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US 2013/0259880 A1Published application
Amatoxin-Conjugates with Improved Linkers
AssigneeHeidelberg Pharma GmbH
InventorsJan Anderl, Werner Simon, Christoph Mueller
Life of this patent
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Abstract
The invention relates to tumour therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by a linker comprising a urea moiety, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.
Claims16
A conjugate comprising a target-binding moiety linked via a linker L to an amatoxin, wherein the linker L is connected to the amatoxin via
- (i) the γ C-atom of amatoxin amino acid 1, particularly via an amide linkage;
- (ii) an oxygen atom bound to the δ C-atom of amatoxin amino acid 3, particularly via an ester linkage, an ether linkage or a urethane linkage;
- or
- (iii) the 6′ C-atom of amatoxin amino acid 4, particularly via an oxygen atom bound to the 6′ C-atom of amatoxin amino acid 4;
- in each case wherein the linker L is connected to the target-binding moiety via a urea moiety.
2 more elements
An amatoxin-conjugation molecule comprising a linker L connected to an amatoxin via
- (i) the γ C-atom of amatoxin amino acid 1, particularly via an amide linkage;
- (ii) an oxygen atom bound to the δ C-atom of amatoxin amino acid 3, particularly via an ester linkage, an ether linkage or a urethane linkage;
- or
- (iii) the 6′ C-atom of amatoxin amino acid 4, particularly via an oxygen atom bound to the 6′ C-atom of amatoxin amino acid 4;
- in each case wherein the linker L comprises a carbamic acid derivative —NH—C(O)—X, wherein X is a leaving group that can be replaced by a primary amine of a target-binding moiety.
2 more elements
Dependencies are inferred from the claim text.