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US 12,673,918 B2Granted
Small molecule RPN13 inhibitors with antitumor properties
AssigneeThe Johns Hopkins University
InventorsRichard B.S. Roden, Ravi K. Anchoori
Life of this patent
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Abstract
Compounds of formula (I), (II), and (III) having the structure shown below are presented: wherein R-R6 are defined herein. These molecules work as proteasome inhibitors and bind to the RPN13 subunit of the 19S regulatory particle, and can be used in methods of treating a condition or a disease, such as cancer, in a mammal.
Claims18
A compound of formula (I):
- wherein
- R is H, C(O)CH2Cl, C(O)CH3, C(O)CH═CH2, or C(O)N(H) CH3;
- R1 at each occurrence is independently selected from NO2, halogen, and
- R2 is a side group from an alpha amino acid;
- R3 is C1-C6 alkyl, or phenyl, wherein C1-C6 alkyl is a saturated, linear or branched carbon chain having up to 6 carbons;
- and n at each occurrence is independently an integer from 0-5, inclusive;
- or a pharmaceutically acceptable salt, hydrate, or solvate thereof;
- wherein when R2 is the benzyl side group from phenylalanine and R3 is hydrogen, R is C (O)CH2Cl;
- and
- wherein the compound of formula (I) is not
7 more elements
Dependencies are inferred from the claim text.