R⁰ is arylalkyl, wherein said aryl is unsubstituted or optionally independently substituted with one or more substituents, which can be the same or different and are independently selected from Q⁰;

R¹ is hydrogen, alkyl, aryl, alkylaryl, arylalkyl, alkylheteroaryl, alkoxy, alkoxyalkyl, alkoxyoxo, amino, aminoalkyl, alkylamino, alkylheterocyclyl, carboxy, cyanoalkyl, cycloalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, hydroxyalkyl, oxo, —CO₂R⁵, —C(O)N(R⁵)₂, or —C═(NOR⁵), where each of said R⁵ is independently hydrogen, alkyl, aryl, heteroaryl, heteroarylalkyl, alkylheteroaryl, alkoxyalkyl, aminoalkyl, cyanoalkyl, oxo, cycloalkyl, heterocyclyl, heterocyclylalkyl, alkylheterocyclyl, or alkylamino; further wherein each of said alkyl, aryl, heteroaryl, cycloalkyl and heterocyclyl is unsubstituted or optionally independently substituted with one or more substituents, which can be the same or different and are independently selected from Q¹;

R² is hydrogen, akyl, aryl, alkylaryl, arylalkyl, carboxy, alkoxyoxo, alkylsulfonamido, heterocyclyl, heteroaryl, heteroarylalkyl, —CO₂R⁶, —N(R⁶)SO₂R⁶, —C(O)NHSO₂R⁶, —SO₂R⁶, —C(O)N(R⁶)₂, or —C(O)NHC(R⁶)C(O)R⁶; where each of said R⁶ is independently hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl alkylheteroaryl, alkoxyalkyl, aminoalkyl, cyanoalkyl, alkyloxo, cycloalkyl, heterocyclyl, heterocyclylalkyl, hydroxy, hydroxyalkyl, alkylheterocyclyl, or alkylamino; further wherein each of said alkyl, aryl, heteroaryl, and cycloalkyl and heterocyclyl is unsubstituted or optionally independently substituted with one or more substituents, which can be the same or different and are independently selected from Q²;

R³ is aryl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, or heteroaryl, further wherein each of said aryl, and heteroaryl, is unsubstituted or optionally independently substituted with one or more substituents, which can be the same or different and are independently selected from Q³;

Q⁰ is alkyl, hydroxy, amino, halo, alkoxy, alkylamino, dialkylamino, aminoalkyl, hydroxyalkyl, haloalkyl, arylalkyl, heteroarylalkyl, aryl, haloaryl, alkylaryl, aryloxy, heteroaryl, haloheteroaryl, alkylheteroaryl, hydroxyheteroaryl, heteroaryloxy, heterocyclyl, heterocyclyloxy, alkylamido, oxo, alkylsulfonamido, alkyloxo, alkoxyoxo, nitro, cyano, haloalkoxy, —C(O)NH, —NHC(O), —S(O)₂NH, or —NHS(O)₂;

Q¹ is hydrogen, alkyl, hydroxy, amino, halo, alkoxy, alkylamino, dialkylamino, aminoalkyl, hydroxyalkyl, haloalkyl, arylalkyl, heteroarylalkyl, aryl, haloaryl. alkylaryl, aryloxy, cycloalkyl, heteroaryl, haloheteroaryl, alkylheteroaryl, hydroxyheteroaryl, heteroaryloxy, heterocyclyl, heterocyclyloxy, alkylamido oxo, alkylsulfonamido, alkyloxo, alkoxyoxo, nitro, cyano, haloalkoxy-C(O)NH, —NHC(O), —S(O)₂NH, or —NHS(O)₂;

Q² is hydrogen, alkyl, alkyloxo, alkylsulfonyl, aryl, arylsulfonyl, hydroxy, hydroxyalkyl, amino, halo, alkoxy, alkoxyoxo, alkylamino, dialkylamino, aminoalkyl, hydroxyalkyl, haloalkyl, arylalkyl, heteroarylalkyl, heteroarylsulfonyl, haloaryl, hydroxysulfonyl, alkylaryl, aryloxy cycloalkyl, heteroaryl, haloheteroaryl, alkylheteroaryl, hydroxyheteroaryl, heteroaryloxy, heterocyclyl, heterocyclyloxy, alkylamido, oxo, alkylsulfonamido, alkyloxo, alkoxyoxo, nitro, cyano, haloalkoxy, —C(O)NH, —NHC(O), —S(O)₂NH, or —NHS(O)₂; and

Q³ is hydrogen, alkyl, alkylamido, alkyloxo, alkylsulfonyl, alkoxyoxo, alkylaryl, alkylheteroaryl, amino, aryloxy, aryl, arylsulfonyl, alkylsulfonamido, halo, alkoxy, alkoxyoxo, alkylamino, aminoakyl, arylalkyl, cycloalkyl, cyano, dialkylamino, dialkylaminoalkyl, hydroxyalkyl, haloalkyl, haloalkoxy, haloaryl, heteroarylalkyl, heteroarylsulfonyl, hydroxy, hydroxyalkyl, hydroxysulfonyl, heteroaryl, haloheteroaryl, hydroxyheteroaryl, hydroxyheterocyclyl, heteroaryloxy, heterocyclyl, heterocyclyloxy, oxo, nitro, —C(O)NH, —NHC(O), —S(O)₂NH, or —NHS(O)₂.