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1. 发明申请

WO1998005625A1 DIAGNOSTIC IMAGING CONTRAST AGENT WITH IMPROVED IN-SERUM-RELAXIVITY 审中-公开
标题翻译：诊断成像对比剂具有改善的血清 - 松弛度
公开(公告)号：WO1998005625A1
公开(公告)日：1998-02-12
申请号：PCT/EP1997004096
申请日：1997-07-28
申请人： BRACCO S.P.A. , DIBRA S.P.A. , CALABI, Luisella , MAIOCCHI, Alessandro , LOLLI, Marco , REBASTI, Fabrizio
发明人： BRACCO S.P.A. , DIBRA S.P.A.
IPC分类号： C07C229/16
CPC分类号： C07C229/26 , A61K49/06 , C07C229/36 , C07C229/76 , C07D209/20
摘要： Compounds of formula (I), either in their racemic or enantiomeric forms, wherein R is H or a C1-C20 alkyl chain, which may be interrupted by O, N, S, -CO-, -CH(OH)-, -CH(NH2)-, -CONH-, -NHCO-, -SO-, -SO2-, -SO2NH-, may be substituted by halogen atoms or -COOH groups or their ester or amide derivatives and which is interrupted or not or substituted or not by one or more cyclic R3 residues. R3 is a 5- or 6-membered optionally substituted carbocyclic or heterocyclic, saturated, unsaturated or aromatic cyclic unit, R1, R2 have the same meanings as R, independently from each other, except H, with the proviso that: when R1 and R2 are both C6H5-CH2-O-CH2-, R is different from either H or C6H5-CH2-O-CH2-; as well as the complexes of the compounds of formula (I) with metal ions and the salts thereof with physiologically acceptable organic bases. The compounds are used in the preparation of diagnostic imaging contrast agents and in particular of contrast agents exhibiting improved serum relaxivity.
摘要翻译：式（I）化合物，以其外消旋或对映体形式，其中R为H或C 1 -C 20烷基链，其可被O，N，S，-CO-， - CH（OH） - ， - CH（NH 2） - ， - CONH - ， - NHCO - ， - SO - ， - SO 2 - ， - SO 2 NH-可以被卤素原子或-COOH基团或其酯或酰胺衍生物取代，或不由一个或多个环状R 3残基。 R 3是5或6元任选取代的碳环或杂环，饱和，不饱和或芳族环状单元，R 1，R 2具有与R相同的含义，彼此独立地除H外，条件是：当R 1和R 2 均为C 6 H 5 -CH 2 -O-CH 2 - ，R不同于H或C 6 H 5 -CH 2 -O-CH 2 - ; 以及式（I）化合物与金属离子及其盐与生理上可接受的有机碱的配合物。该化合物用于制备诊断成像造影剂，特别是显示出改进的血清舒张性的造影剂。

2. 发明申请

WO2006136564A9 MULTIDENTATE AZA LIGANDS ABLE TO COMPLEX METAL IONS AND THE USE THEREOF IN DIAGNOSTICS AND THERAPY 审中-公开
标题翻译：多发AZA配体可复制金属离子及其在诊断和治疗中的应用
公开(公告)号：WO2006136564A9
公开(公告)日：2008-02-07
申请号：PCT/EP2006063368
申请日：2006-06-20
申请人： BRACCO IMAGING SPA , GIOVENZANA GIOVANNI BATTISTA , PALMISANO GIOVANNI , SISTI MASSIMO , CAVALLOTTI CAMILLA , AIME SILVIO , CALABI LUISELLA , SWENSON ROLF , KONDAREDDIAR RAMALINGAM , LATTUADA LUCIANO , MOROSINI PIERFRANCESCO
发明人： GIOVENZANA GIOVANNI BATTISTA , PALMISANO GIOVANNI , SISTI MASSIMO , CAVALLOTTI CAMILLA , AIME SILVIO , CALABI LUISELLA , SWENSON ROLF , KONDAREDDIAR RAMALINGAM , LATTUADA LUCIANO , MOROSINI PIERFRANCESCO
IPC分类号： C07D243/08 , A61K49/00 , A61K49/10 , A61K49/14 , A61K51/00 , A61P35/00 , C07C229/16 , C07C229/26 , C07D243/14 , C07D245/02 , C07F1/08 , C07F1/10 , C07F1/12 , C07F5/00 , C07F7/24 , C07F9/38 , C07F9/645 , C07F9/80 , C07F9/94 , C07F11/00 , C07F13/00 , C07F15/00 , C07F15/02
CPC分类号： C07C209/62 , A61K49/0002 , A61K49/085 , A61K49/106 , A61K49/122 , A61K49/14 , A61K51/088 , C07D243/08 , C07D243/14 , C07F9/301 , C07F9/3808 , C07F9/4816 , C07F9/645 , C07C211/50
摘要： Compounds of general formula (I): in which: R 1 , R 2 , R 3 , R 4 , R 5 and FG are as defined in the specification and claims, optionally conjugated with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes, as well as the salts thereof with physiologically compatible bases or acids.
摘要翻译：通式（I）的化合物：其中：R 1，R 2，R 3，R 4， R 5和FG如说明书和权利要求中所定义，任选地与能够与生理系统相互作用的合适分子缀合; 其螯合物与金属元素的二价离子的原子序数范围在20,31,39,42,43,44,49和57和83之间，放射性同位素以及其与生理上相容的碱基的盐或酸。

3. 发明申请

WO2006136564A1 MULTIDENTATE AZA LIGANDS ABLE TO COMPLEX METAL IONS AND THE USE THEREOF IN DIAGNOSTICS AND THERAPY 审中-公开
标题翻译：多发AZA配体可复制金属离子及其在诊断和治疗中的应用
公开(公告)号：WO2006136564A1
公开(公告)日：2006-12-28
申请号：PCT/EP2006/063368
申请日：2006-06-20
申请人： BRACCO IMAGING S.p.A. , GIOVENZANA, Giovanni, Battista , PALMISANO, Giovanni , SISTI, Massimo , CAVALLOTTI, Camilla , AIME, Silvio , CALABI, Luisella , SWENSON, Rolf , KONDAREDDIAR, Ramalingam , LATTUADA, Luciano , MOROSINI, Pierfrancesco
发明人： GIOVENZANA, Giovanni, Battista , PALMISANO, Giovanni , SISTI, Massimo , CAVALLOTTI, Camilla , AIME, Silvio , CALABI, Luisella , SWENSON, Rolf , KONDAREDDIAR, Ramalingam , LATTUADA, Luciano , MOROSINI, Pierfrancesco
IPC分类号： C07D243/08 , C07D243/14 , C07C229/16 , C07F9/38 , A61K49/14
CPC分类号： C07C209/62 , A61K49/0002 , A61K49/085 , A61K49/106 , A61K49/122 , A61K49/14 , A61K51/088 , C07D243/08 , C07D243/14 , C07F9/301 , C07F9/3808 , C07F9/4816 , C07F9/645 , C07C211/50
摘要： Compounds of general formula (I): in which: R 1 , R 2 , R 3 , R 4 , R 5 and FG are as defined in the specification and claims, optionally conjugated with a suitable molecule able to interact with physiological systems; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes, as well as the salts thereof with physiologically compatible bases or acids.
摘要翻译：通式（I）的化合物：其中：R 1，R 2，R 3，R 4， R 5和FG如说明书和权利要求中所定义，任选地与能够与生理系统相互作用的合适分子缀合; 其螯合物与金属元素的二价离子的原子序数范围为20,31,39,42,43,44,49和57和83之间，以及放射性同位素以及其与生理上相容的碱基的盐或酸。

4. 发明申请

WO2005093409A1 METHOD FOR THE IN VITRO DETERMINATION OF CELLULAR UPTAKE OF EXOGENOUS AND ENDOGENOUS SUBSTANCES USING NMR SHIFT AGENTS AND THE MAGIC ANGLE NMR TECHNIQUE 审中-公开
标题翻译：使用NMR转换剂和魔角NMR技术对外源和内源物质的细胞摄取进行体外测定的方法
公开(公告)号：WO2005093409A1
公开(公告)日：2005-10-06
申请号：PCT/EP2005/003058
申请日：2005-03-22
申请人： BRACCO IMAGING SPA , CALABI, Luisella , ALFIERI, Goffredo , BIONDI, Luca , DEMIRANDA, Mario , PALEARI, Lino , GHELLI, Stefano
发明人： CALABI, Luisella , ALFIERI, Goffredo , BIONDI, Luca , DEMIRANDA, Mario , PALEARI, Lino , GHELLI, Stefano
IPC分类号： G01N33/483
CPC分类号： G01N24/08
摘要： The present invention relates to a method for the in vitro quantitative determination of cellular uptake of exogenous or endogenous substances which method comprises applying MAS-NMR spectroscopy technique to an in vitro cellular sample, in combination with a shift agent. The said method is particularly advantageous as it find general applicability for a variety of substances and cell samples.
摘要翻译：本发明涉及体外定量测定外源或内源物质的细胞摄取的方法，该方法包括将MAS-NMR光谱技术与转移剂组合应用于体外细胞样品。所述方法是特别有利的，因为它找到了各种物质和细胞样品的普遍适用性。

5. 发明申请

WO9517910A3 PARAMAGNETIC DIAGNOSTIC FORMULATIONS AND THEIR METHOD OF USE 审中-公开
标题翻译：参考诊断制剂及其使用方法
公开(公告)号：WO9517910A3
公开(公告)日：1995-07-27
申请号：PCT/EP9403944
申请日：1994-11-28
申请人： BRACCO SPA , DIBRA SPA , AIME SILVIO , BOTTA MARIO , CALABI LUISELLA , PALEARI LINO
发明人： AIME SILVIO , BOTTA MARIO , CALABI LUISELLA , PALEARI LINO
IPC分类号： G01R33/28 , A61B5/055 , A61K49/00 , A61K49/06 , A61P43/00
CPC分类号： A61K49/06
摘要： This invention refers to a method for Magnetic Resonance Imaging (MRI) using proton signals of paramagnetic metal-ion complexes, based on the use of Chemical Shift Imaging (CSI) techniques, as well as Magnetic Resonance Spectroscopy (MRS) for the control and recording of biological parameters.
摘要翻译：本发明是基于使用化学位移成像（CSI）技术以及用于控制和记录的磁共振光谱（MRS），使用顺磁性金属离子络合物的质子信号的磁共振成像（MRI）的方法的生物参数。

6. 发明申请

WO2003008390A1 MULTIDENTATE AZA LIGANDS ABLE TO COMPLEX METAL IONS AND THE USE THEREOF IN DIAGNOSTICS AND THERAPY 审中-公开
标题翻译：多发AZA配体可复制金属离子及其在诊断和治疗中的应用
公开(公告)号：WO2003008390A1
公开(公告)日：2003-01-30
申请号：PCT/EP2002/007658
申请日：2002-07-10
申请人： BRACCO IMAGING S.P.A. , GIOVENZANA, Giovanni, Battista , PALMISANO, Giovanni , SISTI, Massimo , CAVALLOTTI, Camilla , AIME, Silvio , CALABI, Luisella
发明人： GIOVENZANA, Giovanni, Battista , PALMISANO, Giovanni , SISTI, Massimo , CAVALLOTTI, Camilla , AIME, Silvio , CALABI, Luisella
IPC分类号： C07D243/08
CPC分类号： C07D243/08 , A61K49/0002 , A61K49/101
摘要： Compounds of general formula (I):in which: R 1 is hydrogen, C 1 -C 2O alkyl, C 3 -C 10 cycloalkyl, C 4 -C 2O cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C 2 -C 10 alkylene group or an ortho disubstituted arylene; R 2 is hydrogen, C 1 -C 2O alkyl, C 3 -C 10 cycloalkyl, C 4 -C 2O cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R 3 , R 4 and R 5 are hydrogen, C 1 -C 20 alkyl, C 3 -C 10 cycloalkyl, C 4 -C 2O cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42,43,44,49, and between 57 and 83, and radioisotopes chosen among 203 Pb 67 Ga 68 Ga 72 As lll In 113 In 90 Y 97 Ru 62 Cu 64 Cu 52 Fe 52m Mn , 140 La 175 Yb 153 Sm 166 Ho 149 Pm 177 Lu 142 Pr 159 Gd 2l2 Bi 47 Sc 149 Pm 67 Cu, 111 Ag, 199 Au, 161 Tb and 51 Cr as well as the salts thereof with physiologically compatible bases or acids.
摘要翻译：通式（I）的化合物：其中：R 1是氢，C 1 -C 20烷基，C 3 -C 10环烷基，C 4 -C 20环烷基烷基，芳基，芳烷基或两个R 1一起形成直链或环状的C 2 -C 10亚烷基基团或邻二取代的亚芳基; R 2是氢，C 1 -C 20烷基，C 3 -C 10环烷基，C 4 -C 20环烷基烷基，任选被官能团取代的芳基或芳基烷基，其允许与能够与生理系统相互作用的合适分子缀合; R3，R4和R5是氢，C1-C20烷基，C3-C10环烷基，C4-C2O环烷基烷基，芳基，芳基烷基; 并且它们的螯合物与金属元素的二价离子的原子序数范围在20,31,39,42,44,44和57和83之间，并且放射性同位素选自< 68> Ga <72> As <111> In <113> In <90> Y 97 Cu 64 Mn 52 Mn> 52 Mn> 140 La> 175> Yb <153 > Sm <166> Ho <149> Pm <177> Lu <142> Pr <159> Gd <22> Bi 47> Sc <149> Cu，<111> Ag， 161> Tb和51 Cr以及其与生理上相容的碱或酸的盐。

7. 发明申请

WO1995017910A2 PARAMAGNETIC DIAGNOSTIC FORMULATIONS AND THEIR METHOD OF USE 审中-公开
标题翻译：顺铂诊断制剂及其使用方法
公开(公告)号：WO1995017910A2
公开(公告)日：1995-07-06
申请号：PCT/EP1994003944
申请日：1994-11-28
申请人： BRACCO S.P.A. , DIBRA S.P.A. , AIME, Silvio , BOTTA, Mario , CALABI, Luisella , PALEARI, Lino
发明人： BRACCO S.P.A. , DIBRA S.P.A.
IPC分类号： A61K49/00
CPC分类号： A61K49/06
摘要： This invention refers to a method for Magnetic Resonance Imaging (MRI) using proton signals of paramagnetic metal-ion complexes, based on the use of Chemical Shift Imaging (CSI) techniques, as well as Magnetic Resonance Spectroscopy (MRS) for the control and recording of biological parameters.
摘要翻译：本发明涉及基于使用化学位移成像技术以及磁共振波谱学的使用金属离子顺磁性复合物的质子信号的磁共振成像方法。该方法用于观察和记录生物参数。

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