公开(公告)号：US5530140A

公开(公告)日：1996-06-25

申请号：US220522

申请日：1994-03-31

申请人： Sven Andersson ,  Finn Radner ,  Anna Rydbeek ,  Rolf Servin ,  Lars-Goran Wistrand

发明人： Sven Andersson ,  Finn Radner ,  Anna Rydbeek ,  Rolf Servin ,  Lars-Goran Wistrand

IPC分类号： A61K49/20 ,  C07B60/00 ,  C07D493/04 ,  C07D495/04 ,  C07D497/04 ,  C07D519/00 ,  A61K49/00

CPC分类号： C07D493/04 ,  A61K49/20 ,  C07B61/02 ,  C07D495/04 ,  C07D497/04

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 ##STR1## (wherein each X which may be the same or different is an oxygen or sulphur atom or a group CO or S(O).sub.n, (where n is 1 to 3) with the proviso that at least one group X is a sulphur atom or a S(O).sub.n group; R.sup.1 is a hydrogen atom or group of formula --M, --XM, --X--Ar.sup.2, or --Ar.sup.2 where M is a water solubilizing group, and Ar.sup.2 represents a 5-10 membered aromatic ring optionally substituted by a water solubilizing group M; and each of the groups R.sup.7, which may be the same or different, is a hydrogen atom, or a hydrocarbon group or a water solubilizing group M, or two groups R.sup.7 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 with the ring attachment carbon replaced by a silicon atom, and R.sup.7 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 solubilizing group M)). The novel radicals have good stability, long relaxation times and good relaxivity.

摘要翻译： 本发明提供了在Overhauser MRI中有用的新型持久性自由基，其具有作为至少一个芳基的基团为具有下式的基团的三芳基甲基（其中可以相同或不同的X是氧或硫原子或 基团CO或S（O）n，（其中n为1至3），条件是至少一个基团X为硫原子或S（O）n基团; R 1为氢原子或式-M ，-XM，-X-Ar2或-Ar2，其中M是水溶性基团，Ar2表示任选被水增溶基团M取代的5-10元芳香环;并且各基团R7可以是 相同或不同的是氢原子，或烃基或水溶性基团M，或两个R 7与它们所连接的原子一起代表羰基或5-8元环亚烷基，单 - 或二 - 单环或二氮杂环亚烷基或任选具有环连接c的单 - 或二 - 芳烃被硅原子取代，并且其中不是氢的R 7任选被羟基取代，任选烷氧基化，任选羟基化的酰氧基或烷基或水溶性基团M））。 新型自由基具有良好的稳定性，较长的松弛时间和良好的松弛性。