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1. 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。

2. 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。

3. 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。

4. 发明专利

JP2010116415A Improved gastrin-related peptide compound 有权
标题翻译：改进的与胃蛋白相关的肽化合物
公开(公告)号：JP2010116415A
公开(公告)日：2010-05-27
申请号：JP2010015759
申请日：2010-01-27
申请人： Bracco Imaging Spa , ブラッコ・イメージング・ソシエタ・ペル・アチオニBracco Imaging S.P.A.
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： C07K14/595 , A61K45/00 , A61K51/00 , A61K51/08 , A61P35/00 , C07K19/00
CPC分类号： A61K51/088 , C07K7/086
摘要： PROBLEM TO BE SOLVED: To provide a new gastrin releasing peptide (GRP) compound which is useful as a diagnostic contrast agent or a radiotherapeutic agent. SOLUTION: The compound is expressed by the formula: M-N-O-P-G [wherein, M is an optical label or a metal chelator optionally forming a complex with a radionuclide; N is 0, an alpha amino acid or a cyclic group- or other linking group-having non-alpha amino acid; 0 is an alpha amino acid or a cyclic group-having non-alpha amino acid; P is 0, an alpha amino acid or a cyclic group- or other linking group-having non-alpha amino acid; and G is a GRP receptor targeting peptide, where at least one of N, O and P is a cyclic group-having non-alpha amino acid]. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供可用作诊断造影剂或放射治疗剂的新的胃泌素释放肽（GRP）化合物。解决方案：该化合物由下式表示：M-N-O-P-G [其中，M是可选地与放射性核素形成络合物的光学标记或金属螯合剂; N为0，α氨基酸或具有非α氨基酸的环状基团或其它连接基团; 0是α氨基酸或具有非α氨基酸的环状基团; P为0，α氨基酸或具有非α氨基酸的环状基团或其它连接基团; 并且G是一种GRP受体靶向肽，其中N，O和P中的至少一个是具有非α氨基酸的环状基团]。版权所有（C）2010，JPO＆INPIT

5. 发明公开

EP2291075A4 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译：胃泌素释放肽CONNECTIONS
公开(公告)号：EP2291075A4
公开(公告)日：2012-08-22
申请号：EP09751329
申请日：2009-05-19
申请人： BRACCO IMAGING SPA
发明人： LATTUADA LUCIANO , CAPPELLETTI ENRICO , LINDER KAREN E , NUNN ADRIAN D , LANTRY LAURA
IPC分类号： A01N37/18 , A61K38/00 , C07K7/08
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.

6. 发明公开

EP1585549A4 IMPROVED GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译： VERBESSERTE PEPTIDVERBINDUNGEN ZUR GASTRINFREISETZUNG
公开(公告)号：EP1585549A4
公开(公告)日：2009-07-29
申请号：EP03800223
申请日：2003-12-24
申请人： BRACCO IMAGING SPA
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 , A61K51/08 , C07K7/08
CPC分类号： A61K51/088 , C07K7/086

7. 发明公开

EP1898962A4 GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
标题翻译：胃泌素释放肽CONNECTIONS
公开(公告)号：EP1898962A4
公开(公告)日：2013-01-09
申请号：EP06785507
申请日：2006-06-23
申请人： BRACCO IMAGING SPA
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 , A61K51/08
CPC分类号： A61K51/088 , A61K49/0002 , C07C269/04 , C07D257/00 , C07J41/0005 , C07J41/0011 , C07J43/003 , C07K14/57572 , C07C271/22

8. 发明专利

CA2803225C PROCESS FOR THE PREPARATION OF CONTRAST AGENTS 未知
公开(公告)号：CA2803225C
公开(公告)日：2018-01-02
申请号：CA2803225
申请日：2011-07-14
申请人： BRACCO IMAGING SPA
发明人： ANELLI PIER LUCIO , BROCCHETTA MARINO , CAPPELLETTI ENRICO , GAZZOTTI ORNELLA
IPC分类号： C07C231/10
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.

9. 发明专利

PT2593423E PROCESSO PARA A PREPARAÇÃO DE AGENTES DE CONTRASTE 未知
公开(公告)号：PT2593423E
公开(公告)日：2014-11-24
申请号：PT11731379
申请日：2011-07-14
申请人： BRACCO IMAGING SPA
发明人： ANELLI PIER LUCIO , BROCCHETTA MARINO , CAPPELLETTI ENRICO , GAZZOTTI ORNELLA
IPC分类号： C07C231/10

10. 发明专利

NO328627B1 未知
公开(公告)号：NO328627B1
公开(公告)日：2010-04-12
申请号：NO20032440
申请日：2003-05-28
申请人： BRACCO IMAGING SPA
发明人： ANELLI PIER LUCIO , BROCCHETTA MARINO , LUX GIOVANNA , CAPPELLETTI ENRICO
IPC分类号： A61K49/04 , C07C237/46 , C07B51/00 , C07C231/02 , C07C231/12 , C07D319/06
摘要： A process for the preparation of ( S)-N,N' -bis[2-hydroxy-1 (hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzenedicarboxamide (iopamidol) starting from 5-amino- N,N' -bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein -R is a group of formula A or B wherein R 1 is a hydrogen atom, a C 1 -C 4 straight or branched alkyl group or a C 1 -C 4 straight or branched alkoxy group, R 2 is hydrogen, a C 1 -C 4 straight or branched alkyl group or a C 1 -C 4 straight or branched alkoxy group and R 3 is a C 1 -C 4 straight or branched alkyl group, a trifluoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S) -2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions.

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