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1. 发明申请

WO1993015768A1 USE OF FULLERENES IN DIAGNOSTIC AND/OR THERAPEUTIC AGENTS 审中-公开
标题翻译：在诊断和/或治疗药物中使用富勒烯
公开(公告)号：WO1993015768A1
公开(公告)日：1993-08-19
申请号：PCT/GB1993000279
申请日：1993-02-11
申请人： NYCOMED SALUTAR, INC. , WATSON, Alan, D. , KLAVENESS, Jo , JAMIESON, Gene, C. , FELLMANN, Jere, Douglas , VOGT, Nils, Blane , COCKBAIN, Julian, R., M.
发明人： NYCOMED SALUTAR, INC.
IPC分类号： A61K49/00
CPC分类号： A61K51/1268 , A61K41/0057 , A61K41/0095 , A61K49/0084 , A61K49/0438 , A61K49/085 , A61K49/189 , A61K49/228 , A61K2123/00 , B82Y5/00 , Y10S977/927
摘要： Compounds comprising tight molecular meshes, preferably curved in one or two directions, such as fullerenes and met-cars, may be used as carriers for diagnostic or therapeutic agents, especially diagnostic imaging contrast agents.
摘要翻译：包括紧密分子网格的化合物，优选在一个或两个方向上弯曲，例如富勒烯和met-car，可用作诊断或治疗剂，特别是诊断成像造影剂的载体。

2. 发明申请

WO1995024225A1 POLYCHELANTS 审中-公开
公开(公告)号：WO1995024225A1
公开(公告)日：1995-09-14
申请号：PCT/GB1995000464
申请日：1995-03-03
申请人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson , MARGERUM, Lawrence , CARVALHO, Joan , GARRITY, Martha , FELLMANN, Jere, Douglas
发明人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson
IPC分类号： A61K51/00
CPC分类号： A61K49/124 , A61K49/085 , A61K49/12 , A61K51/065 , C07D259/00 , C08G83/00 , Y10S424/16
摘要： The invention provides polychelant compounds which are useful for example in diagnostic imaging procedures and which are degradable in vivo to release excretable fragments. Such compounds conveniently are of the formula (I): R (X R ((X )pL)n)m (where X is a linker moiety metabolically cleavable to release R X m and X R ((X )pL)n fragments where X and X are the cleavage residues of X ; R X m is a biotolerable polymer, preferably a substantially monodisperse polymer and especially one with a molecular weight below 40,000D, particularly below 30,000D and especially below 20,000D, for example a first to sixth generation dendrimer; X R ((X )pL)n is a polychelant fragment having a molecular weight below 40,000D, preferably below 30,000D, especially below 20,000D, each such moiety preferably being the same; p is 0 or 1; X , where present, is a linker moiety metabolically cleavable to release a monochelant fragment; each L is a macrocyclic chelant moiety, wherein the macrocyclic skeleton preferably has 9 to 25 ring members and preferably is an optionally oxygen or sulphur interrupted polyazacycloalkane; R ((X )p)n is a straight chain or branched backbone moiety, preferably providing a chain of up to 20 atoms between each L group and the X moiety to which it is joined and a chain of up to 25 atoms between each pair of L groups linked thereby, such chains conveniently being nitrogen and/or oxygen and/or sulphur interrupted carbon chains; each n is an integer having a value of at least 2, preferably a value of 2 to 25, especially 2 to 12; and each m is an integer having a value of at least 2, preferably a value of up to 200, especially 3 to 100, such that the total number of L groups in the polychelant of formula (I) is at least 20, preferably 50 to 200), having a molecular weight of at least 30,000D, preferably at least 40,000D, and especially preferably 50,000 to 150,000D, and metal chelates and salts thereof.
摘要翻译：本发明提供了可用于例如诊断成像程序并且可在体内降解以释放排泄性片段的聚合物化合物。这样的化合物通常是式（I）：R 1（X 1 R 2）（X 2）p L）n）m（其中X 1是代谢可裂解释放的连接体部分 R 1 X 3 m和X 4 R 2（（X 2）pL）n个片段，其中X 3和X 4是X 1的裂解残基; R X 3是生物可耐受聚合物，优选基本上单分散的聚合物，特别是分子量低于40,000D，特别是低于30,000D，特别是低于20,000D的聚合物，例如第一至第六代树枝状聚合物; X < R 2（（X 2）p L）n是分子量低于40,000D，优选低于30,000D，特别是低于20,000D的聚合物片段，每个这样的部分优选相同; p是0或 1; X 2（其中存在）是可代谢裂解以释放单核桃片段的接头部分;每个L是大环螯合剂部分，其中大环骨架优选具有9至25个环成员，优选为任选的氧或硫中断多氮杂环烷烃; R 2（（X 2））p为n 直链或支链骨架部分，优选在每个L基团与其所连接的X 1部分之间提供至多20个原子的链，以及由此连接的每对L组之间至多25个原子的链，链方便地是氮和/或氧和/或硫中断的碳链; 每个n是具有至少2，优选2至25，特别是2至12的值的整数; 并且每个m是具有至少2，优选至多200，特别是3至100的值的整数，使得式（I）的聚合物中的L基团的总数为至少20，优选为50 至200），分子量为至少30,000D，优选至少40,000D，特别优选50,000至150,000D，以及金属螯合物及其盐。

3. 发明申请

WO1993008846A1 CONTRAST MEDIA 审中-公开
标题翻译：对比媒体
公开(公告)号：WO1993008846A1
公开(公告)日：1993-05-13
申请号：PCT/EP1992002550
申请日：1992-10-29
申请人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED SALUTAR, INC. , FELLMANN, Jere, Douglas
发明人： COCKBAIN, Julian, Roderick, Michaelson , NYCOMED SALUTAR, INC.
IPC分类号： A61K49/00
CPC分类号： A61K49/1893 , A61K51/1258 , A61K2123/00
摘要： There are provided improved diagnostic metal containing molecular sieves for use as contrast agents in diagnostic imaging techniques such as X-ray, scintigraphy and, especially, MRI. For MRI the diagnostic metals are paramagnetic metal ions. Reduced risk of toxic metal release in vivo, especially into the GI tract, is achieved by surface modification of the molecular sieve.
摘要翻译：提供了改进的含有分子筛的诊断金属，用作诊断成像技术如X射线，闪烁照相术，特别是MRI中的造影剂。对于MRI，诊断金属是顺磁金属离子。通过分子筛的表面改性，降低体内有毒金属释放特别是胃肠道的风险。

4. 发明申请

WO1995028967A1 CONTRAST AGENTS 审中-公开
标题翻译：对比剂
公开(公告)号：WO1995028967A1
公开(公告)日：1995-11-02
申请号：PCT/GB1995000899
申请日：1995-04-20
申请人： NYCOMED IMAGING AS , COCKBAIN, Julian , MARGERUM, Larry , CAMPION, Brian , FELLMANN, Jere, Douglas , GARRITY, Martha , VARADARAJAN, John
发明人： NYCOMED IMAGING AS , COCKBAIN, Julian
IPC分类号： A61K49/00
CPC分类号： A61K49/124 , A61K47/60 , A61K49/085 , A61K49/106 , A61K49/1812 , A61K51/065 , A61K2121/00 , A61K2123/00 , C08G79/00
摘要： The invention provides a blood pool contrast agent having an overall molecular weight of at least 10KD comprising a macrostructure which has bound thereto a plurality of opsonization inhibiting moieties and carries chelated ionic paramagnetic or heavy metal moieties, the chelant groups for said chelated moieties being macrocyclic where said macrostructure is liposomal.
摘要翻译：本发明提供了总体分子量至少为10KD的血液池造影剂，其包含宏观结构，其结合有多个调理作用抑制部分并携带螯合的离子顺磁性或重金属部分，所述螯合部分的螯合剂基团是大环的，其中所述宏观结构是脂质体。

5. 发明申请

WO1995009848A2 POLYAZACYCLOALKANES AS DICHELANTS 审中-公开
标题翻译：聚四环素作为狄更斯
公开(公告)号：WO1995009848A2
公开(公告)日：1995-04-13
申请号：PCT/GB1994002115
申请日：1994-09-29
申请人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson , CARVALHO, Joan , FELLMANN, Jere, Douglas , WATSON, Alan, David , KOO, Michael
发明人： NYCOMED SALUTAR, INC. , COCKBAIN, Julian, Roderick, Michaelson
IPC分类号： C07D257/02
CPC分类号： C07D295/15 , A61K49/122 , C07D257/02 , C07D273/08 , C07D403/14 , C07F9/6524
摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula (V) (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ; each Z is a group R or a group CR 2Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 2, preferably COOH; m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1; each R which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups; and D is a bridging group, other than an unsubstituted carbonylaminoethylaminocarbonyl group, having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.
摘要翻译：本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是具有式（Ⅴ）化合物（其中每个X可以相同或不同的是NZ，O或S，至少两个X为NZ;每个Z为基团R 1或基团CR 1 2Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 2Y; 每个Y是CO 2 H，PO 3 H，SO 3 H，CONR 2，CON（OR 1）R 1，CNS或CONR 1 NR 1，优选COOH; m是0或1或 2，优选1;每个n为2或3，优选2; q为1或2，优选1;每个R 1可以相同或不同，是氢原子或任选被一个或多个羟基和/或烷氧基; D是分子量小于1000，优选小于500的未取代的羰基氨基乙基氨基羰基以外的桥连基，通过至少一个酰胺键或酯键连接两个大环）和盐和金属螯合物。

6. 发明申请

WO9628420A3 PREPARATION OF N-ARYLMETHYL AZIRIDINE DERIVATIVES,PREPARATION OF N-ARYLMETHYL AZIRIDINE DERIVATIVES, 1,4,7,10-TETRAAZACYCLODODECANE DERIVATIVES OBTAIN 1,4,7,10-TETRAAZACYCLODODECANE DERIVATIVES OBTAINED THEREFROM AND N-ARYLMETHYL-ETHANOL-AMINE SULPHOED THEREFROM AND N-ARYLMETHYL-ETHANOL-AMINE SULPHONATE ESTERS AS INTERMEDIATES NATE ESTERS AS INTERMEDIATES 审中-公开
标题翻译：制备N-甲基甲基咪唑衍生物，制备N-芳基甲基咪唑衍生物，1,4,7,10-四氮杂十二烷基衍生物，得到由其获得的1,4,7,10-四氮杂环十二烷基衍生物和由其形成的N-芳基甲基 - 乙醇胺作为中间体的N-亚磺酰基 - 乙醇 - 氨基磺酸盐作为中间体
公开(公告)号：WO9628420A3
公开(公告)日：1996-12-12
申请号：PCT/GB9600552
申请日：1996-03-08
申请人： NYCOMED SALUTAR INC , UNIV IOWA RES FOUND , COCKBAIN JULIAN , MESSERLE LOUIS , AMARASINGHE GANDARA , FELLMANN JERE DOUGLAS , GARRITY MARTHA , VARADARAJAN JOHN , VASILEVSKIS JANIS
发明人： MESSERLE LOUIS , AMARASINGHE GANDARA , FELLMANN JERE DOUGLAS , GARRITY MARTHA , VARADARAJAN JOHN , VASILEVSKIS JANIS
IPC分类号： A61K49/00 , A61K49/06 , C07C303/44 , C07C305/06 , C07D203/08 , C07D255/00 , C07D257/02 , C07D259/00 , C07C305/04
CPC分类号： C07D203/08 , A61K49/0002 , A61K49/06 , C07C303/44 , C07D255/00 , C07D257/02 , C07D259/00 , C07C305/06
摘要： Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I), (where each R1 independently is hydrogen or a group Ar and Ar is an optionally substituted phenyl group), said process comprising reacting a purified N-arylmethylethanolamine-sulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula: R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect the invention provides compounds of formula (II), where Ar and R1 are as hereinbefore defined and at least two differing ArCHR1 moieties are present.
摘要翻译：氮杂环丁烷可以被喷射到环烯化反应中以产生用于例如制备用于诊断成像造影剂的螯合剂的多氮杂环烷烃化合物。特别是N-苄基 - 氮丙啶是有用的，因为它可以进行环化聚合和脱苄基化，以产生螯合剂，螯合剂制备中的关键中间体。本发明提供了生产式（I）的N-苄基和其它N-芳基甲基氮丙啶的特别有吸引力的途径，其中每个R 1独立地为氢或基团AR，Ar为任选取代的苯基。该方法包括使纯化的N-芳基甲基乙醇胺 - 磺酸酯磺酸酯与碱反应。作为中间体，式R'NHCH2CH2OSO3H的N-芳基甲基 - 乙醇胺磺酸酯，其中N-芳基甲基R'是N-（二芳基甲基）或N-（三芳基甲基）基团。在另一方面，本发明提供式（II）的化合物，其中Ar和R 1如上所定义，并且存在至少两个不同的ArCHR 21部分。

7. 发明申请

WO1996028420A2 PREPARATION OF N-ARYLMETHYL AZIRIDINE DERIVATIVES, 1,4,7,10-TETRAAZACYCLODODECANE DERIVATIVES OBTAINED THEREFROM AND N-ARYLMETHYL-ETHANOL-AMINE SULPHONATE ESTERS AS INTERMEDIATES 审中-公开
标题翻译： N-芳基甲基咪唑衍生物的制备，其中获得的1,4,7,10-四氮杂环十二烷基衍生物和作为中间体的N-亚磺酰基 - 乙磺酰胺磺酸盐
公开(公告)号：WO1996028420A2
公开(公告)日：1996-09-19
申请号：PCT/GB1996000552
申请日：1996-03-08
申请人： NYCOMED SALUTAR, INC. , UNIVERSITY OF IOWA RESEARCH FOUNDATION , COCKBAIN, Julian , MESSERLE, Louis , AMARASINGHE, Gandara , FELLMANN, Jere, Douglas , GARRITY, Martha , VARADARAJAN, John , VASILEVSKIS, Janis
发明人： NYCOMED SALUTAR, INC. , UNIVERSITY OF IOWA RESEARCH FOUNDATION , COCKBAIN, Julian
IPC分类号： C07D203/08
CPC分类号： C07D203/08 , A61K49/0002 , A61K49/06 , C07C303/44 , C07D255/00 , C07D257/02 , C07D259/00 , C07C305/06
摘要： Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I), (where each R1 independently is hydrogen or a group Ar and Ar is an optionally substituted phenyl group), said process comprising reacting a purified N-arylmethylethanolamine-sulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula: R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect the invention provides compounds of formula (II), where Ar and R1 are as hereinbefore defined and at least two differing ArCHR1 moieties are present.
摘要翻译：氮丙啶可以进行环烯基化反应以产生用于例如制备用于诊断成像造影剂的螯合剂的多氮杂环烷烃化合物。特别是N-苄基 - 氮丙啶是有用的，因为它可以进行环化聚合和脱苄基化，以产生螯合剂，螯合剂制备中的关键中间体。本发明提供了生产式（I）的N-苄基和其它N-芳基甲基氮丙啶的特别有吸引力的途径（其中每个R 1独立地为氢或基团Ar，Ar为任选取代的苯基），所述方法包括使纯化的N-芳基甲基乙醇胺 - 磺酸酯与碱。具有下式的N-芳基甲基 - 乙醇胺磺酸酯：R'NHCH2CH2OSO3H，其中N-芳基甲基R'为N-（二芳基甲基）或N-（三芳基甲基）基团，为中间体。在另一方面，本发明提供式（II）化合物，其中Ar和R 1如上所定义，并且存在至少两个不同的ArCHR 1部分。

8. 发明申请

WO9509848A3 POLYAZACYCLOALKANES AS DICHELANTS 审中-公开
标题翻译：聚四环素作为狄更斯
公开(公告)号：WO9509848A3
公开(公告)日：1995-07-27
申请号：PCT/GB9402115
申请日：1994-09-29
申请人： NYCOMED SALUTAR INC , COCKBAIN JULIAN R M , CARVALHO JOAN , FELLMANN JERE DOUGLAS , WATSON ALAN DAVID , KOO MICHAEL
发明人： CARVALHO JOAN , FELLMANN JERE DOUGLAS , WATSON ALAN DAVID , KOO MICHAEL
IPC分类号： G01R33/28 , A61B5/055 , A61K31/395 , A61K31/495 , A61K49/00 , A61K49/06 , A61K51/00 , A61N5/00 , A61P39/00 , A61P39/02 , A61P43/00 , C07D255/02 , C07D257/02 , C07D273/00 , C07D285/00 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07F5/00 , C07F9/547 , C07F9/6524 , C07H23/00 , C09K3/00
CPC分类号： C07D295/15 , A61K49/122 , C07D257/02 , C07D273/08 , C07D403/14 , C07F9/6524
摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula (V) (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ; each Z is a group R or a group CR 2Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR 2Y; each Y is a group CO2H, PO3H, SO3H, CONR 2, CON(OR )R , CNS or CONR NR 2, preferably COOH; m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1; each R which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups; and D is a bridging group, other than an unsubstituted carbonylaminoethylaminocarbonyl group, having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.

9. 发明申请

WO1995001165A1 MEDICAL USE OF ORGANIC AEROGELS AND BIODEGRADABLE ORGANIC AEROGELS 审中-公开
标题翻译：有机天然气和生物可降解有机天然气的医疗使用
公开(公告)号：WO1995001165A1
公开(公告)日：1995-01-12
申请号：PCT/GB1994001421
申请日：1994-06-30
申请人： HOLMES, Michael, John , NYCOMED IMAGING A/S , BERG, Arne , DROEGE, Michael, William , FELLMANN, Jere, Douglas , KLAVENESS, Jo , RONGVED, Pål
发明人： HOLMES, Michael, John , NYCOMED IMAGING A/S
IPC分类号： A61K09/16
CPC分类号： A61L27/56 , A61K9/1641 , A61K9/1694 , A61K49/00 , A61L27/18 , A61L27/50 , A61L27/52 , A61L27/58 , C08L61/12
摘要： Physiologically acceptable organic aerogels, including pyrolysed aerogels, for use in medicine, for example as diagnostic agents, artificial tissues, organs and organ components etc., and in particular in drug delivery systems. Use of biodegradable organic aerogels, which are themselves novel materials, is preferred e.g. for materials such as diagnostic and therapeutic agents for parenteral administration.
摘要翻译：生理上可接受的有机气凝胶，包括用于医药的热解气凝胶，例如诊断剂，人造组织，器官和器官成分等，特别是在药物递送系统中。使用本身是新颖材料的可生物降解的有机气凝胶是优选的。用于肠胃外给药的诊断和治疗剂等材料。

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