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公开(公告)号：US5347030A
公开(公告)日：1994-09-13
申请号：US833303
申请日：1992-02-10
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。 -
公开(公告)号：US4965391A
公开(公告)日：1990-10-23
申请号：US112865
申请日：1987-10-23
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。
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公开(公告)号：US5795561A
公开(公告)日：1998-08-18
申请号：US304259
申请日：1994-09-12
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。 -
公开(公告)号：US5087721A
公开(公告)日：1992-02-11
申请号：US602157
申请日：1990-10-22
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。
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