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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。

6. 发明授权

US06255519B1 Radioiodinated phospholipid ether analogs and methods of using the same 有权
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：US06255519B1
公开(公告)日：2001-07-03
申请号：US09319406
申请日：1999-09-20
申请人： Raymond E. Counsell , Marc A. Longino , Anatoly N. Pinchuk , Mark A. Rampy , Jamey P. Weichert
发明人： Raymond E. Counsell , Marc A. Longino , Anatoly N. Pinchuk , Mark A. Rampy , Jamey P. Weichert
IPC分类号： C07F910
CPC分类号： C07F9/094 , A61K51/0408 , A61K2123/00 , C07B59/004 , C07F9/091
摘要： Improved radioiodinated phospholipid ether analogs are described which exhibit significant tumor avidity and longer plasma half-life relative to shorter chain analogs. Use of these compounds results in superior imaging and visualization of neoplastic lesions and tumor-specific cytotoxic cancer therapy.
摘要翻译：描述了改进的放射性碘化磷脂类似物，其相对于较短的链类似物显示显着的肿瘤亲合力和更长的血浆半衰期。这些化合物的使用导致肿瘤病变和肿瘤特异性细胞毒性治疗的优异成像和可视化。

7. 发明授权

US4873075A Polyiodinated triglyceride analogs as radiologic agents 失效
标题翻译：多碘化甘油三酯类似物作为放射剂
公开(公告)号：US4873075A
公开(公告)日：1989-10-10
申请号：US774498
申请日：1985-09-10
申请人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert , Susan P. Schwendner
发明人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert , Susan P. Schwendner
IPC分类号： A61K49/04 , A61K51/04 , A61K51/12 , C07C237/20
CPC分类号： C07C237/20 , A61K49/0433 , A61K49/0438 , A61K49/0461 , A61K51/0406 , A61K51/1217 , A61K2123/00
摘要： Novel iodinated arylaliphatic triglyceride analogs, as radiologic agents are liver and hepatocyte site-specific. The triglyceride backbone structure is preferably 1,3-disubstituted or 1,2,3-trisubstituted with, in some embodiments, a 3-substituted-2,4,6-triiodophenyl aliphatic chain wherein the chain has a structure similar to naturally occurring fatty acids. In another embodiment, a monoiodophenyl aliphatic chain is utilized. Any position remaining on the triglyceride backbone is substituted with a saturated or unsaturated aliphatic hydrocarbon chain of the type found in naturally occurring fatty acids. The triglyceride analogs can be radioiodinated. In a preferred embodiment, a lipid emulsion is provided as the carrier vehicle.
摘要翻译：新型碘化芳基脂肪酸甘油三酯类似物，作为放射剂是肝和肝细胞位点特异性。甘油三酯主链结构优选在一些实施方案中被3-取代-2,4,6-三碘苯基脂族链进行1,3-二取代或1,2,3-三取代，其中链具有类似于天然存在的脂肪酸。在另一个实施方案中，使用单碘苯基脂族链。在甘油三酯主链上残留的任何位置被天然存在的脂肪酸中所发现类型的饱和或不饱和脂族烃链所取代。甘油三酯类似物可以放射性碘化。在优选的实施方案中，提供脂质乳剂作为载体载体。

8. 发明授权

US4241088A 1-(Trialkylamino)-3-(phenylphenoxy)-2-propanol quarternary salts 失效
标题翻译： 1-（三烷基氨基）-3-（苯基苯氧基）-2-丙醇季盐
公开(公告)号：US4241088A
公开(公告)日：1980-12-23
申请号：US780880
申请日：1977-03-24
申请人： Raymond E. Counsell , Benedict R. Lucchesi
发明人： Raymond E. Counsell , Benedict R. Lucchesi
IPC分类号： C07D303/22 , A61K31/165
CPC分类号： C07D303/22 , Y10S514/821
摘要： The above captioned compounds exhibit potent and long acting anti-arrhythmic activity while lacking the undesirable side effects, e.g. .beta.-adrenergic receptor blocking activity and local anesthetic activity, characteristic of related prior art compounds.
摘要翻译：上述标题化合物表现出有效的长效抗心律不齐活性，同时缺乏不良副作用，例如， β-肾上腺素能受体阻断活性和局部麻醉活性，相关现有技术化合物的特征。

9. 发明授权

US07582279B2 Blood-pool carrier for lipophilic imaging agents 失效
标题翻译：用于亲脂显像剂的血液池载体
公开(公告)号：US07582279B2
公开(公告)日：2009-09-01
申请号：US10692311
申请日：2003-10-23
申请人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert
发明人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K49/0461 , A61K9/1075 , A61K9/1275 , A61K49/0433 , A61K49/1806 , A61K51/0406 , A61K51/0478 , A61K51/1217 , B82Y5/00 , Y10S514/938 , Y10S977/829 , Y10S977/905 , Y10S977/927 , Y10S977/93
摘要： A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
摘要翻译：用作脂溶性成像剂或水溶性成像剂的亲脂性衍生物的血液池选择性递送载体的表面改性脂蛋白样水包油乳液。血液池选择性输送载体在血液中保持数小时，显示出非常少的早期肝脏螯合，并在24小时内从血液中清除。油相的平均直径小于150nm，其最小化网状内皮系统的螯合。用聚乙二醇修饰的磷脂修饰油相的表面以防止与肝细胞的受体位点的正常相互作用。放射摄影成像中，放射性或稳定的合成或半合成多卤甘油三酸酯如2-油酰甘油-1,3-双[7-（3-氨基-2,4,6-三碘苯基）庚酸酯]或脂溶性衍生物的传统的水溶性造影剂，如碘，脂肪族和代谢酸的脂肪族酯可以并入脂蛋白样乳液颗粒的亲脂性核心中。

10. 发明授权

US6103216A Hepatocyte-selective oil-in-water emulsion 失效
标题翻译：肝细胞选择性水包油乳剂
公开(公告)号：US6103216A
公开(公告)日：2000-08-15
申请号：US737429
申请日：1996-11-15
申请人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert , Douglas A. Bakan
发明人： Raymond E. Counsell , Marc A. Longino , Jamey P. Weichert , Douglas A. Bakan
IPC分类号： A61K9/107 , A61K9/127 , A61K47/14 , A61K49/00 , A61K49/04 , A61K49/18 , A61K51/12 , B01F3/00
CPC分类号： A61K9/1075 , A61K49/0433 , A61K49/1806 , A61K51/1217 , A61K9/1275 , Y10S514/893 , Y10S514/894 , Y10S514/938 , Y10S514/941 , Y10S516/923 , Y10S516/93
摘要： A heat and shelf-stable oil-in-water emulsion useful as a tissue or cell-selective delivery vehicle. Radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate] or 2-oleoylglycerol-1,3-bis[.omega.-(3,5-bis-trifluoromethyl)-heptanoate] or phenyl acetate, can be incorporated into the lipophilic core of a lipoprotein-like emulsion particle. The lipophilic core is surrounded by a phospholipid membrane comprising cholesterol and apolipoproteins. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm as measured by number weighting analysis with a narrow size distribution (
摘要翻译： PCT No.PCT / US95 / 05974 371日期1996年11月15日 102（e）日期1996年11月15日PCT提交1995年5月16日PCT公布。公开号WO95 / 31181 日期1995年11月23日用作组织或细胞选择性递送载体的热稳定的水包油乳液。放射性或稳定的合成或半合成多卤甘油三酸酯，如2-油酰甘油-1,3-双[7-（3-氨基-2,4,6-三碘苯基）庚酸酯]或2-油酰甘油-1,3-二双（ω-（3,5-双 - 三氟甲基） - 庚酸酯]或乙酸苯酯可加入脂蛋白样乳液颗粒的亲脂性核心中。亲脂性核被包含胆固醇和载脂蛋白的磷脂膜包围。对于肝细胞选择性递送，通过具有窄尺寸分布的数量加权分析（<3％大于300nm）测量并具有自然模拟的组成，通过在50至200nm的尺寸范围内，乳液是乳糜微粒残留的发生乳糜微粒残留物。在乳液配方中使用胆固醇促进载脂蛋白，特别是由肝细胞识别并且是结合和摄取所必需的Apo E的缔合。稳定性和尺寸限制可以通过超高能量混合设备（例如MicroFluidizer（Microfluidics Corp.，Newton，Mass。））来实现，以形成乳液。在优选的实施方案中，乳液的重量摩尔渗透压浓度由甘油而不是生理盐水控制。

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