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    • 4. 发明授权
    • Cyclic triamine chelating agents
    • 环状三胺螯合剂
    • US5476644A
    • 1995-12-19
    • US227161
    • 1994-04-13
    • Carl R. IlligThomas J. CaulfieldJohn L. TonerPeng GuoDavid L. Ladd
    • Carl R. IlligThomas J. CaulfieldJohn L. TonerPeng GuoDavid L. Ladd
    • A61K49/00A61K49/06C07C227/02C07C229/16C07C229/76C07C237/06C07C237/08C07C265/12C07C327/38C07C331/28C07F5/00C07F9/00C07F11/00C07F13/00C07F15/02C07F15/04C07F15/06C09K3/00A61K51/00A61K31/28
    • A61K49/06C07C229/16C07C2101/14
    • The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.20);n is 1 or 2;m is 1 to 15;X is a targeting moiety; andAr is phenyl optionally substituted with one, two or three substituents selected from the group consisting of amino, acylamino, hydroxy, alkyl (C1-C5) and halogen.
    • 本发明提供了与顺磁金属离子螯合的式“IMAGE”化合物,其中Z 1和Z 2各自表示完成单环或多环碳环或杂环系统所必需的原子,所述Z 1和Z 2独立地任选地被R6和R7取代, 分别; R1,R2,R3和R4独立地是羧基烷基(C1-C2), - (CH2)nC(= O)-NH-R8或 - (CH2)nC(= O)-O-R8 R5是羧基烷基 C2); R6和R7独立地是氢,苄基或苄氧基,所述苄基或苄氧基任选地被一个,两个或三个选自氨基,异氰酸酯基(-N = C = O),异硫氰酸酯(-N = C = S),-NH-C(= O)-X或-NH-C(= S)-X; R8是烷基(C1-C20), - (CH2)m-Ar或多羟基烷基(C1-C20); n为1或2; m为1〜15; X是靶向部分; 并且Ar是任选地被一个,两个或三个选自氨基,酰基氨基,羟基,烷基(C 1 -C 5)和卤素的取代基取代的苯基。