| 主权项 |
1. A compound of formula I: wherein R1 is selected from —OH, —CN, —CHO , —OCH2CH3, —OCH(CH3)2, —NO2, —COR10, —COOR10, —SO2R10, —CONH2, —CSNH2, —CONR10NR11R12, —CONR10OR11, —CONR10((C(R12)(R13))tCONR10R11, —CONR10((C(R12)(R13))tCOOR11, —C(═S)R10, —C(═NOR11)R10, C(═NR10)R11, and —SO2NR10R11; R2 is selected from hydrogen, halogen, —OH, —CN, —CHO, OCH2CH3, —OCH(CH3)2, —NO2, —COR10, —COOR10, —SO2R10, —CONR10R11, —CSNR10R11, —CONR10NR11R12, —CONR10OR11, —CONR10 ((C(R12)(R13))tCONR10R11, —CONR10 ((C(R12)(R13))tCOOR11, —C(═S)R10, —C(═NOR11)R10, C(═NR10R11, —SO2NR10R11, heterocyclyl, optionally substituted lower alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, halo(C1-C6)alkyl, halo(C1-C6)alkoxy, and (C1-C6)alkylthio;or, R1 and R2 together with the atoms to which they are attached, and a fragment selected from —OCH2O—, or —OCH2CH2O—, form a ring,wherein when Cy is an aromatic group R1 and R2 cannot both be hydrogen;wherein when Cy is an aromatic group R1 and R2 cannot both be halogen;
R3 is chosen from C1-C8 hydrocarbon, heterocyclyl, aryl and hydroxyalkyl; R4 is chosen from hydrogen, hydroxyl, amino, lower alkoxy, C1-C20 alkyl and C1-C20 alkyl substituted with hydroxyl or carbonyl; R5 is lower alkyl; R6 is lower alkyl; R7 is chosen from hydrogen, NR10R11 and —OR10; or together R4, R5, R6 and R7 may form from one, two, three, or four rings, said rings having optional additional substitution; R8 and R8a are both hydrogen or taken together R8 and R8a are ═O; R9 is chosen from hydrogen and lower alkyl; R10, R11, R12 and R13 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, hydroxyl, —NR100R101 or optionally substituted lower alkoxy, or R10 and R11, together with the nitrogen atom to which they are attached, form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; t is 0, 1, 2, 3, 4, 5, or 6; R100 and R101 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, hydroxyl, or optionally substituted lower alkoxy, or R100 and R101, together with the nitrogen atom to which they are attached, form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; Y is a direct bond or —(C(R10)(R11))q—, wherein q is 0, 1, 2, 3, 4 or 5; L is a direct bond or —(C(R10)(R11))q—; and Cy is Ar1—B—Ar2, whereinAr1 is absent, or an aryl or heteroaryl radical having from 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by halogen, lower alkyl, alkenyl, alkynyl, cycloalkyl, —OR10, —NR10R11, —CN, —COR10 or —COOR10;
B is a direct bond, —O—, —NR10, —SO2, or —(C(R10)(R11)s—, wherein s is 0, 1, 2, 3, 4 or 5; andAr2 is aryl or heteroaryl radical having from 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by halogen, lower alkyl, alkenyl, alkynyl, cycloalkyl, —OR10, —NR10R11, —CN, —COR10 or —COOR10, wherein when Cy is phenyl or biphenyl, R1 is other than —OCH3. |
