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US 2025/0064991 A1Published application
Compounds specific to granzyme b and uses thereof
AssigneeCytoSite Biopharma Inc.
InventorsGeoffrey Malcolm BILCER, Hui XIONG, Carey HORCHLER, Mark A. CASTANARES, Brian LIEBERMAN, Juntian ZHANG, Francisco A. VALENZUELA
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Abstract
Compounds capable of binding to granzyme B and comprising a radioactive moiety, for examples, compounds of Formula (I), and pharmaceutical compositions comprising such. Also provided herein are uses of the compounds and pharmaceutical composition in cancer treatment and/or imaging.
Claims31
A compound of formula (I):
- or a stereoisomer, tautomer, or a salt thereof,
- wherein:
- M is a radioactive moiety;
- A is a chelating moiety chelating the radioactive moiety;
- X is selected from the group consisting of —CH2C(NH)—, —CH2C(O)—, —CH2C(S)—, —NHC(NH)—, —NHC(O)—, —NHC(S)—, —OC(NH)—, —OC(O)—, and —OC(S)—, optionally wherein X is —CH2C(O)— or —NHC(S)—;
- Y is CH or N;
- Z is —CH2—, —CH2C(NH)—, —CH2C(O)—, —CH2C(S)—, —NHC(NH)—, —NHC(O)—, —NHC(S)—, —O(NH)—, —O—C(O)—, or —OC(S)—;
- optionally wherein Z is —CH2— or —CH2C(O)—;
- L is a peptide linker having 1-6 amino acid residues, inclusive;
- R1 is H or C1-6 alkyl, optionally wherein R1 is H or methyl;
- and
- R2 is C1-6 alkyl or C3-6 cycloalkyl.
9 more elements
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Dependencies are inferred from the claim text.