A compound having the general formula (Ia): or a pharmaceutically acceptable salt thereof or a hydrate thereof, wherein A is O, S, CH, NH or NR', wherein, R' is C 1 -C 6 alkyl substituted or unsubstituted by halogen which includes 0∼3 heteroatom(s) of O, S or N; Ra, Rb, Rc, Rd, Re, Rf, Rg and Rh independently is H, OH, halogen or -Y 1 -R m, Y 1 is linking bond, O, S, SO, SO 2 or NR n; R m is hydrogen, or a substituted or unsubstituted substituent selected from the following group: (C 1 -C 8) alkyl, N≡ C-(C 1 -C 6) alkyl, (C 2 -C 8) alkenyl, (C 2 -C 8) alkynyl, (C 3 -C 7) cycloalkyl, (C 3 -C 7 cycloalkyl) (C 1 -C 6) alkyl, and 5∼6 membered aryl or heteroaryl including 0∼2 heteroatom(s) independently selected from N, O, S; R n is H, (C 1 -C 6) alkyl or (C 3 -C 6) cycloalkyl; A 1 is NH or CH 2; A 2 is N, O or linking bond; R 1 ' is a substituted or unsubstituted substituent selected from the following group: C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, aryl, (aryl) C 1 -C 2 alkyl, C 3 -C 7 cycloalkyl, (C 3 -C 7 cycloalkyl) C 1 -C 2 alkyl, C 3 -C 7 cycloalkenyl, (C 3 -C 7 cycloalkenyl) C 1 -C 2 alkyl, heterocycloalkyl, (heterocycloalkyl) C 1 -C 2 alkyl, C 5 -C 10 heteroaryl and (C 5 -C 10 heteroaryl) C 1 -C 2 alkyl; R 1 is hydrogen; or; R 1 linking covalently with R 3 together forms a C 5 -C 9 saturated or unsaturated hydrocarbon chain which can be inserted by 0∼2 heteroatom(s) independently selected from N, S and O, or which can be substituted by none or more halogen, O, S or -NR p R q, wherein, R p and R q independently is hydrogen or C 1 -C 6 alkyl; R 3 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, heterocycloalkyl, (C 3 -C 7 cycloalkyl) C 1 -C 4 alkyl, (C 3 -C 7 cycloalkenyl) C 1 -C 4 alkyl, (heterocycloalkyl) C 1 -C 4 alkyl, C 2 -C 6 alkylacyl, (C 1 -C 4 alkyl) 1-2 (C 3 -C 7) cycloalkyl or (C 1 -C 6 alkyl) 1-2 amino; and R 4 is substituted or unsubstituted C 1 -C 10 alkoxycarbonyl, (C 1 -C 10 alkyl)NHCO, (C 1 -C 10 alkyl) 2 NCO, aryl, heteroaryl or formyl substituted by 3∼7 membered cycloalkyl, heterocycloalkyl or cycloalkoxy. A is O, S, CH, NH or NR', wherein, R' is C 1 -C 6 alkyl substituted or unsubstituted by halogen which includes 0∼3 heteroatom(s) of O, S or N; Ra, Rb, Rc, Rd, Re, Rf, Rg and Rh independently is H, OH, halogen or -Y 1 -R m, Y 1 is linking bond, O, S, SO, SO 2 or NR n; R m is hydrogen, or a substituted or unsubstituted substituent selected from the following group: (C 1 -C 8) alkyl, N≡ C-(C 1 -C 6) alkyl, (C 2 -C 8) alkenyl, (C 2 -C 8) alkynyl, (C 3 -C 7) cycloalkyl, (C 3 -C 7 cycloalkyl) (C 1 -C 6) alkyl, and 5∼6 membered aryl or heteroaryl including 0∼2 heteroatom(s) independently selected from N, O, S; R n is H, (C 1 -C 6) alkyl or (C 3 -C 6) cycloalkyl; A 1 is NH or CH 2; A 2 is N, O or linking bond; R 1 ' is a substituted or unsubstituted substituent selected from the following group: C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, aryl, (aryl) C 1 -C 2 alkyl, C 3 -C 7 cycloalkyl, (C 3 -C 7 cycloalkyl) C 1 -C 2 alkyl, C 3 -C 7 cycloalkenyl, (C 3 -C 7 cycloalkenyl) C 1 -C 2 alkyl, heterocycloalkyl, (heterocycloalkyl) C 1 -C 2 alkyl, C 5 -C 10 heteroaryl and (C 5 -C 10 heteroaryl) C 1 -C 2 alkyl; R 1 is hydrogen; or; R 1 linking covalently with R 3 together forms a C 5 -C 9 saturated or unsaturated hydrocarbon chain which can be inserted by 0∼2 heteroatom(s) independently selected from N, S and O, or which can be substituted by none or more halogen, O, S or -NR p R q, wherein, R p and R q independently is hydrogen or C 1 -C 6 alkyl; R 3 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkenyl, heterocycloalkyl, (C 3 -C 7 cycloalkyl) C 1 -C 4 alkyl, (C 3 -C 7 cycloalkenyl) C 1 -C 4 alkyl, (heterocycloalkyl) C 1 -C 4 alkyl, C 2 -C 6 alkylacyl, (C 1 -C 4 alkyl) 1-2 (C 3 -C 7) cycloalkyl or (C 1 -C 6 alkyl) 1-2 amino; and R 4 is substituted or unsubstituted C 1 -C 10 alkoxycarbonyl, (C 1 -C 10 alkyl)NHCO, (C 1 -C 10 alkyl) 2 NCO, aryl, heteroaryl or formyl substituted by 3∼7 membered cycloalkyl, heterocycloalkyl or cycloalkoxy.