Macrocyclic chelating agents and chelates thereof

US5132409A · kind A · utility

Assignee

• Bracco - Industria Chimica S.p.A. · IT

Inventors

• Ernst Felder · Lugano, CH
• Carlo Musu · Milano, IT
• Luciano Fumagalli · Milano, IT
• Fulvio Uggeri · Codogno, IT

Key dates

• Filing date: Nov 27, 1989
• Grant date: Jul 21, 1992
• Expiry date: Nov 27, 2009

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D257/02
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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##