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US 6,855,689 B2Granted
Enzyme-activated anti-tumor prodrug compounds
AssigneeBoehringer Ingelheim Pharmaceuticals, Inc.
InventorsRaymond A. Firestone, Leila A. Telan
Life of this patent
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Abstract
Disclosed are enzyme-activated anti-tumor and anti-metastatic prodrug compounds. The specific enzymes are collagenase(IV) and elastase. Also disclosed are methods of making and using such compounds.
Claims6
A prodrug compound comprising:
- a targeting-peptide chosen from SEQ ID NO:6 or SEQ ID NO:7, wherein the targeting-peptide has L or L and D amino acid residues and wherein the targeting-peptide is optionally covalently capped by a terminal amino capping group Z;
- a linker group covalently attached to the targeting-peptide at the carboxy terminus;
- and
- a cytotoxic drug covalently attached to the linker;
- wherein:
- the targeting-peptide is an amino acid sequence which is catalytically cleaved by elastase;
- the linker group is a bond or a self-immolating linker;
- and
- Z is an amino protecting group chosen from tert-butyloxycarbonyl, benzyloxycarbonyl or an adhesion peptide;
- wherein there is an optional spacer molecule between Z and the targeting-peptide.
7 more elements
Dependencies are inferred from the claim text.