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US 5,010,176 AGranted
Antibody-drug conjugates
AssigneeEli Lilly and Company
InventorRussell L. Barton
Life of this patent
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Abstract
Modified antibodies or antigen-recognizing fragments are prepared with a linker consisting of a malonate, wherein the antibody or fragment thereof is attached through a carbonyl to an ester or amide group on one of the malonate carboxyls, and the drug is linked through a methylene to the 2-position carbon of the malonate.
Claims20
A modified antibody or antibody fragment of the formula ##STR14## wherein R.sup.1 is a carboxylic acid protecting group;
- R.sup.4 is C.sub.1 -C.sub.4 alkoxy;
- Y is --O--, --NH--, --NCH.sub.3 -- or --NC.sub.2 H.sub.5 --;
- n is an integer from 1 to about 8;
- m is an integer from 1 to about 10;
- and
- Ab is an antibody or antigen-recognizing fragment thereof, which recognizes an antigen associated with a cell to which delivery of the drug is desirable.
3 more elements
Dependencies are inferred from the claim text.