A compound having the following general formula: wherein A is -CHR 7 -, wherein R 7 is hydrogen, optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl, optionally substituted C 2-10 alkynyl, optionally substituted C 6-14 aryl-C 1-10 alkyl, optionally substituted 5-14 membered heteroaryl-C 1-10 alkyl, optionally substituted C 3-10 cycloalkyl-C 1-10 alkyl, optionally substituted 3-10 membered heterocycloalkyl-C 1-10 alkyl, optionally substituted C 6-14 aryl, optionally substituted 5-14 membered heteroaryl, optionally substituted C 3-10 cycloalkyl or optionally substituted 3-10 membered heterocycloalkyl; G is -NH-, -NR 6 -, -O-, or -C(R 6) 2 -, wherein R 6 is independently selected from optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl and optionally substituted C 2-10 alkynyl; R 1 is -Ra-R 10; wherein Ra is optionally substituted C 1-6 alkylene and R 10 is optionally substituted naphthyl or optionally substituted bicyclic fused heteroaryl; R 2 is -W 21 -W 22 -Rb-R 20, wherein W 21 is - - or -(SO 2)-; W 22 is bond, -O-, -NH- or optionally substituted C 1-6 alkylene; Rb is bond or optionally substituted C 1-6 alkylene; and R 20 is optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl, optionally substituted C 2-10 alkynyl, optionally substituted C 6-14 aryl, optionally substituted 5-14 membered heteroaryl, optionally substituted C 3-10 cycloalkyl or optionally substituted 3-10 membered heterocycloalkyl; R 3 is optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl or optionally substituted C 2-10 alkynyl; the "optionally substituted" means that a given radical may consist of only hydrogen substituents through available valencies or may further comprise one or more non-hydrogen substituents through available valencies, and the non-hydrogen substituents are selected from the group consisting of -R 8, -OH, -OR 8, -OC R 8, -OC OR 8, -COOH, -COOR 8, -CONH 2, -CONHR 8,-CONR 8 R 4, -NH 2, -NHR 8, -NR 8 R 4, -SH, -SR 8, -SO 2 R 8, -SO 2 NH 2, -SO 2 NHR 8, -SO 2 NR 8 R 4 -SO 3 H, -SOR 8, -NHC(NH 2)(=NH), -NHC(NHR 8)(=NR 4),-OP(=O) 2, -OP(=O)(ONa) 2, -OP(=0)(OR 8) 2, -OP(=O)(OR 8),-OP(=O) -O-P(=O) 2, -OP(=O)(ONa)-O-OP(=O)(ONa) 2, -CN, -NO 2 and halogen, wherein R 8 and R 4 are independently selected from linear or branched chain, cyclic or noncyclic C 1-10 alkyl chain, C 6-14 aryl and C 6-14 aryl-C 1-10 alkyl; the "heteroaryl" means a monocyclic or bicyclic aromatic radical wherein at least one ring atom is a heteroatom and the remaining ring atoms are carbon; the "cycloalkyl" means a non-aromatic, saturated or partially unsaturated, monocyclic, fused bicyclic or bridged polycyclic ring radical; the "heterocycloalkyl" means cycloalkyl provided that one or more of the atoms forming the ring are a heteroatom; the "heteroatom" is selected from the group consisting nitrogen, oxygen, and sulfur; and the "bicyclic fused" means a ring that is bonded to another ring to form a compound having a bicyclic structure when the ring atoms that are common to both rings are directly bound to each other; or a pharmaceutically acceptable salt thereof. A is -CHR 7 -, wherein R 7 is hydrogen, optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl, optionally substituted C 2-10 alkynyl, optionally substituted C 6-14 aryl-C 1-10 alkyl, optionally substituted 5-14 membered heteroaryl-C 1-10 alkyl, optionally substituted C 3-10 cycloalkyl-C 1-10 alkyl, optionally substituted 3-10 membered heterocycloalkyl-C 1-10 alkyl, optionally substituted C 6-14 aryl, optionally substituted 5-14 membered heteroaryl, optionally substituted C 3-10 cycloalkyl or optionally substituted 3-10 membered heterocycloalkyl; G is -NH-, -NR 6 -, -O-, or -C(R 6) 2 -, wherein R 6 is independently selected from optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl and optionally substituted C 2-10 alkynyl; R 1 is -Ra-R 10; wherein Ra is optionally substituted C 1-6 alkylene and R 10 is optionally substituted naphthyl or optionally substituted bicyclic fused heteroaryl; R 2 is -W 21 -W 22 -Rb-R 20, wherein W 21 is - - or -(SO 2)-; W 22 is bond, -O-, -NH- or optionally substituted C 1-6 alkylene; Rb is bond or optionally substituted C 1-6 alkylene; and R 20 is optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl, optionally substituted C 2-10 alkynyl, optionally substituted C 6-14 aryl, optionally substituted 5-14 membered heteroaryl, optionally substituted C 3-10 cycloalkyl or optionally substituted 3-10 membered heterocycloalkyl; R 3 is optionally substituted C 1-10 alkyl, optionally substituted C 2-10 alkenyl or optionally substituted C 2-10 alkynyl;