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1. 发明申请

WO2009143101A2 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： GASTRIN释放肽化合物
公开(公告)号：WO2009143101A2
公开(公告)日：2009-11-26
申请号：PCT/US2009/044447
申请日：2009-05-19
申请人： BRACCO IMAGING S.P.A. , LATTUADA, Luciano , CAPPELLETTI, Enrico , LINDER, Karen, E. , NUNN, Adrian, D. , LANTRY, Laura
发明人： LATTUADA, Luciano , CAPPELLETTI, Enrico , LINDER, Karen, E. , NUNN, Adrian, D. , LANTRY, Laura
IPC分类号： A61K51/08
CPC分类号： A61K51/088 , A61K49/0056 , G01N33/57492 , G01N2333/5758
摘要： Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.
摘要翻译：提供用于诊断，分期疾病，监测药物的治疗效果和成像患者的方法和组合物，包括放射性药物制剂。提供了包含与放射性同位素复合的Ga-AMBA的组合物; 成像胃泌素释放肽受体（GRP-R）携带组织的成像方法以及疑似与异常GRP-R功能相关疾病的患者诊断或分期疾病的方法。此外，提供监测靶向与GRP-R串扰的受体的药物的治疗效果的方法; 预先给药/共同给予含有GRP-R的非靶组织的方法也是如此。特别地，提供了通过使用与GRP-R结合的配体来体内/体外监测受体和受体途径的活性的方法; 以及通过使用也可以通过外部手段检测的配体来测量与GRP-R显示串扰的受体或受体组及其相关途径的活性的方法。

2. 发明申请

WO2007090022A8 NOVEL COMPOUNDS FOR TARGETING ENDOTHELIAL CELLS, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR THEIR USE 审中-公开
标题翻译：用于靶向内皮细胞的新化合物，包含其的组合物及其使用方法
公开(公告)号：WO2007090022A8
公开(公告)日：2009-07-23
申请号：PCT/US2007061019
申请日：2007-01-25
申请人： BRACCO INT BV , VON WRONSKI MATHEW A , MARINELLI EDMUND R , NUNN ADRIAN D , PILLAI RADHAKRISHNA , RAMALINGAM KONDAREDDIAR , TWEEDLE MICHAEL F , LINDER KAREN E , NANJAPPAN PALANIAPPA , RAJU NATARAJAN
发明人： VON WRONSKI MATHEW A , MARINELLI EDMUND R , NUNN ADRIAN D , PILLAI RADHAKRISHNA , RAMALINGAM KONDAREDDIAR , TWEEDLE MICHAEL F , LINDER KAREN E , NANJAPPAN PALANIAPPA , RAJU NATARAJAN
IPC分类号： A61K38/08
CPC分类号： A61K49/0067 , A61K38/00 , A61K47/6923 , A61K47/6929 , A61K49/0056 , A61K49/14 , A61K49/223 , A61K51/088 , B82Y5/00 , B82Y10/00 , B82Y30/00 , C07K7/06
摘要： The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-I receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.
摘要翻译：本发明提供用于靶向表达NP-1受体的内皮细胞，肿瘤细胞或其他细胞的化合物，其含有该组合物的组合物及其使用方法。另外，本发明包括可用于可视化，治疗或放射治疗的诊断，治疗和放射治疗组合物。

3. 发明申请

WO2007090022A3 NOVEL COMPOUNDS FOR TARGETING ENDOTHELIAL CELLS, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR THEIR USE 审中-公开
标题翻译：用于靶向内皮细胞的新化合物，含有该化合物的组合物及其使用方法
公开(公告)号：WO2007090022A3
公开(公告)日：2007-11-22
申请号：PCT/US2007061019
申请日：2007-01-25
申请人： BRACCO INT BV , VON WRONSKI MATHEW A , MARINELLI EDMUND R , NUNN ADRIAN D , PILLAI RADHAKRISHNA , RAMALINGAM KONDAREDDIAR , TWEEDLE MICHAEL F , LINDER KAREN E , NANJAPPAN PALANIAPPA , RAJU NATARAJAN
发明人： VON WRONSKI MATHEW A , MARINELLI EDMUND R , NUNN ADRIAN D , PILLAI RADHAKRISHNA , RAMALINGAM KONDAREDDIAR , TWEEDLE MICHAEL F , LINDER KAREN E , NANJAPPAN PALANIAPPA , RAJU NATARAJAN
IPC分类号： A61K38/08
CPC分类号： A61K49/0067 , A61K38/00 , A61K47/6923 , A61K47/6929 , A61K49/0056 , A61K49/14 , A61K49/223 , A61K51/088 , B82Y5/00 , B82Y10/00 , B82Y30/00 , C07K7/06
摘要： The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-I receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.
摘要翻译：本发明提供了靶向表达NP-1受体的内皮细胞，肿瘤细胞或其他细胞的化合物，含有该化合物的组合物及其使用方法。另外，本发明包括用于可视化，治疗或放疗的诊断，治疗和放射治疗组合物。

4. 发明申请

WO2007095443A2 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： GASTRIN释放肽化合物
公开(公告)号：WO2007095443A2
公开(公告)日：2007-08-23
申请号：PCT/US2007/061813
申请日：2007-02-08
申请人： BRACCO IMAGING S.P.A. , CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian, D. , RAJU, Natarajan , RAMALINGAM, Kondareddiar , SWENSON, Rolf, E. , TWEEDLE, Michael, F.
发明人： CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , NUNN, Adrian, D. , RAJU, Natarajan , RAMALINGAM, Kondareddiar , SWENSON, Rolf, E. , TWEEDLE, Michael, F.
IPC分类号： A61K51/00 , A61K49/00 , C07K14/775
CPC分类号： C07K14/57572 , A61K49/085 , A61K49/122 , A61K49/14 , A61K51/088
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is a metal chelator having the structure (I): wherein Rl -R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N-O-P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译：用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是具有结构（I）的金属螯合剂：其中R 1 -R 5和FG如本文所定义（以与金属放射性核素复合的形式），NOP是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。还提供了用于制备放射治疗剂的方法和试剂盒。

5. 发明申请

WO2007090022A2 NOVEL COMPOUNDS FOR TARGETING ENDOTHELIAL CELLS, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR THEIR USE 审中-公开
标题翻译：用于靶向内皮细胞的新化合物，包含其的组合物及其使用方法
公开(公告)号：WO2007090022A2
公开(公告)日：2007-08-09
申请号：PCT/US2007/061019
申请日：2007-01-25
申请人： BRACCO INTERNATIONAL B.V. , VON WRONSKI, Mathew, A. , MARINELLI, Edmund, R. , NUNN, Adrian, D. , PILLAI, Radhakrishna , RAMALINGAM, Kondareddiar , TWEEDLE, Michael, F. , LINDER, Karen, E. , NANJAPPAN, Palaniappa , RAJU, Natarajan
发明人： VON WRONSKI, Mathew, A. , MARINELLI, Edmund, R. , NUNN, Adrian, D. , PILLAI, Radhakrishna , RAMALINGAM, Kondareddiar , TWEEDLE, Michael, F. , LINDER, Karen, E. , NANJAPPAN, Palaniappa , RAJU, Natarajan
IPC分类号： C07K7/08 , A61K49/14
CPC分类号： A61K49/0067 , A61K38/00 , A61K47/6923 , A61K47/6929 , A61K49/0056 , A61K49/14 , A61K49/223 , A61K51/088 , B82Y5/00 , B82Y10/00 , B82Y30/00 , C07K7/06
摘要： The present invention provides compounds for targeting endothelial cells, tumor cells or other cells that express the NP-I receptor, compositions containing the same and methods for their use. Additionally, the present invention includes diagnostic, therapeutic and radiotherapeutic compositions useful for visualization, therapy or radiotherapy.
摘要翻译：本发明提供用于靶向表达NP-1受体的内皮细胞，肿瘤细胞或其他细胞的化合物，其含有该组合物的组合物及其使用方法。另外，本发明包括可用于可视化，治疗或放射治疗的诊断，治疗和放射治疗组合物。

6. 发明申请

WO2007002500A1 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： GASTRIN释放肽化合物
公开(公告)号：WO2007002500A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024641
申请日：2006-06-23
申请人： BRACCO IMAGING S.P.A. , CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , RAJU, Natarajan , RAMALINGAM, Kondareddiar , SWENSON, Rolf, E. , TWEEDLE, Michael, F.
发明人： CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Edmund, R. , NANJAPPAN, Palaniappa , RAJU, Natarajan , RAMALINGAM, Kondareddiar , SWENSON, Rolf, E. , TWEEDLE, Michael, F.
IPC分类号： A61K51/00 , A61K36/14
CPC分类号： A61K51/088 , A61K49/0002 , C07C269/04 , C07D257/00 , C07J41/0005 , C07J41/0011 , C07J43/003 , C07K14/57572 , C07C271/22
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is a metal chelator having the structure (8): wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N-O-P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.
摘要翻译：用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是具有结构（8）的金属螯合剂：其中R1-R5和FG如本文所定义（以与金属放射性核素复合的形式），NOP是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。还提供了用于制备放射治疗剂的方法和试剂盒。

7. 发明申请

WO03074005A8 KDR AND VEGF/KDR BINDING PEPTIDES AND THEIR USE IN DIAGNOSIS AND THERAPY 审中-公开
标题翻译： KDR和VEGF / KDR结合肽及其在诊断和治疗中的应用
公开(公告)号：WO03074005A8
公开(公告)日：2005-07-21
申请号：PCT/US0306731
申请日：2003-03-03
申请人： DYAX CORP , BRACCO INT BV , SATO AARON K , SEXTON DANIEL J , LADNER ROBERT C , DRANSFIELD DANIEL T , SWENSON ROLF E , MARINELLI EDMUND R , RAMALINGAM KONDAREDDIAR , NUNN ADRIAN D , VON WRONSKI MATHEW A , SHRIVASTAVA AJAY , POCHON SIBYLLE , BUSSAT PHILIPPE , ARBOGAST CHRISTOPHE , PILLAI RADHAKRISHNA , FAN HONG , LINDER KAREN E , SONG BO , NANJAPPAN PALANIAPPA
发明人： SATO AARON K , SEXTON DANIEL J , LADNER ROBERT C , DRANSFIELD DANIEL T , SWENSON ROLF E , MARINELLI EDMUND R , RAMALINGAM KONDAREDDIAR , NUNN ADRIAN D , VON WRONSKI MATHEW A , SHRIVASTAVA AJAY , POCHON SIBYLLE , BUSSAT PHILIPPE , ARBOGAST CHRISTOPHE , PILLAI RADHAKRISHNA , FAN HONG , LINDER KAREN E , SONG BO , NANJAPPAN PALANIAPPA
IPC分类号： A61K38/00 , A61K49/22 , A61K51/08 , C07K7/08 , C07K14/00 , C07K14/52 , C07K14/71 , C07K7/00
CPC分类号： C07K7/08 , A61K38/00 , A61K49/223 , A61K51/088 , C07K14/001 , C07K14/52 , C07K14/71 , C07K2319/00
摘要： The present invention provides binding polypeptides for KDR or VEGF/KDR complex, which have a variety of uses wherever treating, detecting, isolating or localizing angiogenesis is advantageous. Particularly disclosed are synthetic, isolated polypeptides capable of binding KDR or VEGF/KDR complex with high affinity ( e . g ., having a K D

8. 发明申请

WO2004065407A2 IMPROVED GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译：改进的GASTRIN释放肽化合物
公开(公告)号：WO2004065407A2
公开(公告)日：2004-08-05
申请号：PCT/US0341328
申请日：2003-12-24
申请人： BRACCO IMAGING SPA , CAPPELLETTI ENRICO , LATTUADA LUCIANO , LINDER KAREN E , MARINELLI ED , NANJAPPAN PALANIAPPA , RAJU NATARAJAN , SWENSON ROLF E , TWEEDLE MICHAEL
发明人： CAPPELLETTI ENRICO , LATTUADA LUCIANO , LINDER KAREN E , MARINELLI ED , NANJAPPAN PALANIAPPA , RAJU NATARAJAN , SWENSON ROLF E , TWEEDLE MICHAEL
IPC分类号： A61K51/08 , C07K
CPC分类号： A61K51/088 , C07K7/086
摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is an optical label or a metal chelator (in the form complexed with a metal radionuclide or not), N-O-P is the linker, and G is the GRP receptor targeting peptide. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent is further provided.
摘要翻译：用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是光学标记或金属螯合剂（以与金属放射性核素复合的形式），NOP是接头，G是GRP受体靶向肽。还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。还提供了制备放射治疗剂的方法和试剂盒。

9. 发明申请

WO0232294A3 RADIOPHARMACEUTICAL FORMULATIONS 审中-公开
标题翻译：放射性药物制剂
公开(公告)号：WO0232294A3
公开(公告)日：2002-07-11
申请号：PCT/US0150802
申请日：2001-10-19
申请人： BRACCO RES USA , CAGNOLINI ALDO , LINDER KAREN E , MARINELLI EDMUND R
发明人： CAGNOLINI ALDO , LINDER KAREN E , MARINELLI EDMUND R
IPC分类号： A61K51/04 , A61K51/12 , A61K51/00
CPC分类号： A61K51/1282 , A61K51/0478
摘要： A method is described for inhibiting the degradation of a diagnostic or radiotherapeutic radiopharmaceutical, especially radiolabeled compounds containing reducible moieties, by including oxidants either as a part of the composition for the preparation of such radiopharmaceuticals, or by adding an oxidant to such compositions immediately after the preparation of such radiopharmaceuticals.
摘要翻译：描述了一种用于抑制诊断或放射性治疗放射性药物，特别是含有可还原部分的放射性标记化合物的降解的方法，通过包括氧化剂作为用于制备这种放射性药物的组合物的一部分，或者通过在这种放射性药物的制备。

10. 发明申请

WO2010002976A2 ENZYME-CLEAVABLE DYE-CONTAINING FLUOR-QUENCHER CONSTRUCTS 审中-公开
标题翻译： ENZYME-CLEAVABLE DYE含有荧光检查器结构
公开(公告)号：WO2010002976A2
公开(公告)日：2010-01-07
申请号：PCT/US2009/049380
申请日：2009-07-01
申请人： BRACCO IMAGING S.P.A. , LINDER, Karen, E.
发明人： LINDER, Karen, E.
IPC分类号： C07K7/06
CPC分类号： C12Q1/37 , C07K7/06 , C09B23/0025 , C09B23/0066 , C09B23/086 , C09B56/00 , G01N2333/914 , G01N2333/96494
摘要： This invention relates to novel compounds that contain a fluor and a quencher linked by an enzyme cleavable substrate. The constructs contain fluor/quencher moieties that are optically silent until cleaved by enzymes, in a preferred embodiment by matrix metalloproteases (MMPs). After cleavage, the constructs become fluorescent - the resulting fluorescent moieties provide imageable emissions that can be used for in vitro evaluation of enzyme activity or for in vivo detection of disease. In a preferred embodiment the fluor is detectable in the hear infrared (NIR). Unlike imaging methods that provide information on morphology, these constructs provide biochemical information about the disease.
摘要翻译：本发明涉及含有通过酶切割底物连接的氟和猝灭剂的新化合物。构建体含有光学沉默的荧光/猝灭剂部分，直到被酶切割为止，在一个优选的实施方案中由基质金属蛋白酶（MMPs）。切割后，构建体变为荧光 - 所得荧光部分提供可成像的排放物，其可用于酶活性的体外评估或体内检测疾病。在优选的实施方案中，荧光在听到红外（NIR）中是可检测的。与提供形态信息的成像方法不同，这些构建体提供有关疾病的生化信息。

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