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公开(公告)号：US5344639A
公开(公告)日：1994-09-06
申请号：US719715
申请日：1991-06-26
申请人： Kwok W. Chiu , Wassif Hussain , John R. Thornback
发明人： Kwok W. Chiu , Wassif Hussain , John R. Thornback
IPC分类号： A61K49/00 , C07K5/02 , C07K5/06 , A61B5/055 , C07C229/00
CPC分类号： C07K5/022 , Y10T436/24
摘要： The present invention relates to a contrast agent for NMR imaging constituted by a complex between a chelating agent and paramagnetic metal cations, wherein said complex corresponds to the formula I: ##STR1## or a physiologically acceptable salt of this complex, in which formula: n and n' are whole numbers from 1 to 4R.sub.1 -R.sub.7 are selected from among H, a halogen, alkyl, alkoxy, aryl, alkenyl, and cycloalkyl groups; with the alkyl groups being optionally substituted by halogen, alkoxy, alkyl, nitrile, nitro or amino; >C(R.sub.6, R.sub.7) can in addition represent >C=O;the three substituents Y are identical or different and represent H or an ionic equivalent of a divalent or trivalent paramagnetic metal cation or of a physiologically acceptable cation derived from an inorganic or organic base,with the condition that at least two of the substituents Y represent ionic equivalents of paramagnetic metal cations.
摘要翻译： 本发明涉及由螯合剂和顺磁性金属阳离子之间的络合物构成的NMR成像造影剂，其中所述复合物对应于该络合物的式I：t，式中n和n'为 1至4个R 1 -R 7选自H，卤素，烷基，烷氧基，芳基，烯基和环烷基; 烷基，腈，硝基或氨基任选被烷基取代; > C（R 6，R 7）可以另外表示> C = O; 三个取代基Y相同或不同，表示二价或三价顺磁金属阳离子或衍生自无机或有机碱的生理学上可接受的阳离子的H或离子当量，条件是至少两个取代基Y表示离子 顺磁金属阳离子的当量。
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公开(公告)号：US5276147A
公开(公告)日：1994-01-04
申请号：US510958
申请日：1990-04-19
IPC分类号： C07D213/36 , A61K51/00 , A61K51/04 , C07C323/60 , C07D207/32 , C07D207/33 , C07D207/335 , C07D213/38 , A61K49/02
CPC分类号： C07D213/38 , A61K51/0478 , C07C323/60 , C07D207/335 , A61K2123/00
摘要： The subject of the present invention is compounds which correspond to the following general formula: ##STR1## in which R.sub.1 and R.sub.3 independently of one another represent H, an alkyl, alkenyl, cycloalkyl, aryl, arylalkyl or an alkylaryl group, a heterocycle, or groups which are unsubstituted or substituted, in particular by one or more hydroxyl or alkoxy groups or halogen;n represents an integer from 1 to 5;i in each case takes values from 1 to n for the n successive ##STR2## links; R.sub.2, R.sub.4.sup.i and R.sub.5.sup.i independently of one another represent H, an alkyl, alkenyl, aryl, alkoxy, hydroxyalkyl, alkoxyalkyl, amido, acyl or carboxyalkyl group, or a salt, or an alkyl ester of the latter; or R.sub.4.sup.i and R.sub.5.sup.i together form an oxo group ##STR3## R.sub.6 and R.sub.7 represent H, or R.sub.6 and R.sub.7 together form an oxo group ##STR4## x represents a 5- or 6-membered heterocycle which contains at least one nitrogen atom, or, in the event that ##STR5## where R.sub.8 and R.sub.9 independently represent H, alkyl, aryl or arylalkyl, and R.sub.10 represents H, alkyl, aryl or arylalkyl.The present invention likewise relates to coordination complexes between these ligands and a metal as well as to kits containing these ligands and to reagents which permit the formation of a coordination complex between the ligand and the metals. More particularly, the present invention relates to complexes between these ligands and technetium .sup.99m Tc, which complexes can be used as diagnostic agents for brain imaging, heart imaging and blood imaging.
摘要翻译： 本发明的主题是对应于以下通式的化合物：（*化学结构*）其中R 1和R 3彼此独立地表示H，烷基，烯基，环烷基，芳基，芳基烷基或烷基芳基的I， 或未被取代或特别被一个或多个羟基或烷氧基或卤素取代的基团; n表示1〜5的整数， 我在每种情况下为n个连续（*化学结构*）链接获取1到n的值; R2，R4i和R5i彼此独立地表示H，烷基，烯基，芳基，烷氧基，羟烷基，烷氧基烷基，酰胺基，酰基或羧基烷基，或其盐或后者的烷基酯; 或者R4i和R5i一起形成氧基（*化学结构*）R6和R7代表H，或R6和R7一起形成氧代基（*化学结构*）x表示至少含有5或6元杂环 （*化学结构*）（*化学结构*），其中R8和R9独立地表示H，烷基，芳基或芳基烷基，R10表示H，烷基，芳基或芳基烷基。 本发明同样涉及这些配体和金属之间的配位络合物，以及含有这些配体的试剂盒和允许在配体和金属之间形成配位络合物的试剂。 更具体地，本发明涉及这些配体和锝99mTc之间的配合物，其复合物可用作脑成像，心脏成像和血液成像的诊断剂。
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公开(公告)号：US5081232A
公开(公告)日：1992-01-14
申请号：US194285
申请日：1988-05-16
CPC分类号： A61K51/0497 , A61K51/04 , C07F13/005 , A61K2123/00
摘要： Complexes useful as radiopharmaceuticals contain the .sup.99m Tc-NO moiety and up to four organic ligands which confer biological target-seeking properties on the complex. Preferred are mono-cationic complexes, particularly having the formula[.sup.99m Tc(NO)L.sub.2 X].sup.+where X is halide or pseudohalide and L is a bidentate ligand for Technetium, which have interesting properties for use as heart visualizing agents. Examples of ligands include di-(dialkyl and diphenyl)phosphinoethanes and o-phenylenebisdimethylarsine. The complexes may be made by reacting generator eluate pertechnetate with a hydroxylamine salt and with the ligands, preferably in a single step by providing a reaction mixture containing the three reagents optionally in the presence of a reducing agent.
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