Complexes of functionalized tetraazacyclododecane chelates with bismuth, lead, ytriium, actinium, or lanthanide metal ions

US5428154A · kind A · utility

Assignee

• The United States of America, as represented by the Department of Health and Human Services · US

Inventors

• Otto A. Gansow · Washington, US
• Martin W. Brechbiel · Annandale, US
• Michael Magerstadt · Hofheim, DE

Key dates

• Filing date: Oct 22, 1993
• Grant date: Jun 27, 1995
• Expiry date: Oct 22, 2013

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K2123/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention is a chelate of formula I: ##STR1## wherein R.sub.1-4 is --CH.sub.2 COOH; PA0 n is 1 to 5; PA0 X is a member selected from the group consisting of PA1 --NO.sub.2, PA1 --NH.sub.2, PA1 --NCS, PA1 --NHCOCH.sub.2 --Z, with Z being a member selected from the group consisting of Br and I, PA1 --COOH; and PA1 --OCH.sub.2 OOCH; PA0 and M is a metal ion selected from the group of elements consisting of PA1 Bi, Pb, Y, Cd, Hg, Al, Th, Sr, and Lanthanides. The invention also includes a chelate, wherein M is a copper ion and n is an integer from 2 to 5. The invention includes chelate conjugates of formula I and ligand conjugates of formula II: ##STR2## The invention also includes methods to use these compounds for treatment of cellular disorders and for diagnostic tests.