A compound, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, having Formula VIi: wherein: X-Y is selected from the group consisting of -N(R 1a)-C(=O)-; -C(=O)-O-; -C(=O)-N(R 1b)-; -CH 2 N(R 1c)-CH 2 -; -C(=O)N(R 1d)-CH 2 -; -CH 2 CH 2 -N(R 1e)-; -CH 2 N(R 1f)-C(=O)-; and -CH 2 O-CH 2 -; or X and Y do not form a chemical bond, and X is selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy; and Y is selected from the group consisting of cyano, hydroxy, and -CH 2 -R 12; R 1a is selected from the group consisting of hydrogen and alkyl; R 1b is selected from the group consisting of hydrogen, alkyl, and aralkyl; R 1c is selected from the group consisting of hydrogen, alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted heterocyclo, (cycloalkyl)alkyl, (heterocycloalkyl)alkyl, aralkyl, (heteroaryl)alkyl, alkylcarbonyl, arylcarbonyl, and alkoxycarbonyl; R 1d is selected from the group consisting of hydrogen, alkyl, and aralkyl; R 1e is selected from the group consisting of hydrogen, alkyl, and (aryloxy)alkyl; R 1f is selected from the group consisting of hydrogen and alkyl; R 2 is selected from the group consisting of hydrogen, alkyl, alkenyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocyclo, optionally substituted heteroaryl, and aralkyl; R 3a and R 3b are each independently selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy; R 12 is selected from the group consisting of hydroxy, amino, optionally substituted heteroaryl, optionally substituted heterocyclo, and -NHC(=O)-R 16; R 16 is selected from the group consisting of alkyl, optionally substituted aryl, optionally substituted heteroaryl, and optionally substituted cycloalkyl; R 17a is selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, haloalkylsulfonyl, cycloalkylsulfonyl, (cycloalkyl)alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, heterocyclosulfonyl, sulfonamido, optionally substituted heteroaryl, optionally substituted heterocyclo, carboxamido, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, carboxy, and carboxyalkyl; and R 17b and R 17c are independently selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy. X-Y is selected from the group consisting of -N(R 1a)-C(=O)-; -C(=O)-O-; -C(=O)-N(R 1b)-; -CH 2 N(R 1c)-CH 2 -; -C(=O)N(R 1d)-CH 2 -; -CH 2 CH 2 -N(R 1e)-; -CH 2 N(R 1f)-C(=O)-; and -CH 2 O-CH 2 -; or -N(R 1a)-C(=O)-; -C(=O)-O-; -C(=O)-N(R 1b)-; -CH 2 N(R 1c)-CH 2 -; -C(=O)N(R 1d)-CH 2 -; -CH 2 CH 2 -N(R 1e)-; -CH 2 N(R 1f)-C(=O)-; and -CH 2 O-CH 2 -; or X and Y do not form a chemical bond, and X is selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy; and Y is selected from the group consisting of cyano, hydroxy, and -CH 2 -R 12; R 1a is selected from the group consisting of hydrogen and alkyl; R 1b is selected from the group consisting of hydrogen, alkyl, and aralkyl; R 1c is selected from the group consisting of hydrogen, alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted heterocyclo, (cycloalkyl)alkyl, (heterocycloalkyl)alkyl, aralkyl, (heteroaryl)alkyl, alkylcarbonyl, arylcarbonyl, and alkoxycarbonyl; R 1d is selected from the group consisting of hydrogen, alkyl, and aralkyl; R 1e is selected from the group consisting of hydrogen, alkyl, and (aryloxy)alkyl; R 1f is selected from the group consisting of hydrogen and alkyl; R 2 is selected from the group consisting of hydrogen, alkyl, alkenyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heterocyclo, optionally substituted heteroaryl, and aralkyl; R 3a and R 3b are each independently selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy; R 12 is selected from the group consisting of hydroxy, amino, optionally substituted heteroaryl, optionally substituted heterocyclo, and -NHC(=O)-R 16; R 16 is selected from the group consisting of alkyl, optionally substituted aryl, optionally substituted heteroaryl, and optionally substituted cycloalkyl; R 17a is selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, haloalkylsulfonyl, cycloalkylsulfonyl, (cycloalkyl)alkylsulfonyl, arylsulfonyl, heteroarylsulfonyl, heterocyclosulfonyl, sulfonamido, optionally substituted heteroaryl, optionally substituted heterocyclo, carboxamido, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, carboxy, and carboxyalkyl; and R 17b and R 17c are independently selected from the group consisting of hydrogen, alkyl, halo, hydroxy, cyano, amino, alkylamino, dialkylamino, haloalkyl, alkoxy, and haloalkoxy.