Macrocyclic chelating agents and chelates thereof

Details Macrocyclic chelating agents and chelates thereof Macrocyclic chelating agents and chelates thereof

1989-11-27

1992-07-21

Stoll, Robert L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Radioactive metal containing

534 14, 534 15, 534 16, 540450, 540465, 540452, 540475, 424 11, 556 40, 556 44, 556 50, 556 56, 556 63, 556 77, 556116, 556125, 556134, 556136, 556141, 556148, 556 62, 556115, 556 55, 556133, C07F 500, A61K 4900

Patent

active

051324091

ABSTRACT:
Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. ##STR1##

REFERENCES:
patent: 4639365 (1987-01-01), Sherry
patent: 4885363 (1989-12-01), Tweedle et al.
patent: 4994560 (1991-02-01), Kruper, Jr. et al.
patent: 5006643 (1991-04-01), Fazio et al.
patent: 5049667 (1991-09-01), Schaefer et al.
Desreux et al., "Highly Stable Lanthanide Macrocyclic Complexes", Nucl. Med. Biol. vol. 15, pp. 9-15, 1988.

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