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公开(公告)号：US4883649A
公开(公告)日：1989-11-28
申请号：US257181
申请日：1988-10-13
IPC分类号： A61K51/04
CPC分类号： A61K51/0453 , A61K2123/00
摘要： Iodinated clonidine derivatives useful, inter alia, as a probe for identification and characterization of .alpha..sub.2 -adrenergic receptor sites and as tracers for imaging techniques such as positron emission tomography or computer assisted tomography. Binding competition studies have indicated that p-iodoclonidine, for example, is a particularly efficacious binder for .alpha..sub.2 -adrenergic sites.
摘要翻译： 碘化可乐定衍生物尤其用作用于鉴定和表征α2-肾上腺素能受体位点的探针，以及用于诸如正电子发射断层扫描或计算机辅助层析成像技术的成像技术的示踪剂。 结合竞争研究表明，例如，对碘碘喹啉是α2-肾上腺素能位点特别有效的粘合剂。
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公开(公告)号：US06255519B1
公开(公告)日：2001-07-03
申请号：US09319406
申请日：1999-09-20
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。
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公开(公告)号：US4873075A
公开(公告)日：1989-10-10
申请号：US774498
申请日：1985-09-10
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。
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4.发明授权
公开(公告)号：US4241088A
公开(公告)日：1980-12-23
申请号：US780880
申请日：1977-03-24
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。
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公开(公告)号：US07582279B2
公开(公告)日：2009-09-01
申请号：US10692311
申请日：2003-10-23
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。
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公开(公告)号：US6103216A
公开(公告)日：2000-08-15
申请号：US737429
申请日：1996-11-15
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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公开(公告)号：US5851510A
公开(公告)日：1998-12-22
申请号：US243596
申请日：1994-05-16
IPC分类号： A61K9/107 , A61K9/127 , A61K47/14 , A61K49/00 , A61K49/04 , A61K49/18 , A61K51/12 , B01J13/00
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： 可用作组织或细胞选择性递送载体的热和储存稳定的水包油乳液。 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]或乙酸苯酯可以掺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。 通过使用诸如MicroFluidizer（Microfluidics Corp.，Newton，Mass。）的超高能量混合设备可以实现稳定性和尺寸限制以形成乳液。 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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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：US06645463B1
公开(公告)日：2003-11-11
申请号：US09058715
申请日：1998-04-10
IPC分类号： A61K5100
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。
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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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