公开(公告)号：US5650133A

公开(公告)日：1997-07-22

申请号：US226760

申请日：1994-04-12

申请人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael David Koo

发明人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael David Koo

IPC分类号： A61K49/00 ,  A61K49/06 ,  C07D257/02 ,  C07D403/14 ,  C07F9/6524 ,  A61K51/04 ,  A61B5/055 ,  C07D225/00 ,  C07F5/00

CPC分类号： C07D403/14 ,  A61K49/0002 ,  A61K49/06 ,  C07D257/02 ,  C07F9/6524

摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.

摘要翻译： 本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是具有式Vb的化合物（其中每个可以相同或不同的X可以是NZ，O或S ，至少两个X为NZ;每个Z为基团R 1或基团CR 12 Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 12Y;每个Y为CO 2 H，PO 3 H，SO 3 H ，CONR12，CON（OR1）R1，CNS或CONR1NR12，优选COOH; m为0或1或2，优选1;每个n为2或3，优选2; q为1或2，优选1; 相同或不同的是氢原子或任选被一个或多个羟基和/或烷氧基取代的烷基; D是分子量小于1000，优选小于500的桥连基，连接两个大环 通过至少一个酰胺或酯键）及其盐和金属螯合物。