公开(公告)号：US5993780A

公开(公告)日：1999-11-30

申请号：US826077

申请日：1997-03-24

申请人： Torsten Almen ,  Sven Goran Andersson ,  Lars-Goran Wistrand ,  Klaes Golman ,  .O slashed.yvind Antonsen ,  Rune Fossheim ,  Unni Nordby Wiggen ,  H.ang.kan Wikstrom ,  Tomas Klingstedt ,  Ib Leunbach ,  Arne Berg ,  Harald Dugstad

发明人： Torsten Almen ,  Sven Goran Andersson ,  Lars-Goran Wistrand ,  Klaes Golman ,  .O slashed.yvind Antonsen ,  Rune Fossheim ,  Unni Nordby Wiggen ,  H.ang.kan Wikstrom ,  Tomas Klingstedt ,  Ib Leunbach ,  Arne Berg ,  Harald Dugstad

IPC分类号： A61K49/04 ,  C07C33/46 ,  C07C33/48 ,  C07C43/295 ,  C07C49/83 ,  C07C69/02 ,  C07C69/12 ,  C07C233/43 ,  C07C235/16 ,  C07C237/46 ,  C07C275/42 ,  C07C307/10 ,  C07C311/29 ,  C07C317/22 ,  A61K49/00 ,  C07C233/00

CPC分类号： C07C33/46 ,  A61K49/0433 ,  C07C235/16 ,  C07C237/46 ,  C07C33/483

摘要： The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula I ##STR1## (wherein n is 0 or 1, and where n is 1 each C.sub.6 R.sub.5 moeity may be the same or different; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M.sub.1, two or three non-adjacent R groups in each C.sub.6 R.sub.5 moiety being iodine and at least one, and preferably two or three, R groups in each C.sub.6 R.sub.5 moiety being M or M.sub.1 moieties; X denotes a bond or a group providing a 1 to 7 atom chain linking two C.sub.6 R.sub.5 moieties or, where n is 0, X denotes a group R; each M independently is a non-ionic hydrophilic moiety; and each M.sub.1 independently represents a C.sub.1-4 alkyl 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 M.sub.1 moiety; with the proviso that where n is zero either at least one M.sub.1 group other than a hydroxymethyl or 1,2-dihydroxyethyl group is present or then if one hydroxymethyl or 1,2-dihydroxyethyl M.sub.1 group is present at least one nitrogen-attached or hydroxylated-C.sub.3-4 alkyl moiety-containing M group is also present) and isomers thereof.

摘要翻译： 本发明提供了可用作式I的X射线对比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的摩尔可以相同或不同;每个基团R为氢原子 ，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 表示提供连接两个C 6 R 5部分的1至7个原子链的键或基团，或其中n为0，X表示基团R;每个M独立地为非离子亲水部分;并且每个M 1独立地表示C 1-4烷基 至少一个被至少一个羟基取代并且任选地通过羰基，砜或亚砜基团与苯环连接的基团，至少一个R基团是M1部分;条件是其中n为0，或者至少一个除了 存在羟甲基或1,2-二羟乙基， 甲基或1,2-二羟乙基M1基团存在，还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）及其异构体。