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US 5,514,794 AGranted
Antibody-drug conjugates
AssigneeEli Lilly and Company
InventorRussell L. Barton
Life of this patent
Estimating the term…
Abstract
Derivatized drugs are prepared with a linker consisting of a malonate, wherein the drug is linked through a methylene to the 2-position carbon of the malonate.
Claims4
A derivatized drug of the formula ##STR14## wherein R is a drug having a reactively-available amino, hydroxy, or thiol function;
- R.sup.1 is a carboxylic acid protecting group;
- Y is --O--, --NH--, --NCH.sub.3 --, or --NC.sub.2 H.sub.5 --;
- n is an integer from 1 to about 8;
- R.sup.3 is hydroxy,
- a carboxylic acid protecting group,
- a carboxylic acid activating group selected from the group consisting of benzenesulfonyloxy, methanesulfonyloxy, toluenesulfonyloxy, phthalimidyloxy, succinimidyloxy, chloro, benzotriazolyloxy, bromo, and azido or
- a moiety which completes a salt of the carboxylic acid;
- said carboxylic acid protecting groups being independently selected from the group consisting of methoxymethoxy, tetrahydropyranyloxy, tetrahydrofuranyloxy, benzyloxymethoxy, phenacyloxy, substituted phenacyloxy, 2,2,2-trichloroethoxy, haloethoxy, trimethylsilylethoxy, methylthioethoxy, toluenesulfonylethoxy, t-butoxy, cyclopentoxy, benzyloxy, diphenylmethoxy, triphenylmethoxy, amino, ethylamino, dimethylamino, pyrrolidino, morpholino, piperidino, diethylaminoethylamino, morpholinoethylamino, and benzylmethylaminoethylamino
5 more elements
Dependencies are inferred from the claim text.