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US 12,427,124 B1Granted
Phenylalanine-based LAT1 inhibitors and uses thereof
AssigneeMaxymune Therapeutics, Inc.
InventorsBernd Jandeleit, Guangyao Gao, Wolf-Nicolas Fischer, Gordon Ringold
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Abstract
Phenylalanine-based inhibitors of the Large Amino Acid Transporter 1 (LAT1) are disclosed. The compounds are useful in modulating the transcellular transport of substrates of LAT1 such as large neutral amino acids. The compounds are useful in immunomodulation therapies.
Claims28
A compound having the structure of Formula (3):
- or a pharmaceutically acceptable salt thereof, wherein,
- R6 is selected from —COOH, —COORa, —CORa, and —CON(Rb)2, wherein,
- Ra is C1-4 alkyl;
- and
- each Rb is independently selected from hydrogen, —OH, C1-4 alkyl, and C1-4 alkoxy;
- R7 is selected from hydrogen and methyl;
- R8 is selected from hydrogen, halogen, C1-3 alkyl, and C1-3 alkoxy;
- R9 is selected from —S(O)2—NR— and —NR—S(O)2—, wherein R is selected from hydrogen and methyl;
- R10 is selected from C6-10 aryl, substituted C6-10 aryl, C5-6 cycloalkyl, and biphenyl;
- and
- each substituent is independently selected from halogen, phenyl, —N(—R)2, C1-4 alkoxy, and C1-4 alkyl, wherein each R is independently selected from hydrogen and methyl.
8 more elements
Dependencies are inferred from the claim text.