Antibody conjugates with macrocyclic ligands
US5271927A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 18, 1993 |
| Grant date | Dec 21, 1993 |
| Priority date | — |
| Expiry date | Mar 18, 2013 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2123/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The conjugation of antibodies to a macrocyclic conjugate compound wherein the conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --((CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody. The conjugate compound provides for complexes of metals such as Tc, Co, Re, Cu, Au and Ag which are useful reagents for in vivo imaging and therapy.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.