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US 5,824,805 AGranted
Branched hydrazone linkers
OwnerDalton King, Raymond A. Firestone +1inventors
InventorsDalton King, Raymond A. Firestone, Pamela Trail
Life of this patent
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Abstract
Branched hydrazone linkers for linking a targeting ligand such as an antibody to a therapeutically active drug. The point of branching is at a polyvalent atom and the number of drugs increases by a factor of two for each generation of branching. A preferred drug is doxorubicin.
Claims13
Having the formula ##STR44## wherein A is a thiol acceptor;
- Q is a bridging group;
- b is an integer of 0 or 1;
- W is a spacer moiety;
- m is an integer of 0 or 1;
- a is an integer of 2, 3 or 4;
- and
- X is a moiety of the formula --NH--NH.sub.2 or ##STR45## or a moiety of the formula ##STR46## wherein W, a, b and m are as defined hereinbefore, and
- X.sup.1 is a moiety of the formula --NH--NH.sub.2 or ##STR47## or a moiety of the formula ##STR48## wherein W, a, b, and m are defined hereinbefore, and
- X.sup.2 is a moiety of the formula NH--NH.sub.2 or ##STR49## or a moiety of the formula ##STR50## 10 wherein W, a, b, and m are as defined hereinbefore, and
- X.sup.3 is a moiety of the formula --NH--NH.sub.2 or ##STR51## or a moiety of the formula ##STR52## wherein W, a, b and m are as defined hereinbefore, and
- X.sup.4 is a moiety of the formula --NH--NH.sub.2 or ##STR53##
8 more elements
Dependencies are inferred from the claim text.