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1. 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。

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