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1. 发明申请

WO2011073409A1 PROCESS FOR THE PREPARATION OF THYROID HORMONES AND SALTS THEREOF 审中-公开
标题翻译：制备甲状腺激素的方法及其制备方法
公开(公告)号：WO2011073409A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/070118
申请日：2010-12-17
申请人： BRACCO IMAGING SpA , VISCARDI, Carlo Felice , GAZZETTO, Sonia , GALIMBERTI, Laura , CAPPELLETTI, Enrico , SINI, Loredana
发明人： VISCARDI, Carlo Felice , GAZZETTO, Sonia , GALIMBERTI, Laura , CAPPELLETTI, Enrico , SINI, Loredana
IPC分类号： C07C227/16 , C07C229/36
CPC分类号： C07C227/16 , C07C229/36
摘要： The present invention generally refers to a process for the preparation of L- thyroxine derivatives. More in particular, the present invention relates to a iodination reaction of an aromatic derivative with an appropriate iodinating agent, so to afford the related iodinated compound as disodium salt, which may represent a useful intermediate for the synthesis of the L-thyroxine mono-sodium salt, and the free form thereof.
摘要翻译：本发明通常是指制备L-甲状腺素衍生物的方法。更具体地，本发明涉及芳族衍生物与适当的碘化剂的碘化反应，从而得到相关的碘化合物作为二钠盐，其可以代表用于合成L-甲状腺素单钠的有用中间体盐及其游离形式。

2. 发明申请

WO2009143101A3 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： GASTRIN释放肽化合物
公开(公告)号：WO2009143101A3
公开(公告)日：2010-01-14
申请号：PCT/US2009044447
申请日：2009-05-19
申请人： BRACCO IMAGING SPA , 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： A01N37/18 , A61K38/00
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这种配体来测量与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。

3. 发明申请

WO2007095443A3 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： GASTRIN释放肽化合物
公开(公告)号：WO2007095443A3
公开(公告)日：2008-05-02
申请号：PCT/US2007061813
申请日：2007-02-08
申请人： BRACCO IMAGING SPA , 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 formula (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：用于诊断成像或治疗的新的和改进的化合物，其具有下式：MNOPG，其中M是具有结构式（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或不是），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使患者成像和/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。

4. 发明申请

WO2012007547A1 PROCESS FOR THE PREPARATION OF CONTRAST AGENTS 审中-公开
标题翻译：制备对比剂的方法
公开(公告)号：WO2012007547A1
公开(公告)日：2012-01-19
申请号：PCT/EP2011/062052
申请日：2011-07-14
申请人： BRACCO IMAGING S.P.A. , ANELLI, Pier Lucio , BROCCHETTA, Marino , CAPPELLETTI, Enrico , GAZZOTTI, Ornella
发明人： ANELLI, Pier Lucio , BROCCHETTA, Marino , CAPPELLETTI, Enrico , GAZZOTTI, Ornella
IPC分类号： C07C231/10
CPC分类号： C07C231/12 , C07C231/10 , C07C237/46
摘要： The present invention relates to a process for the preparation of 5-[(2- hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives comprising the Smiles rearrangement of a suitable precursor, by contact of an aqueous solution of this latter with an anion exchanger solid phase.
摘要翻译：本发明涉及一种制备5 - [（2-羟基酰基）氨基] -2,4,6-三碘-1,3-苯二甲酰胺衍生物的方法，包括合适的前体的微升重排，该溶液用阴离子交换剂固相。

5. 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。

6. 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。

7. 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。

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

WO2005067983A1 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：WO2005067983A1
公开(公告)日：2005-07-28
申请号：PCT/US2004/022115
申请日：2004-07-12
申请人： BRACCO IMAGING S.P.A. , CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Ed , NANJAPPAN, Palaniappa , RAJU, Natarajan , SWENSON, Rolf, E. , TWEEDLE,Michael , RAMALINGAM, Kondareddiar
发明人： CAPPELLETTI, Enrico , LATTUADA, Luciano , LINDER, Karen, E. , MARINELLI, Ed , NANJAPPAN, Palaniappa , RAJU, Natarajan , SWENSON, Rolf, E. , TWEEDLE,Michael , RAMALINGAM, Kondareddiar
IPC分类号： A61K51/00
CPC分类号： A61K51/088 , A61K51/0493 , C07K7/086 , C07K14/57572
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 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。还提供了用于制备放射治疗剂的方法和试剂盒。

10. 发明申请

WO2004065407A3 IMPROVED GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
公开(公告)号：WO2004065407A3
公开(公告)日：2004-08-05
申请号：PCT/US2003/041328
申请日：2003-12-24
申请人： BRACCO IMAGING S.P.A. , 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： A61K49/00
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.

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