Cyclic triamine chelating agents
申请公布号:AU2261395(A)
申请号:AU19950022613
申请日期:1995.04.12
申请公布日期:1995.11.10
发明人:CARL ROOT ILLIG;THOMAS JOSEPH CAULFIELD;JOHN LUKE TONER;PENG GUO;DAVID LEE LADD
分类号:A61K49/00;A61K49/06;C07C227/02;C07C229/16;C07C229/76;C07C237/06;C07C237/08;C07C265/12;C07C327/38;C07C331/28;C07F5/00;C07F9/00;C07F11/00;C07F13/00;C07F15/02;C07F15/04;C07F15/06;C09K3/00
主分类号:A61K49/00
摘要:The present invention provides compounds of the formula <IMAGE> 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 R6 and R7, respectively; Rl, R2, R3 and R4 are independently carboxyalkyl (C1-C2), -(CH2)n-C(=O)-NH-R8, or -(CH2)n-C(=O)-O-R8 R5 is carboxyalkyl (C1-C2); R6 and R7 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=C=O), isothiocyanato (-N=C=S), -NH-C(=O)-X or -NH-C(=S)-X; R8 is alkyl (C1-C20), -(CH2)m-Ar, or polyhydroxyalkyl (C1-C20); n is 1 or 2; m is 1 to 15; X is a targeting moiety; and Ar is phenyl optionally substituted with one, two or three substituents selected from the group consisting of amino, acylamino, hydroxy, alkyl (C1-C5) and halogen.
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