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US 6,214,345 B1Granted
Lysosomal enzyme-cleavable antitumor drug conjugates
AssigneeBristol-Myers Squibb Company
InventorsRaymond Armand Firestone, Gene Michael Dubowchik
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Abstract
The present invention relates to drug-ligand conjugates wherein the drug is linked to the ligand through a protein peptide linker and a connector, a process for the preparation of the conjugates, method of controlling the growth of undesirable cells, pharmaceutical compositions, and intermediates thereof.
Claims258
A compound of the Formula (I):
- in which
- L is a ligand, wherein L is capable of specifically targeting a selected cell population;
- A is a carboxylic acyl unit;
- Y is an amino acid;
- Z is an amino acid;
- X and W are each a self-immolative spacer;
- D is a drug moiety having pendant to the backbone thereof a chemically reactive functional group, said functional group selected from the group consisting of a primary or secondary amine, hydroxyl, sulflydryl, carboxyl, aldehyde and a ketone;
- n is an integer of 0 or 1, with the proviso that n cannot be the integer 0 for both Xn and Wn;
- and
- m is an integer of 1, 2, 3, 4, 5 or 6;
- and wherein Y and Z comprise a protein peptide sequence which is selectively enzymatically cleavable by tumor associated proteases.
8 more elements
Dependencies are inferred from the claim text.