| 主权项 |
1. A compound of formula I or a pharmaceutical acceptable salt thereof, a hydrate thereof, or a solvate thereof: wherein: K is NH, O, S, SO, SO2, CH2, C═O or absent; A is aryl, heterocycloalkyl, cycloalkyl or heteroaryl; m is an integer of 0 to 4; X is O, S; R1 is hydrogen, halogen, —CN, —NO, —NO2, —NR9R10, —OR11, —CO2R12, —SR13, —COR14, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, wherein the groups of alkyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl are optionally substituted by R32; R32 is halogen, —CN, —CF3, —OH, —NH2, —SO2, —CO2H, alkyl unsubstituted or substituted by R33, heteroalkyl unsubstituted or substituted by R33, cycloalkyl unsubstituted or substituted by R33, heterocycloalkyl unsubstituted or substituted by R33, aryl unsubstituted or substituted by R33, heteroaryl unsubstituted or substituted by R33; R9, R10, R11, R12, R13 and R14 are each independently selected from hydrogen, alkyl unsubstituted or substituted by R34, heteroalkyl unsubstituted or substituted by R34, cycloalkyl unsubstituted or substituted by R34, heterocycloalkyl unsubstituted or substituted by R34, aryl unsubstituted or substituted by R34, heteroaryl unsubstituted or substituted by R34; R34 is selected from halogen, —CN, —CF3, —OH, —NH2, —SO2, —CO2H, alkyl unsubstituted or substituted by R35, heteroalkyl unsubstituted or substituted by R35, cycloalkyl unsubstituted or substituted by R35, heterocycloalkyl unsubstituted or substituted by R35, aryl unsubstituted or substituted by R35, heteroaryl unsubstituted or substituted by R35; R33 and R35 are each independently selected from halogen, —CN, —CF3, —OH, —NH2, —SO2, —CO2H, unsubstituted alkyl, unsubstituted heteroalkyl, unsubstituted cycloalkyl, unsubstituted heterocycloalkyl, unsubstituted aryl, or unsubstituted heteroaryl; R2 is hydrogen, amino, alkylamino, arylamino, heteroarylamino, thioalkyl, sulfoxide, sulfone, sulfamoyl, mercapto, halogen, alkoxy, alkanoyl, alkoxycarbonyl, C1-C6 alkyl, C2-C6 alkenyl, cycloalkyl, C2-C6 alkynyl, C5-C7 cycloalkenyl, aryl, heterocyclic aryl, heteroaryl, C1-C6 trifluoroalkyl, cyano, wherein each of the substituents is independently substituted by any of 0 to 3 groups selected from halogen, amino, hydroxy, mercapto, nitro or cyano; R3 is selected from the following substituents: (i) aryloxy, amino, —NH-alkyl, —N—(R9)(R10), —NH-aryl, —N-(aryl)2, —NHCOR9, —CO2H, —CO2-alkyl, —CO2-aryl, —CONH—R9, —CON—(R9)(R10), —CONH-alkyl, —CON-(alkyl)2, —SO3H, —SO2NH2, —CF3, —CO—R9 or —CO-aryl, wherein the groups of alkyl, aryl, aryl-substituted alkyl and heterocyclic group are each respectively further substituted by 0 to 3 groups which are selected from halogen, NO2, CN, OH, methoxy, NH2, CO2H, N—(R9)(R10), CONH2, CHF2 and CF3; (ii) hydrogen, halogen, —CN, —NO, —NO2, —SO2NHR9, —CF2H, —OR11, —SR13, —CH2CN, —CH2CH2OH, —NHCOCH3, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, wherein the groups of alkyl, aryl, heterocycloalkyl and heteroaryl are optionally substituted by 0 to 3 groups which are independently selected from halogen, NO2, CN, OH, methoxy, NH2, CO2H, N—(R9)(R10), R25, CONH2 and CF3; R25 is halogen, —CN, —CF3, —OH, —NH2, —SO2, —COOH, —NO, —SH, —NO2, oxo group, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R4 is hydrogen, alkyl, heteroalkyl, substituted alkyl, cycloalkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, or COR5; wherein the groups of cycloalkyl, aryl, heteroaryl, cycloalkyl-substituted alkyl, heterocycloalkyl, arylalkyl or heteroarylalkyl are independently of each other substituted by 0 to 3 groups which are selected from alkyl, halogen, CN, NO2, NH2, NHR5, N(R5)2, SR5, heteroalkyl, alkoxy, hydroxy, heteroalkoxy, CHF2, CF3, OCF3, OCF2H; R5 is alkyl, heteroalkyl, substituted alkyl, cycloalkyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, wherein the groups of cycloalkyl, aryl, heteroaryl, cycloalkyl-substituted alkyl, heterocycloalkyl, arylalkyl or heteroarylalkyl are independently of each other substituted by 1 to 3 groups which are selected from aryl, halogen, heteroalkyl, alkoxy, heteroalkoxy. |
