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1. 发明公开

EP0029659A2 Vasopressin analogs, processes for their production and a method of treating mammals 失效
标题翻译：口服加压素，Verfahren zu ihrer Herstellung und BehandlungverfahrenfürSäugetiere。
公开(公告)号：EP0029659A2
公开(公告)日：1981-06-03
申请号：EP80303774.6
申请日：1980-10-24
申请人： Cort, Joseph H. , Fischman, Alan
发明人： Cort, Joseph H. , Fischman, Alan
IPC分类号： C07C103/52 , C07C149/40 , A61K37/02
CPC分类号： C07K7/16 , A61K38/00 , C07C323/59 , Y10S514/807 , Y10S930/15
摘要： Novel vasopressin analogs have the general schematic formula:
wherein X is selected from the group consisting of H and NH 2 and Y is selected from the group consisting of -S-S-, -CH 2 Sand -SCH 2 - and A = L when B = D and A = D when B = L. They can be administered to increase the level of Factor VIII and plasminogen activator in a subject's blood. The 1-desamino-1- and 1-desamino-6-monocarba [9-D-Ala-NH 2 ]-arginine-vasopressin analogs can be prepared by coupling a respective select group of amino acid residues in a predetermined sequence. Such a method includes the use of an amino acid residue which can be prepared by reacting beta-mercaptopropionic acid with 4-methylbenzyl bromine in the presence of triethylamine and a mutual solvent.
摘要翻译：具有以下通式的新型加压素类似物：其中X选自H和NH 2，Y选自-SS - ， - CH 2 S - 和-SCH 2 - 且A = L，当B = D，A = D，B = L时使用这些化合物的方法来增加受试者血液中因子VIII和纤溶酶原激活物的水平。

2. 发明公开

EP0029659A3 Vasopressin analogs, processes for their production and a method of treating mammals 失效
标题翻译： VASOPRESSIN模拟物，其生产方法和处理母体的方法
公开(公告)号：EP0029659A3
公开(公告)日：1981-08-26
申请号：EP80303774
申请日：1980-10-24
申请人： Cort, Joseph H. , Fischman, Alan
发明人： Cort, Joseph H.
IPC分类号： C07C103/52 , C07C149/40 , A61K37/02
CPC分类号： C07K7/16 , A61K38/00 , C07C323/59 , Y10S514/807 , Y10S930/15
摘要： Novel vasopressin analogs have the general schematic formula:
wherein X is selected from the group consisting of H and NH 2 and Y is selected from the group consisting of -S-S-, -CH 2 Sand -SCH 2 - and A = L when B = D and A = D when B = L. They can be administered to increase the level of Factor VIII and plasminogen activator in a subject's blood. The 1-desamino-1- and 1-desamino-6-monocarba [9-D-Ala-NH 2 ]-arginine-vasopressin analogs can be prepared by coupling a respective select group of amino acid residues in a predetermined sequence. Such a method includes the use of an amino acid residue which can be prepared by reacting beta-mercaptopropionic acid with 4-methylbenzyl bromine in the presence of triethylamine and a mutual solvent.
摘要翻译：具有以下通式的新型加压素类似物：其中X选自H和NH 2，Y选自-SS - ， - CH 2 S - 和-SCH 2 - 且A = L，当B = D，A = D，B = L时使用这些化合物的方法来增加受试者血液中因子VIII和纤溶酶原激活物的水平。

3. 发明申请

WO2005082425A1 CATALYTIC RADIOFLUORINATION 审中-公开
标题翻译：催化射线辐射
公开(公告)号：WO2005082425A1
公开(公告)日：2005-09-09
申请号：PCT/US2005/005837
申请日：2005-02-24
申请人： THE GENERAL HOSPITAL CORPORATION , ELMALEH, David , SHOUP, Timothy, M. , FISCHMAN, Alan, J.
发明人： ELMALEH, David , SHOUP, Timothy, M. , FISCHMAN, Alan, J.
IPC分类号： A61K51/00
CPC分类号： A61K51/04 , A61B6/507 , A61B6/508 , C07B59/00 , C07B2200/05 , C07D241/04
摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium sait. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
摘要翻译：本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。在优选的实施方案中，使用氟化钾-18。本发明的另一方面涉及可用作成像剂的含有氟-18的哌嗪化合物。在某些实施方案中，哌嗪化合物含有季胺。本发明的另一方面涉及可用作成像剂的含有氟-18的芳基鏻化合物。在某些实施方案中，鏻化合物是四芳基鏻盐。本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

4. 发明申请

WO2005032598A1 POLYBIOTIN COMPOUNDS FOR MAGNETIC RESONANCE IMAGINING AND DRUG DELIVERY 审中-公开
标题翻译：用于磁共振成像和药物递送的聚异氰酸酯化合物
公开(公告)号：WO2005032598A1
公开(公告)日：2005-04-14
申请号：PCT/US2004/032153
申请日：2004-10-01
申请人： THE GENERAL HOSPITAL CORPORATION , ELMALEH, David, R. , SHOUP, Timothy, M. , FISCHMAN, Alan, J.
发明人： ELMALEH, David, R. , SHOUP, Timothy, M. , FISCHMAN, Alan, J.
IPC分类号： A61K51/00
CPC分类号： C07D519/00 , A61B5/0059 , A61B5/055 , A61B5/412 , A61B5/4839 , A61K47/557 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/124 , A61K51/0446 , A61K51/0497 , G01R33/5601
摘要： The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.
摘要翻译：本发明一般涉及可用作成像剂和药物递送剂的含生物素的化合物。本发明的另一方面涉及上述与金属原子螯合的化合物。在优选的实施方案中，金属原子是钆。本发明的另一方面涉及包含三个生物素部分和共价结合到杂环核心的药剂的化合物。在某些实施方案中，药剂是抗生素，抗病毒剂或放射性核素。本发明的另一方面涉及一种治疗涉及将哺乳动物施用本发明化合物的疾病的方法。本发明的另一方面涉及使用本发明化合物获得磁共振图像的方法。

5. 发明申请

WO2004093650A3 METHOD FOR MONITORING BLOOD FLOW AND METABOLIC UPTAKE IN TISSUE WITH RADIOLABELED ALKANOIC ACID 审中-公开
标题翻译：用无菌醇酸监测组织中血液流和代谢摄取的方法
公开(公告)号：WO2004093650A3
公开(公告)日：2005-04-14
申请号：PCT/US2004012084
申请日：2004-04-19
申请人： GEN HOSPITAL CORP , ELMALEH DAVID R , FISCHMAN ALAN J , SHOUP TIMOTHY M
发明人： ELMALEH DAVID R , FISCHMAN ALAN J , SHOUP TIMOTHY M
IPC分类号： A61B20060101 , A61K31/19 , A61K31/20 , A61K51/00 , B65D71/00 , C07C61/04 , C07C63/33 , C07F5/00
CPC分类号： A61K51/0402
摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.
摘要翻译：本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换为2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

6. 发明申请

WO2008134618A3 NOVEL IMAGING TRACERS FOR EARLY DETECTION AND TREATMENT OF AMYLOID PLAQUES CAUSED BY ALZHEIMER'S DISEASE AND RELATED DISORDERS 审中-公开
公开(公告)号：WO2008134618A3
公开(公告)日：2008-11-06
申请号：PCT/US2008/061742
申请日：2008-04-28
申请人： THE GENERAL HOSPITAL CORPORATION , ELMALEH, David, R. , SHOUP, Timothy , FISCHMAN, Alan, J.
发明人： ELMALEH, David, R. , SHOUP, Timothy , FISCHMAN, Alan, J.
IPC分类号： A61K51/00 , A61K31/44 , A61K49/00 , A61K31/426 , A61B5/055
摘要： The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4'-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.

7. 发明申请

WO2003003975A3 DETECTION AND THERAPY OF VULNERABLE PLAQUE WITH PHOTODYNAMIC COMPOUNDS 审中-公开
公开(公告)号：WO2003003975A3
公开(公告)日：2003-01-16
申请号：PCT/US2002/018472
申请日：2002-06-04
申请人： THE GENERAL HOSPITAL CORPORATION , HAMBLIN, Michael, R. , TAWAKOL, Ahmed , HASAN, Tayyaba , FISCHMAN, Alan , MULLER, James , ANDERSON, Rox
发明人： HAMBLIN, Michael, R. , TAWAKOL, Ahmed , HASAN, Tayyaba , FISCHMAN, Alan , MULLER, James , ANDERSON, Rox
IPC分类号： A61K38/16
摘要： The present invention relates to methods for selectively targeting Photodynamic Therapy ("PDT") to inflammatory components of vulnerable plaques. As such, the present invention provides methods for the identification of vulnerable plaques, as well as methods to treat vulnerable plaques by selectively targeting and/or eliminating the inflammatory components of vulnerable plaques. The invention further relates to a specially designed intravascular device that delivers excitation light to the plaque surface inside the artery and receives emitted fluorescence light when a fluorescent signal is detected.

8. 发明申请

WO2003003975A2 DETECTION AND THERAPY OF VULNERABLE PLAQUE WITH PHOTODYNAMIC COMPOUNDS 审中-公开
标题翻译：具有光化学活性的易碎液的检测与治疗
公开(公告)号：WO2003003975A2
公开(公告)日：2003-01-16
申请号：PCT/US2002/018472
申请日：2002-06-04
申请人： THE GENERAL HOSPITAL CORPORATION , HAMBLIN, Michael, R. , TAWAKOL, Ahmed , HASSAN, Tayaba , FISCHMAN, Alan , MULLER, James , ANDERSON, Rox
发明人： HAMBLIN, Michael, R. , TAWAKOL, Ahmed , HASSAN, Tayaba , FISCHMAN, Alan , MULLER, James , ANDERSON, Rox
IPC分类号： A61K
CPC分类号： A61B18/245 , A61B5/0071 , A61B5/0075 , A61B5/0084 , A61B5/0086 , A61B6/4258 , A61B18/20 , A61B2017/00057 , A61B2017/00079 , A61B2018/00904 , A61K41/0057 , A61K41/0061 , A61K41/0071 , A61K41/0076 , A61K47/643 , A61K51/0474 , A61K51/0491 , A61N5/0601 , A61N5/062 , A61N2005/0602
摘要： The present invention relates to methods for selectively targeting Photodynamic Therapy ("PDT") to inflammatory components of vulnerable plaques. As such, the present invention provides methods for the identification of vulnerable plaques, as well as methods to treat vulnerable plaques by selectively targeting and/or eliminating the inflammatory components of vulnerable plaques. The invention further relates to a specially designed intravascular device that delivers excitation light to the plaque surface inside the artery and receives emitted fluorescence light when a fluorescent signal is detected.
摘要翻译：本发明涉及将光动力疗法（“PDT”）选择性地靶向易受伤害斑块的炎性成分的方法。因此，本发明提供了用于鉴定易受伤害的斑块的方法，以及通过选择性靶向和/或消除脆弱斑块的炎症组分来治疗易感斑块的方法。本发明还涉及一种特别设计的血管内装置，其将激发光传递到动脉内的斑块表面，并在检测到荧光信号时接收发射的荧光。

9. 发明申请

WO2008134618A2 NOVEL IMAGING TRACERS FOR EARLY DETECTION AND TREATMENT OF AMYLOID PLAQUES CAUSED BY ALZHEIMER'S DISEASE AND RELATED DISORDERS 审中-公开
标题翻译：用于早期检测和治疗由阿尔茨海默病和相关疾病引起的淀粉样蛋白的新型成像追踪器
公开(公告)号：WO2008134618A2
公开(公告)日：2008-11-06
申请号：PCT/US2008061742
申请日：2008-04-28
申请人： GEN HOSPITAL CORP , ELMALEH DAVID R , SHOUP TIMOTHY , FISCHMAN ALAN J
发明人： ELMALEH DAVID R , SHOUP TIMOTHY , FISCHMAN ALAN J
IPC分类号： A61K51/00 , A61B5/055 , A61K31/426 , A61K31/44 , A61K49/00
CPC分类号： C07D277/66 , A61K51/0446 , A61K51/0453
摘要： The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4'-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.
摘要翻译：本发明涉及用于成像和治疗阿尔茨海默病或淀粉样变性相关病理状况的化合物和方法，其利用新型淀粉样蛋白成像示踪剂来检测患有这些病症的受试者中的淀粉样蛋白沉积物。在某些实施方案中，本发明涉及[N-2 [18F]氟丙基] -2-（4' - （甲基氨基） - 苯基）-6-羟基苯并噻唑（F-18MHT）及其二聚体。

10. 发明申请

WO2008022319A3 CATALYTIC RADIOFLUORINATION 审中-公开
标题翻译：催化放射性
公开(公告)号：WO2008022319A3
公开(公告)日：2008-07-24
申请号：PCT/US2007076219
申请日：2007-08-17
申请人： GEN HOSPITAL CORP , ELMALEH DAVID R , FISCHMAN ALAN J , SHOUP TIMOTHY M
发明人： ELMALEH DAVID R , FISCHMAN ALAN J , SHOUP TIMOTHY M
IPC分类号： C07C209/74 , A61K51/04 , C07C211/64 , C07C381/12 , G21G4/08
CPC分类号： A61K51/04 , A61B6/507 , A61K9/0021 , A61K49/0433 , A61K51/00 , A61K51/0459 , A61K51/0489 , C07B2200/05 , C07C209/74 , C07C211/64 , C07C381/12 , C07D241/04 , C07D295/073 , C07F9/5442
摘要： One aspect of the present invention relates to a method of preparing radio fluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
摘要翻译：本发明的一个方面涉及制备放射性氟化取代的烷基，环烷基，芳基和烯基化合物的方法。在一个优选的实施方案中，使用氟化钾-18。本发明的另一方面涉及可用作显像剂的含有氟-18的芳基铵化合物。在某些实施方案中，铵化合物是四芳基铵盐。本发明的另一方面涉及可用作显像剂的含有氟-18的芳基锍化合物。在某些实施方案中，锍化合物是三芳基锍盐。本发明的另一方面涉及一种获得哺乳动物的正电子发射图像的方法，该方法包括以下步骤：将本发明的化合物给予哺乳动物，并获得哺乳动物的正电子发射光谱。

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