公开(公告)号：EP0832054B1

公开(公告)日：2000-12-27

申请号：EP95931302.4

申请日：1995-09-08

申请人： NYCOMED IMAGING AS

发明人： ANDERSSON, Sven ,  RYDBECK, Anna ,  SERVIN, Rolf ,  WISTRAND, Lars-Goran ,  RADNER, Finn

IPC分类号： C07B61/02 ,  C07D519/00 ,  A61K49/00

CPC分类号： A61K49/20 ,  C07B61/02 ,  C07D493/04 ,  C07D495/04 ,  C07D497/04 ,  C07D519/00 ,  C07F7/0814

公开(公告)号：EP0832054A1

公开(公告)日：1998-04-01

申请号：EP95931302.0

申请日：1995-09-08

申请人： NYCOMED IMAGING AS

发明人： ANDERSSON, Sven ,  RYDBECK, Anna ,  SERVIN, Rolf ,  WISTRAND, Lars-Goran ,  RADNER, Finn

IPC分类号： C07D493 ,  A61K31 ,  A61K49 ,  C07B60 ,  C07D495 ,  C07D497 ,  C07D519 ,  C07F7

CPC分类号： A61K49/20 ,  C07B61/02 ,  C07D493/04 ,  C07D495/04 ,  C07D497/04 ,  C07D519/00 ,  C07F7/0814

摘要： The invention provides novel persistent free radicals useful in Overhauser MRI being triarylmethyl radicals having as at least one aryl group a group of formula (1) or (2), wherein each X which may be the same or different is an oxygen or sulphur atom or a group CO or S(O)n (where n is 1 to 3) with the proviso that at least one group X is a sulphur atom or an S(O)n group; R1 is a hydrogen atom or group of formula -M, -XM, -X-Ar2 where M is a water solubilising group, and Ar2 represents a 5-10 membered aromatic ring optionally substituted by a water solubilising group M; and each of the groups R7, which may be the same or different, is a hydrogen atom, or a hydrocarbon group or a water solubilising group M, or two groups R7 together with the atom to which they are bound represent a carbonyl group or a 5 to 8 membered cycloalkylidene, mono- or di-oxacycloalkylidene, mono or di-azacycloalkylidene or mono- or di-thiacycloalkylidene group optionally wit the ring attachment carbon replaced by a silicon atom, and R7 where it is other than hydrogen, is optionally substituted by a hydroxyl group, an optionally alkoxylated, optionally hydroxylated acyloxy or alkyl group or a water solubilising group M. The novel radicals have good stability, long relaxation times and good relaxivity.

公开(公告)号：EP0782565B1

公开(公告)日：1999-04-07

申请号：EP95932108.4

申请日：1995-09-22

申请人： NYCOMED IMAGING AS

发明人： RYDBECK, Anna ,  ALMEN, Torsten ,  THANING, Mikkel ,  ANDERSSON, Sven ,  WISTRAND, Lars-Göran ,  GOLMAN, Klaes

IPC分类号： C07C275/42 ,  C07C237/46 ,  C07C235/16 ,  A61K49/04

CPC分类号： C07C237/46 ,  A61K49/0433 ,  C07C233/25 ,  C07C235/16 ,  C07C275/42

摘要： The invention provides iodinated bis phenyl compounds, useful as X-ray contrast agents, of formula (I) (wherein each C6R5 moiety may be the same or different; each R denotes a hydrogen or iodine atom or a group M, two or three non-adjacent R groups on each C6R5 moiety denoting iodine atoms and one, two or three R groups on each C6R5 moiety denoting M groups; X denotes a group providing a 1, 2 or 3 atom chain linking the two C6R5 groups, preferably where X is or contains in the bridging chain a carbonyloxy group each C6R5 group being a triodophenyl group or a group in which each R is other than hydrogen; and each M is independently a non-ionic hydrophilic moiety, M preferably being a non-ionic hydrophilic moiety comprising a monohydroxy- or polyhydroxy-alkyl group) and isomers, especially stereoisomers and rotamers, thereof.

公开(公告)号：EP0782565A1

公开(公告)日：1997-07-09

申请号：EP95932108.0

申请日：1995-09-22

申请人： NYCOMED IMAGING AS

发明人： RYDBECK, Anna ,  ALMEN, Torsten ,  THANING, Mikkel ,  ANDERSSON, Sven ,  WISTRAND, Lars-Göran ,  GOLMAN, Klaes

IPC分类号： A61K49 ,  C07C33 ,  C07C43 ,  C07C49 ,  C07C69 ,  C07C233 ,  C07C235 ,  C07C237 ,  C07C275 ,  C07C307 ,  C07C311 ,  C07C317

CPC分类号： C07C237/46 ,  A61K49/0433 ,  C07C233/25 ,  C07C235/16 ,  C07C275/42

摘要： The invention provides iodinated bis phenyl compounds, useful as X-ray contrast agents, of formula (I) (wherein each C6R5 moiety may be the same or different; each R denotes a hydrogen or iodine atom or a group M, two or three non-adjacent R groups on each C6R5 moiety denoting iodine atoms and one, two or three R groups on each C6R5 moiety denoting M groups; X denotes a group providing a 1, 2 or 3 atom chain linking the two C6R5 groups, preferably where X is or contains in the bridging chain a carbonyloxy group each C6R5 group being a triodophenyl group or a group in which each R is other than hydrogen; and each M is independently a non-ionic hydrophilic moiety, M preferably being a non-ionic hydrophilic moiety comprising a monohydroxy- or polyhydroxy-alkyl group) and isomers, especially stereoisomers and rotamers, thereof.

摘要翻译： 本发明提供了可用作式（I）的X射线造影剂的碘化双苯基化合物（其中每个C 6 R 5部分可以相同或不同;每个R表示氢或碘原子或M组，两个或三个非 在每个C 6 R 5部分上的相邻R基团表示碘原子和每个C 6 R 5部分上的一个，两个或三个R基团表示M基团; X表示提供连接两个C 6 R 5基团的1,2或3个原子链的基团，优选其中X是 或者在桥连链中含有羰氧基，每个C 6 R 5基团是三联苯基或其中每个R不是氢的基团;并且每个M独立地为非离子型亲水部分，M优选为非离子型亲水部分， 单羟基 - 或多羟基 - 烷基）和异构体，特别是其立体异构体和旋转异构体。