Prodrugs of CC-1065 analogs
AssigneeImmunoGen, Inc.
InventorsRobert Yongxin Zhao, Ravi V. J. Chari
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Abstract
Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
Claims5
A prodrug formed from a first subunit of formula (I) covalently linked to a second subunit of formula (V) via an amide bond from the secondary amino group of the pyrrole moiety of the first subunit to the C-2 carboxyl of the second subunit,
- wherein the formula (I) is as follows:
- wherein the Formula (V) is as follows:
- wherein R represents an amide-containing side chain that enables linkage of said prodrug to a cell binding agent;
- R1-R6 are each independently hydrogen, C1-C3 linear alkyl, methoxy, hydroxyl, primary amino, secondary amino, tertiary amino, or amido;
- and R7 is a phosphate group.
Dependencies are inferred from the claim text.