Cyclic triamine chelating agents

Details Cyclic triamine chelating agents Cyclic triamine chelating agents

1994-04-13

1995-12-19

Nazario-Gonzalez, Porfirio

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

424 934, 424617, 424630, 424639, 424646, 424 9341, 424 935, 424 9361, 424 9364, 424 9365, 514492, 514499, 514501, 514502, 514505, 514579, 534 10, 534 16, 556 44, 556 50, 556 61, 556116, 556148, 556 1, 560125, 562507, 564152, 564153, 564191, 544259, 546 1, 546 2, 546104, 546134, 546255, 548240, 548446, 548469, 549211, 549212, 549388, 549398, A61K 4300, A61K 4900, A61K 3128

Patent

active

054766443

ABSTRACT:
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.8
R.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; 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.

REFERENCES:
patent: 4647447 (1987-03-01), Gries et al.
patent: 5021571 (1991-06-01), Mease et al.
patent: 5089663 (1992-02-01), Mease et al.
patent: 5124471 (1992-06-01), Gansow et al.
patent: 5344729 (1994-08-01), Mease et al.

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