| 主权项 |
1. A compound of the formulawherein:
A is optionally substituted heteroaryl or optionally substituted heterocyclo, wherein the substituents are one or more R14, R15 or R16; R is hydrogen, optionally substituted (C1-C6)alkyl, optionally substituted (C3-C8)cycloalkyl(C1-C6)alkyl, optionally substituted aryl(C1-C6)alkyl, optionally substituted heteroaryl(C1-C6)alkyl, optionally substituted heterocyclo(C1-C6)alkyl, optionally substituted (C1-C6)alkyl-CO—, optionally substituted aryl-CO—, optionally substituted (C3-C8)cycloalkyl-CO—, optionally substituted heteroaryl, optionally substituted heterocyclo-CO—, optionally substituted aryl-SO2—, optionally substituted (C1-C6)alkyl-SO2—, optionally substituted (C3-C8)cycloalkyl-SO2—, optionally substituted heteroaryl-SO2—, optionally substituted (C1-C6)alkyl-OCO— or optionally substituted (C3-C8)cycloalkyl-OCO—; or R is wherein X and Y are independently selected from hydrogen, optionally substituted (C1-C6)alkyl, optionally substituted (C3-C8)cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclo; Z is hydrogen, halogen, —OH, (C1-C6)alkyl, (C1-C6)alkoxy, —NR3R4, —CONR3R4, —OCONR3R4, —NR6OCOR3, —NR6CONR3R4, —NR6SO2NR3R4 or —NR6SO2R4; R1 is halogen, —CN, OH, —NR3R4, —CONR3R4, —COOH, —OCONR3R4, —NHOCOR7, —NHCONR7R8, —NHSO2NR7R8, optionally substituted (C1-C6)alkyl, optionally substituted (C2-C6)alkenyl, optionally substituted (C2-C6)alkynyl, optionally substituted (C1-C6)alkoxy, optionally substituted (C3-C8)cycloalkyl, optionally substituted (C3-C8)cycloalkyl-CO—, optionally substituted (C3-C8)cycloalkyl-SO2—, optionally substituted aryl (C1-C6)alkoxy, optionally substituted (C3-C8)cycloalkyl (C1-C6)alkoxy, optionally substituted heterocyclyl-CO—, optionally substituted heterocyclyl, optionally substituted (C1-C6)alkyl-SO2—, —NHSO2-optionally substituted (C1-C6)alkyl, —NHSO2-optionally substituted heterocyclo, optionally substituted (C1-C6)alkyl-NHSO2— or optionally substituted heterocyclo-NHSO2—; R2 is H, halogen, —CN, —COOH, —CONR7R8, —NHCOR3R4, —OCONR3R4, —NHCOOR3R4, optionally substituted (C1-C6)alkyl, optionally substituted (C2-C6)alkynyl, optionally substituted (C1-C6)alkoxy, optionally substituted heteroaryl or optionally substituted heterocyclo; R3 is hydrogen, optionally substituted (C1-C6)alkyl, optionally substituted (C3-C8)cycloalkyl, optionally substituted (C2-C6)alkenyl, optionally substituted (C2-C6)alkynyl, cyano(C1-C6)alkyl, hydroxy(C1-C6)alkyl, optionally substituted aryl, optionally substituted aryl(C1-C6)alkyl, optionally substituted aryloxy(C1-C6)alkyl, optionally substituted (C1-C6)alkyl-SO2—, optionally substituted heterocyclyl, optionally substituted heterocyclyl(C1-C6)alkyl, optionally substituted heteroaryl or optionally substituted heteroaryl(C1-C6)alkyl, R4 is hydrogen, optionally substituted (C1-C6)alkyl or optionally substituted (C3-C8)cycloalkyl; or R3 and R4 may be taken together with the nitrogen atom to which they are attached to form an optionally substituted (C4-C8)heteroaryl or (C4-C8)heterocyclic ring; R6 is hydrogen or optionally substituted (C1-C6)alkyl; R7 and R8 are independently hydrogen, optionally substituted (C1-C6)alkyl, optionally substituted (C3-C8)cycloalkyl, optionally substituted (C2-C6)alkenyl, optionally substituted (C2-C6)alkynyl, cyano(C1-C6)alkyl, hydroxy(C1-C6)alkyl, optionally substituted aryl, optionally substituted aryl(C1-C6)alkyl, optionally substituted aryloxy(C1-C6)alkyl, optionally substituted (C1-C6)alkyl-SO2—, optionally substituted heterocyclyl, optionally substituted heterocyclyl(C1-C6)alkyl, optionally substituted heteroaryl or optionally substituted heteroaryl(C1-C6)alkyl; or R7 and R8 may be taken together with the nitrogen atom to which they are attached to form an optionally substituted (C4-C8)heteroaryl or (C4-C8)heterocyclic ring; R12 and R13 are independently hydrogen, halogen, —CN, OH, —CONR3R4, —NHCOOR4, —NHCONR3R4, —NHCOR4, —NHSO2R7, —SO2NR3R4, —NHSO2NR3R4, —SO2R7, optionally substituted (C1-C6)alkyl, optionally substituted (C3-C8)cycloalkyl, optionally substituted (C1-C6)alkoxy, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclo; R14 is hydrogen, optionally substituted(C1-C6)alkyl, (C1-C6)alkoxy, halogen, —CN, —NR3R4, OH, —NHOCOR7, —OCONR7R8, —NHCONR7R8 or —CF3; R15 is hydrogen, optionally substituted(C1-C6)alkyl, (C1-C6)alkoxy, halogen, —CN, —NR3R4, OH, —NHOCOR7, —OCONR7R8, —NHCONR7R8 or —CF3; R16 is hydrogen, optionally substituted(C1-C6)alkyl, (C1-C6)alkoxy, halogen, —CN, —NR3R4, OH, —NHOCOR7, —OCONR7R8, —NHCONR7R8 or —CF3; with the proviso that only one of R14, R15 and R16 is hydrogen; and/or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof. |
