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1. 发明授权

US5795561A Radioiodinated phospholipid ether analogues 失效
标题翻译：放射性碘化磷脂类似物
公开(公告)号：US5795561A
公开(公告)日：1998-08-18
申请号：US304259
申请日：1994-09-12
申请人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
发明人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
IPC分类号： A61K51/04 , C07B59/00 , C07F9/10 , A61K51/00 , A61M36/14
CPC分类号： A61K51/0408 , A61K31/685 , C07B59/004 , C07F9/10 , A61K2123/00
摘要： Novel radioiodinated analogues of naturally-occurring phospholipid ethers are tumor-specific and have a triglycerol backbone structure which, in certain embodiments, is substituted at the 3-position with an alkyl phosphocholine and include a monoiodinated benzoyl side chain substituted at the 2-position in accordance with the general formula: ##STR1## where n=1-15 ##STR2## M=0-15; Z=.sup.123 I, .sup.125 I, and .sup.131 I; Y=NH.sub.2, NR.sub.2, and NR.sub.3, and R=alkyl, aralkyl.
摘要翻译：天然存在的磷脂醚的新型放射性碘化物类似物是肿瘤特异性的，并且具有三甘油主链结构，其在某些实施方案中在3-位被烷基磷酸胆碱取代，并且包括在2-位取代的单碘化苯甲酰侧链符合以下通式：其中n = 1-15 M = 0-15; Z = 123I，125I和131I; Y = NH2，NR2和NR3，R =烷基，芳烷基。

2. 发明授权

US5087721A Radioiodinated phosphate esters 失效
标题翻译：放射碘化磷酸酯
公开(公告)号：US5087721A
公开(公告)日：1992-02-11
申请号：US602157
申请日：1990-10-22
申请人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
发明人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
IPC分类号： A61K51/04 , C07B59/00 , C07F9/10
CPC分类号： C07F9/10 , A61K31/685 , A61K51/0408 , C07B59/004 , A61K2123/00
摘要： Novel radioiodinated analogues of naturally-occurring phospholipid ethers are tumor-specific and have a triglycerol backbone structure which is substituted at the 3-position with an alkyl phosphocholine and include a monoiodinated benzoyl side chain substituted at either the 1- or 2-position. In some embodiments of the invention, the monoiodinated aralkyl side chain may be substituted directly onto alkyl phosphocholine in accordance with general Formula: provided that one and only one of X or Y is a monoiodinated aralkyl ##STR1## where Y=NH.sub.2, NR.sub.2, NR.sub.3, NR.sub.2 R'R=alkyl, aralkylR'=a monoiodinated aralkyl, such as ##STR2## Z=.sup.122 I, .sup.123 I, .sup.125 I, and .sup.131 I n=1-15X=a monoiodinated aralkyl, like R', where n=1-15; or an alkyl, such as --CH.sub.2 --(CH).sub.m --CH.sub.3, where m=1-15.
摘要翻译：天然存在的磷脂醚的新型放射性碘化物类似物是肿瘤特异性的，并且具有在3-位被烷基磷酸胆碱取代的三甘油主链结构，并且包括在1-位或2-位取代的单碘化苯甲酰侧链。在本发明的一些实施方案中，单碘化芳烷基侧链可以根据通式直接取代到烷基磷酸胆碱上：条件是X或Y中的一个并且仅一个是单碘化芳烷基，其中Y = NH 2，NR 2，NR 3 ，NR2R'R =烷基，芳烷基R'=单碘化芳烷基，例如Z = 122I，123I，125I和131I，n = 1-15 X =单碘化芳烷基，如R'，其中n = 1- 15; 或烷基，例如-CH 2 - （CH）m -CH 3，其中m = 1-15。

3. 发明授权

US5347030A Radioiodinated phospholipid ether analogues and methods of using same 失效
标题翻译：放射性碘化磷脂类似物及其使用方法
公开(公告)号：US5347030A
公开(公告)日：1994-09-13
申请号：US833303
申请日：1992-02-10
申请人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
发明人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner , Terushi Haradahira
IPC分类号： A61K51/04 , C07B59/00 , C07F9/10 , C07F9/09
CPC分类号： A61K51/0408 , A61K31/685 , C07B59/004 , C07F9/10 , A61K2123/00
摘要： Novel radioiodinated analogues of naturally-occurring phospholipid ethers are tumor-specific and have a triglycerol backbone structure which, in certain embodiments, is substituted at the 3-position with an alkyl phosphocholine and include a monoiodinated benzoyl side chain substituted at the 2-position in accordance with the general formula: ##STR1## where n= 1-15 ##STR2## m= 0-15; Z=.sup.123 I, .sup.125 I, and .sup.131 I; Y=NH.sub.2, NR.sub.2, and NR.sub.3, and R=alkyl, aralkyl.
摘要翻译：天然存在的磷脂醚的新型放射性碘化物类似物是肿瘤特异性的，并且具有三甘油主链结构，其在某些实施方案中在3-位被烷基磷酸胆碱取代，并且包括在2-位取代的单碘化苯甲酰侧链根据以下通式：其中n = 1-15 或： m = 0-15; Z = 123I，125I和131I; Y = NH2，NR2和NR3，R =烷基，芳烷基。

4. 发明授权

US4965391A Radioiodinated phospholipid ether analogues 失效
标题翻译：放射性碘化磷脂类似物
公开(公告)号：US4965391A
公开(公告)日：1990-10-23
申请号：US112865
申请日：1987-10-23
申请人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner
发明人： Raymond E. Counsell , Karen L. Meyer , Susan W. Schwendner
IPC分类号： A61K51/04 , C07B59/00 , C07F9/10
CPC分类号： C07F9/10 , A61K31/685 , A61K51/0408 , C07B59/004 , A61K2123/00
摘要： Novel radioiodinated analogues of naturally occurring phospholipid ethers are tumor-specific to enable selective visualization of neoplastic lesions by gamma-camera scintigraphy. The novel compounds enable a physician to differentiate neoplastic lesions from non-neoplastic lesions in a manner not heretofore available.
摘要翻译：天然存在的磷脂醚的新型放射性碘化物类似物是肿瘤特异性的，以通过γ相机闪烁扫描技术选择性地观察肿瘤病变。新型化合物使得医师能够以迄今未有的方式将肿瘤病变与非肿瘤性病变区分开来。

5. 发明授权

US4933157A Radioiodinated arylaliphatic ether analogues of cholesterol 失效
标题翻译：胆固醇的放射碘化芳基脂肪醚类似物
公开(公告)号：US4933157A
公开(公告)日：1990-06-12
申请号：US212196
申请日：1988-06-27
申请人： Raymond E. Counsell , Mohamed K. Ruyan , Susan W. Schwendner , Laura E. Deforge
发明人： Raymond E. Counsell , Mohamed K. Ruyan , Susan W. Schwendner , Laura E. Deforge
IPC分类号： C07J9/00
CPC分类号： C07J9/00
摘要： Novel radioiodinated analogues of naturally-occurring cholestrol esters, arylaliphatic cholesteryl ethers, are selective for low density lipoproteins and have been shown to be successful imaging agents for adrenal glands. The arylaliphatic cholesteryl ethers have the general formula: ##STR1## where X is a radioactive isotope of iodine and n is an integer between 1 and 20. Two illustrative examples, m-iodobenzyl cholesteryl ether and 12-(m-iodophenyl) dodecyl cholesteryl ether, were radiolabeled with .sup.125 I by an isotope exchange reaction. Tissue distribution studies indicate significant accumulation of the cholesteryl ethers in the adrenal glands, and to a lesser extent in the liver. The cholesteryl ethers selectively incorporate into plasma lipoproteins as determined by polyacrylamide gel electrophoresis.
摘要翻译：天然存在的胆甾醇酯，芳基脂族胆固醇醚的新型放射性碘化物类似物对于低密度脂蛋白是选择性的，并且已被证明是用于肾上腺的成功的成像剂。芳基脂族胆甾醇醚具有以下通式：其中X是碘的放射性同位素，n是1至20之间的整数。两个说明性实例，间 - 碘苄基胆固醇醚和12-（间碘苯基）十二烷基胆固醇醚用125I通过同位素交换反应进行放射性标记。组织分布研究表明胆固醇醚在肾上腺中的显着积累，在肝脏中的程度较小。通过聚丙烯酰胺凝胶电泳测定，胆固醇醚选择性地掺入到血浆脂蛋白中。

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