Amino acid transport inhibitors and the uses thereof

A compound of Formula I:

• wherein:
• R is selected from the group consisting of hydrogen, C1-C4 alkyl, and aralkyl;
• E is selected from the group consisting of ═C(R5)—, ═C(R1a)—, and ═N—;
• E1 is selected from the group consisting of ═C(R5)—, ═C(R1a)—, and ═N—;
• with the proviso that one of E or E1 is ═C(R5)— and the other is ═C(R1a)— or ═N—;
• E2 is selected from the group consisting of ═C(R1b)— and ═N—;
• E3 is selected from the group consisting of ═C(R1c)— and ═N—;
• E4 is selected from the group consisting of ═C(R1d)— and ═N—;
• R1a, R1b, R1c, and R1d are each independently selected from the group consisting of hydrogen, halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, and C1-C4 alkoxy;
• R5 is selected from the group consisting of optionally substituted aryl and optionally substituted heteroaryl;
• Q is selected from the group consisting of:
• with the proviso that the bond designated with an “*” is attached to —C(═O)OR;
• G is selected from the group consisting of —S—, —O—, and —N(R2a)—;
• G1 is selected from the group consisting of ═C(R3a)— and ═N—;
• G2 is selected from the group consisting of ═C(R3b)— and ═N—;
• A is selected from the group consisting of ═C(R4a)— and ═N—;
• A1 is selected from the group consisting of ═C(R4b)— and ═N—;
• A2 is selected from the group consisting of ═C(R4c)— and ═N—;
• R2a is selected from the group consisting of hydrogen and C1-C4 alkyl;
• R3a and R3b are independently selected from the group consisting of hydrogen, hydroxy, halo, C1-C4 alkyl, and C1-C4 haloalkyl;
• and
• R4a, R4b, and R4c are each independently selected from the group consisting of hydrogen, halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, and C1-C4 alkoxy,
• or a pharmaceutically acceptable salt or solvate thereof,
• with the proviso that the compound is not:
• 5-([1,1′-biphenyl]-4-yl)-6-chloro-1H-pyrrolo[3,2-b]pyridine-2-carboxylic acid;
• 1-methyl-3-((4-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzyl)oxy)-1H-pyrazole-5-carboxylic acid;
• or
• 3-((4-(4-phenyl-1H-indol-1-yl)benzyl)oxy)isoxazole-5-carboxylic acid.