Caspase inhibitor prodrugs
AssigneeVertex Pharmaceuticals Incorporated
InventorsMichael Mortimore, Julian M. C. Golec
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Abstract
The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.
Claims15
A compound of the formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is a saturated or unsaturated, straight-chain or branched, unsubstituted hydrocarbon chain;
- R2 is choline;
- X is a direct covalent bond;
- and
- Y is a residue of a caspase inhibitor selected from a structure in Table 1 below:
- TABLE 1
- Structures of Selected Caspase Inhibitors
- Comp.
- No.
- Structure
- 1
- 2
- 3
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12
- 13
- 14
- 15
- 16
- 17
- 18
- 19
- 20
Dependencies are inferred from the claim text.