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US 2025/0367304 A1Published application
Fap-activated proteasome inhibitors for treating solid tumors
AssigneeTrustees of Tufts College
InventorsWilliam W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski
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Abstract
Disclosed are proteasome inhibitors, FAP-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
Claims21
1-122. (canceled)
A compound represented by the formula:
- A-B,
- or a pharmaceutically acceptable salt thereof, wherein:
- A is peptide comprising (D)-Ala-Pro, and optionally comprising an N-terminal blocking group;
- the peptide A is C-terminally linked to B;
- and
- B is bortezomib or a moiety comprising:
3 more elements
Dependencies are inferred from the claim text.