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    • 5. 发明申请
    • IODINATED X-RAY CONTRAST MEDIA
    • IODINATED X-RAY对比媒体
    • WO1996009282A1
    • 1996-03-28
    • PCT/GB1995002265
    • 1995-09-22
    • NYCOMED IMAGING A/SREED, Michael, AntonyALMÉN, TorstenANDERSSON, SvenWISTRAND, Lars-GöranGOLMAN, KlaesANTONSEN, OyvindFOSSHEIM, RuneWIGGEN, Unni, NordbyWIKSTRÖM, HåkanKLINGSTEDT, TomasLEUNBACH, IbBERG, ArneDUGSTAD, Harald
    • NYCOMED IMAGING A/SREED, Michael, Antony
    • C07C237/46
    • C07C33/46A61K49/0433C07C33/483C07C235/16C07C237/46
    • The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula (I), wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one, and preferably two or three, R groups in each C6R5 moiety being M or M1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M1 independently represents a C1-4alkyl group substituted by at least one hydroxyl group and optionally linked to the phenyl ring via a carbonyl, sulphone or sulphoxide group, at least one R group being an M1 moiety; with the proviso that where n is zero either at least one M1 group other than a hydroxymethyl or 1,2-dihydroxyethyl group is present or then if one hydroxymethyl or 1,2-dihydroxyethyl M1 group is present at least one nitrogen-attached or hydroxylated-C3-4 alkyl moiety-containing M group is also present and isomers thereof.
    • 本发明提供了可用作式(I)的X射线造影剂的低粘度碘化芳基化合物,其中n为0或1,并且其中n为1,每个C 6 R 5部分可以相同或不同; 每个基团R是氢原子,碘原子或亲水部分M或M1,每个C 6 R 5部分中两个或三个不相邻的R基团是碘,并且每个C 6 R 5部分中至少一个,优选两个或三个R基团 是M或M1部分; X表示键或提供连接两个C 6 R 5部分的1至7个原子链的基团,或其中n为0,X表示基团R; 每个M独立地是非离子亲水部分; 并且每个M1独立地表示被至少一个羟基取代的C 1-4烷基,并且任选地通过羰基,砜或亚砜基与苯环连接,至少一个R基团是M1部分; 条件是在n为0的情况下,至少一个除羟甲基或1,2-二羟乙基之外的M1基团存在或如果一个羟甲基或1,2 - 二羟乙基M1基团存在至少一个含氮连接或羟基化的含C3-4烷基部分的M基团以及其异构体。