preparing nanoparticles covered with a gem-bisphosphonate stabilizing layer coupled to hydrophilic distribution ligands 有权
标题翻译：制备纳米颗粒的方法，该纳米粒子与偶联到亲水性配位配体上的偕二膦酸盐稳定层覆盖
公开(公告)号：US08722018B2
公开(公告)日：2014-05-13
申请号：US12681378
申请日：2008-10-06
申请人： Marc Port , Olivier Rousseaux
发明人： Marc Port , Olivier Rousseaux
IPC分类号： A61B5/055
CPC分类号： A61K49/0428 , A61K49/1842 , A61K49/186 , B82Y5/00 , C09B11/24 , C09B23/0033 , C09B23/0066 , C09B23/083
摘要： A novel method for preparing nanoparticles for medical imaging, including a metal core, an organic stabilizing layer containing gem-bisphosphonate compounds and at least one hydrophilic biodistribution ligand.
摘要翻译：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。

7. 发明申请

US20060239913A1 Peptide conjugate for magnetic resonance imaging 审中-公开
标题翻译：用于磁共振成像的肽缀合物
公开(公告)号：US20060239913A1
公开(公告)日：2006-10-26
申请号：US10560807
申请日：2004-06-17
申请人： Marc Port , Olivier Rousseaux , Christelle Medina , Claire Corot , Iréne Guilbert , Jean-Sébastien Raynaud
发明人： Marc Port , Olivier Rousseaux , Christelle Medina , Claire Corot , Iréne Guilbert , Jean-Sébastien Raynaud
IPC分类号： A61K51/00 , A61K49/10 , C07K7/06
CPC分类号： A61K49/0002 , A61K49/085 , A61K49/14 , C07K5/1005
摘要： The invention relates to new compounds and compositions for the imaging diagnostic of pathologies, namely for cardiovascular diseases, more precisely atherosclerosis disease. These compounds are contrast agents useful namely in the field of magnetic resonance imaging MRI and nuclear medicine. The compounds comprise a particular peptidic MMP inhibitor coupled with a signal entity.
摘要翻译：本发明涉及用于病理学成像诊断的新化合物和组合物，即心血管疾病，更准确地说是动脉粥样硬化疾病。这些化合物是可用于磁共振成像MRI和核医学领域的造影剂。这些化合物包括与信号实体结合的特定的肽MMP抑制剂。

8. 发明申请

US20100297025A1 Novel compositions magnetic particles covered with gem-bisphosphonate derivatives 审中-公开
标题翻译：新颖的组合物磁性颗粒被宝石二膦酸盐衍生物覆盖
公开(公告)号：US20100297025A1
公开(公告)日：2010-11-25
申请号：US12801980
申请日：2010-07-06
申请人： Marc Port , Claire Corot , Isabelle Raynal , Olivier Rousseaux
发明人： Marc Port , Claire Corot , Isabelle Raynal , Olivier Rousseaux
IPC分类号： A61K49/10
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, the acid magnetic particles (p) being complexed by one or more gem-bisphosphonate compounds, of formula I: X-L-CH(PO3H2)2 (I) in which: L represents an organic group connecting the X group to the gem-bisphosphonate group —CH(PO3H2)2; X represents a chemical group capable of reacting with a biovector; all or some of the X groups of the particles optionally being coupled to a biovector. The invention relates also to a process for the preparation of the compositions and their use, in particular as contrast products for Magnetic Resonance Imaging (MRI).
摘要翻译：本发明涉及一种组合物，其包含基于铁化合物的酸性磁性颗粒（p），酸性磁性颗粒（p）由一种或多种式偕二膦酸盐化合物络合：式I：XL-CH（PO 3 H 2）2 ）其中：L表示连接X基团与偕 - 双膦酸基团-CH（PO3H2）2的有机基团; X表示能够与生物载体反应的化学基团; 所有或一些X组的颗粒任选地与生物载体偶联。本发明还涉及制备组合物及其用途的方法，特别是作为磁共振成像（MRI）的对比产品。

9. 发明申请

US20070098643A1 Oligomers of gadolinium chelates, their applicationascontrast products in magnetic resonance imaging and their synthesis intermediates 审中-公开
标题翻译：钆螯合物的低聚物，它们在磁共振成像中的应用及其合成中间体
公开(公告)号：US20070098643A1
公开(公告)日：2007-05-03
申请号：US10505875
申请日：2003-03-05
申请人： Isabelle Nachman , Marc Port , Isabelle Raynal , Olivier Rousseaux
发明人： Isabelle Nachman , Marc Port , Isabelle Raynal , Olivier Rousseaux
IPC分类号： A61K49/10 , C07F5/00
CPC分类号： C07D403/14 , A61K49/124 , C07D257/02 , C07D471/08 , C07F9/65815
摘要： The invention relates to high-relaxivity macrocyclic gadolinium chelate oligomers of formula W-(A)m in which W, A and m are as defined in claim 1, and their use as a blood pool contrast product for magnetic resonance imaging.
摘要翻译：本发明涉及公式<β的高弛豫度大环钆螯合物低聚物，描述=“In-line formula”end =“lead”？> W-（A）＆lt; 在线公式描述=“在线公式”end =“尾”→其中W，A和m如权利要求1中所定义，并且它们用作磁共振成像的血池对比产物。

10. 发明申请

US20060239926A1 Specific high-relaxivity compounds 审中-公开
标题翻译：具体的高弛豫化合物
公开(公告)号：US20060239926A1
公开(公告)日：2006-10-26
申请号：US10560830
申请日：2004-06-17
申请人： Marc Port , Olivier Rousseaux , Claire Corot , Philippe Prigent , Eric Lancelot
发明人： Marc Port , Olivier Rousseaux , Claire Corot , Philippe Prigent , Eric Lancelot
IPC分类号： A61K49/10 , A61K31/555 , C07F5/00
CPC分类号： A61K51/0491 , A61K49/0002 , A61K49/085 , A61K49/122 , A61K49/124 , A61K49/14 , C07D471/08 , C07F9/10 , C07K5/1005
摘要： The invention relates to novel compounds that are useful for the diagnosis of many pathologies, in particular cardiovascular, cancer-related and inflammatory pathologies, and to pharmaceutical compositions comprising said compounds. These compounds comprise a component for targeting a pathological region, linked to a detection component which is effective in diagnostic terms.
摘要翻译：本发明涉及可用于诊断许多病症，特别是心血管，癌症相关和炎性病理学的新化合物，以及包含所述化合物的药物组合物。这些化合物包含用于靶向病理区域的组分，其与检测组分相连，其在诊断方面是有效的。

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