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1. 发明授权

US6149890A Chelated complexes of paramagnetic metals with low toxicity 失效
标题翻译：顺磁金属的螯合络合物具有低毒性
公开(公告)号：US6149890A
公开(公告)日：2000-11-21
申请号：US61036
申请日：1998-04-16
申请人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
发明人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
IPC分类号： C07D401/06 , A61K49/00 , A61K49/06 , C07D257/02 , C07F5/00 , A61B5/055 , C07D225/00
CPC分类号： A61K49/06 , C07D257/02
摘要： Compounds of formulae (I) and (II) ##STR1## wherein the R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.
摘要翻译：其中R，R 1，R 2，R 3和R 4基团具有本发明中定义的含义的式（I）和（II）化合物是用于金属离子的螯合剂。化合物（I）和（II）与顺磁离子的配合物可用作M.R.I.的对比剂。成像。

2. 发明授权

US06177562B1 Chelated complexes of paramagnetic metals with low toxicity 有权
标题翻译：顺磁金属的螯合络合物具有低毒性
公开(公告)号：US06177562B1
公开(公告)日：2001-01-23
申请号：US09597979
申请日：2000-06-20
申请人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
发明人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
IPC分类号： C07D25702
CPC分类号： A61K49/06 , C07D257/02
摘要： Compounds of formulae (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.
摘要翻译：其中R，R 1，R 2，R 3和R 4基团具有本发明中定义的含义的式（I）和（II）化合物是用于金属离子的螯合剂。化合物（I）和（II）与顺磁离子的配合物可用作M.R.I.的对比剂。成像。

3. 再颁专利

USRE38329E1 Chelated complexes of paramagnetic metals with low toxicity 有权
标题翻译：顺磁金属的螯合络合物具有低毒性
公开(公告)号：USRE38329E1
公开(公告)日：2003-11-25
申请号：US10157462
申请日：2002-09-27
申请人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
发明人： Fulvio Uggeri , Franco Fedeli , Alessandro Maiocchi , Maurizio Franzini , Mario Virtuani
IPC分类号： A61B5055
CPC分类号： A61K49/06 , C07D257/02
摘要： Compounds of formula (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.

4. 发明申请

US20110117015A1 Diagnostic Agents Selective Against Metalloproteases 有权
标题翻译：诊断药物选择性抗金属蛋白酶
公开(公告)号：US20110117015A1
公开(公告)日：2011-05-19
申请号：US13000794
申请日：2009-07-21
申请人： Armando Rossello , Elisa Nuti , Stanislava Ivanova Avramova , Fulvio Uggeri , Alessandro Maiocchi
发明人： Armando Rossello , Elisa Nuti , Stanislava Ivanova Avramova , Fulvio Uggeri , Alessandro Maiocchi
IPC分类号： A61K51/04 , C07C311/01 , C07D209/48 , C07D403/02 , C07D241/02 , C07D403/14 , A61K31/18 , A61K31/4035 , A61K31/497 , A61K49/00 , A61P9/10 , A61P25/28 , A61P9/00 , A61P37/02
CPC分类号： A61K49/0017 , A61K49/085 , A61K49/10 , A61K49/101 , A61K49/103 , A61K49/105 , A61K49/106 , A61K49/221 , A61K51/0497
摘要： The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.
摘要翻译：本发明涉及具有对金属蛋白酶MMP的亲和力的芳基 - 磺酰氨基化合物，其具有式（I），其中R，R 1，R 2，R 3，G和n具有说明书中报道的含义，适当地用诊断成像部分或甚至放射治疗部分。本发明还涉及其制备方法，包含它们的药物组合物及其作为诊断显像剂或放射治疗剂的用途。

5. 发明授权

US5424423A Intermediates for chelating agents with prefixed symmetry and process for their preparation 失效
标题翻译：具有前缀对称性的螯合剂中间体及其制备方法
公开(公告)号：US5424423A
公开(公告)日：1995-06-13
申请号：US30007
申请日：1993-02-26
申请人： Fulvio Uggeri , Pier L. Anelli , Marcella Murru , Mario Virtuani
发明人： Fulvio Uggeri , Pier L. Anelli , Marcella Murru , Mario Virtuani
IPC分类号： C07D257/02 , C07D405/06 , C07D487/14 , C07D487/18 , C07D257/00
CPC分类号： C07D405/06 , C07D257/02 , C07D487/14
摘要： The preparation of compounds of formula (I), wherein R and R.sub.1 have the meanings specified in claim 1, is disclosed compounds (I) are useful intermediates for the preparation of chelating agents.
摘要翻译： PCT No.PCT / EP91 / 01546 Sec。 371日期：1993年2月26日 102（e）日期1993年2月26日PCT 1991年8月14日PCT PCT。公开号WO92 / 04336 日本3月19日公开。式（I）化合物的制备，其中R和R 1具有权利要求1中所定义的含义，化合物（I）是制备螯合剂的有用中间体。

6. 发明授权

US09012483B2 Use of L-Histidine and derivatives thereof 有权
标题翻译： L-组氨酸及其衍生物的应用
公开(公告)号：US09012483B2
公开(公告)日：2015-04-21
申请号：US14235128
申请日：2012-07-24
申请人： Baranyai Zsolt , Ernö Brücher , Simona Bussi , Alessandro Maiocchi , Fulvio Uggeri
发明人： Baranyai Zsolt , Ernö Brücher , Simona Bussi , Alessandro Maiocchi , Fulvio Uggeri
IPC分类号： A61K31/415 , A61K31/28 , A61K31/4172
CPC分类号： A61K31/4172 , A61K31/28
摘要： The present invention discloses the use of L-Histidine to reduce Gadolinium accumulation into target organs, preventing its toxic effects, after administration of gadolinium based contrast agents. The invention thus, also disclose the use of L-Histidine to prevent the NSF syndrome in patients with renal functionality impairment. A kit of part is also disclosed by the use of which toxicity associated to free Gd3+, deriving from GDBCA, is prevented by oral administration of L-histidine before administration of the contrast agent. A method for the prevention of toxic metal accumulation which consists in the administration, preferably by the oral route, of L-Histidine is also disclosed. L-Histidine is preferably administered as a single oral dose comprised from 0.2-20 g.
摘要翻译：本发明公开了在施用钆基造影剂之后，L-组氨酸用于减少钆累积到靶器官中，防止其毒性作用。因此，本发明还公开了使用L-组氨酸来预防肾功能损害患者的NSF综合征。还通过使用与给予造影剂之前通过口服给予L-组氨酸来防止与GDBCA相关的游离Gd3 +相关毒性的试剂盒。还公开了一种用于预防毒性金属积聚的方法，该方法包括优选通过口服途径施用L-组氨酸。 L-组氨酸优选以0.2-20g的单一口服剂量施用。

7. 发明授权

US09694090B2 Process for preparing hyperpolarized substrates and method for MRI 有权
公开(公告)号：US09694090B2
公开(公告)日：2017-07-04
申请号：US13639682
申请日：2011-04-08
申请人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
发明人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
IPC分类号： A61K49/10 , A61B5/05 , A61M5/00 , A61B5/055
CPC分类号： A61K49/10 , A61B5/055 , A61M5/007
摘要： The present invention generally relates to a process for the preparation of aqueous solutions of hyperpolarized molecules ready for use in in-vivo MR diagnostic imaging, the use thereof as MRI contrast agent in investigation methods for producing diagnostic MR images of a human or non-human animal body organ, region or tissue.

8. 发明申请

US20130096420A1 Process For Preparing Hyperpolarized Substrates And Method For MRI 有权
标题翻译：制备超极化基质的方法及MRI的方法
公开(公告)号：US20130096420A1
公开(公告)日：2013-04-18
申请号：US13639682
申请日：2011-04-08
申请人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
发明人： Silvio Aime , Giovanni Battista Giovenzana , Fabio Tedoldi , Alessandro Maiocchi , Fulvio Uggeri , Pernille Rose Jensen , Magnus Karlsson , Mathilde H. Lerche , Massimo Visigalli , Marco Crosetti , Luisa Poggi
IPC分类号： A61K49/10 , A61M5/00 , A61B5/055
CPC分类号： A61K49/10 , A61B5/055 , A61M5/007
摘要： The present invention generally relates to a process for the preparation of aqueous solutions of hyperpolarized molecules ready for use in in-vivo MR diagnostic imaging, the use thereof as MRI contrast agent in investigation methods for producing diagnostic MR images of a human or non-human animal body organ, region or tissue.
摘要翻译：本发明一般涉及准备用于体内MR诊断成像的超极化分子的水溶液的制备方法，其用于生成人或非人的诊断性MR图像的调查方法中的MRI造影剂动物体器官，区域或组织。

9. 发明授权

US6099824A Benzyloxy derivatives of DTPA for MRI 失效
标题翻译：用于MRI的DTPA的苄氧基衍生物
公开(公告)号：US6099824A
公开(公告)日：2000-08-08
申请号：US904646
申请日：1997-08-01
申请人： Pier Lucio Anelli , Andrea Beltrami , Fulvio Uggeri , Mario Virtuani
发明人： Pier Lucio Anelli , Andrea Beltrami , Fulvio Uggeri , Mario Virtuani
IPC分类号： A61K49/06 , C07C229/16 , C07C229/22 , C07C229/76 , A61B5/055
CPC分类号： C07C229/76 , A61K49/06 , C07C229/16 , C07C229/22 , Y10S514/836
摘要： Compounds which can chelate paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI), the compounds having formula (I) ##STR1## wherein R is a --(CH.sub.2).sub.m --O--R.sub.2 group or hydrogen,R.sub.2 is a (C.sub.6 -C.sub.10) aryl, or an alkyl(C.sub.1 -C.sub.5)-aryl(C.sub.6 -C.sub.10) group, substituted or not by a group L corresponding to a OH group or a OR.sub.3 group, wherein R.sub.3 is a linear or branched (C.sub.1 -C.sub.5) alkyl group; or L is NH.sub.2, halogen, COOH or CONR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently hydrogen, or a linear or branched (C.sub.1 -C.sub.5) alkyl which can be substituted by 1-6 hydroxy groups and/or 1-6 alkoxy groups,R.sub.1 can have the same meanings as R, independently from it, except for hydrogen,Z is independently OH or OR.sub.6, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as previously defined, and R.sub.6 is a (C.sub.1 -C.sub.10) alkyl, linear or branched, which can be substituted by 1-6 hydroxyl and/or alkoxyl groups,m is between 1 and 5.
摘要翻译：可以螯合顺磁性双金属和三价金属离子的化合物，它们与所述金属离子的螯合物以及它们在磁共振成像（MRI）中作为造影剂的用途，具有式（I）的化合物其中R是 - （CH 2）m O-R 2 基团或氢，R2是（C6-C10）芳基或（C1-C5） - 芳基（C6-C10）烷基，被对应于OH基团或OR3基团的基团L取代或不被取代，其中R3 是直链或支链（C1-C5）烷基; 或L是NH 2，卤素，COOH或CONR 4 R 5，其中R 4和R 5独立地是氢，或可被1-6个羟基和/或1-6个烷氧基取代的直链或支链（C1-C5）烷基，R1可以具有与R独立的含义，除氢外，Z独立地为OH或OR 6，或NR 4 R 5，其中R 4和R 5如前所定义，R 6为直链或支链的（C1-C10）烷基，其可以是被1-6个羟基和/或烷氧基取代，m在1和5之间。

10. 发明授权

US5539105A Intermediates for chelating agents with prefixed symmetry and process for their preparation 失效
标题翻译：具有前缀对称性的螯合剂中间体及其制备方法
公开(公告)号：US5539105A
公开(公告)日：1996-07-23
申请号：US415529
申请日：1995-04-03
申请人： Fulvio Uggeri , Pier L. Anelli , Marcella Murru , Mario Virtuani
发明人： Fulvio Uggeri , Pier L. Anelli , Marcella Murru , Mario Virtuani
IPC分类号： C07D257/02 , C07D405/06 , C07D487/14 , C07D257/00
CPC分类号： C07D405/06 , C07D257/02 , C07D487/14
摘要： The preparation of compounds of formula (I), wherein R and R.sup.1 have the meanings specified in claim 1, is disclosed compounds (I) are useful intermediates for the preparation of chelating agents.
摘要翻译：式（I）化合物的制备，其中R和R 1具有权利要求1中所定义的含义，化合物（I）是制备螯合剂的有用的中间体。

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