Antibody drug-conjugates
AssigneeEli Lilly and Company
InventorsRussell L. Barton, Deborah L. Guttman-Carlisle, Gary A. Koppel
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Abstract
Immunoconjugates of antibodies or antigen-recognizing fragments of antibodies and monovalent cytotoxic drug derivatives make use of .beta.-alanine derived linkers wherein the antibody or fragment thereof is attached to the linker's carboxy group via an ester or amide group and the drug is attached through the linker's 2-position methylene group. Intermediates, compositions and methods of use also are provided.
Claims19
A compound of the formula ##STR25## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl;
- R.sup.4 is a carboxy protecting group;
- R.sup.5 is H .dbd.C(OH)2, .dbd.CHOR.sup.6, or .dbd.CHSR.sup.6 ;
- and
- R.sup.6 is C.sub.1 -C.sub.4 alkyl.
A compound of the formula ##STR26## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl;
- R.sup.2 is a monovalent drug derivative having a reactively-available amino, hydroxy or thiol function to which the .dbd.CH-- is attached;
- and
- R.sup.7 is H, a carboxy protecting group, or a carboxy activating group, or a moiety which completes a salt of the carboxy group.
The compound of clam 14 wherein R.sup.7 is H.
Dependencies are inferred from the claim text.