| 主权项 |
1. A compound represented by the formula Ia or Ib, or a stereoisomer, tautomer, esterification or amidation prodrug or pharmaceutically acceptable salt thereof:wherein:
m=1, 2 or 3; n=1, 2 or 3; each dashed line “” is, independently, a single bond or double bond; when “ ” is a single bond, D and D1 are each, independently, selected from the group consisting of O, S, N(Ra), CH2, CH(OH), or C(Rb)(Rc); Ra is H, C1-C20 hydroxy, alkyl, C1-C20 cycloalkyl, C6-C20 aryl, C2-C20 heteroaryl, C1-C20 alkoxycarbonyl, C3-C20 cycloalkyloxycarbonyl, C6-C20 aryloxycarbonyl, C2-C20 heterocyclo-oxycarbonyl, C1-C20 alkylaminocarbonyl, C3-C20 cycloalkylamino-carbonyl, C1-C20 alkylamino sulfonamido, C2-C20 heterocyclo-aminosulfonyl, or C6-C20 arylaminosulfonyl; Rb and Rc are each, independently, selected from the group consisting of H, halogen, hydroxy, cyano, C1-C20 alkyl, C3-C20 cycloalkyl, C2-C20 heterocyclo, C6-C20 aryl, C1-C20 alkoxy, C1-C20 alkylthio, C1-C20 alkoxycarbonyl, C6-C20 aryloxy, C6-C20 heteroaryloxy, C6-C20 fused aryloxy, C6-C20 fused heterocyclo-oxy, C6-C20 aryloxycarbonyl, C2-C20 heterocyclo oxycarbonyl, C2-C20 heteroaryl, C1-C20 alkylamino, C2-C20 heterocycloamino, C6-C20 arylamino, C1-C20 alkylaminocarbonyl, C6-C20 alkylcarbonylamino, C1-C20 alkylsulfonamido, C2-C20 heterocyclosulfonamido, C6-C20 arylsulfonamido, and C1-C20 alkylaminosulfonamido; or Rb and Rc may be linked to form a C2-C20 cycloalkyl, C2-C20 cycloalkenyl, or C1-C20 cycloethereal group; when “” is a double bond, D and/or D1 are each, independently, selected from the group consisting of N, CH, and C(Rb), wherein the definition of Rb is the same as the Rb in D and D1 above; Ar, Ar1, Ar2 and Ar3 are each, independently, selected from the group consisting of C6-C20 aryl, C2-C20 heteroaryl, C8-C20 fused aryl, and C4-C20 fused heteroaryl, or Ar and Ar1 or Ar1 and Ar2 may be linked each other to form C10-C20 fused alkylaryl or C8-C20 aryl group, or Ar1 or Ar2 does not exist and the groups bonded to Ar1 or Ar2 are directly linked; E and G are each, independently, selected from the group consisting of N, CH and C(Rb); wherein the definition of Rb is the same as the Rb in D and D1 above; K is C2-C20 mono-heteroaryl, C2-C20 poly-heteroaryl, or C2-C20 fused-heteroaryl represented by one of the following structures: L and L1 are each, independently, linked with D and/or D1, selected from the group consisting of O, S, N(Ra), C(═O), C(═O)O, C(═S)O, and C(═O)N(Ra), wherein the definition of Ra is the same as the Ra in D and D1 above; or L and/or L1 are not present; Q and Q1 are each, independently, selected from the group consisting of C1-C20 alkyl, C1-C20 alkoxy, C1-C20 alkylamino, C3-C20 cycloalkylamino, C6-C20 aryl, C3-C20 heteroaryl, C3-C20 poly-heteroaryl, C3-C20 fused aryl, and C3-C20 heteroaryl group, wherein when L and/or L1 is not present, Q and/or Q1 is not present; W and W1 are each, independently, selected from the group consisting of carbonyl, thiocarbonyl, C1-C20 alkyl, C6-C20 aryl, and C2-C20 heteroaryl group; W2 and W3 are each, independently, selected from the group consisting of carbonyl, thiocarbonyl, sulfonyl, C1-C20 alkyl, C2-C20 heterocyclo, C6-C20 aryl, and C2-C20 heteroaryl group; Y and Y1 are each, independently, selected from the group consisting of H, C1-C20 alkyl, C3-C20 cycloalkyl, C6-C20 aryl, C1-C20 alkylcarbonyl, C6-C20 arylcarbonyl, C2-C20 heterocycloalkylcarbonyl, C1-C20 alkoxycarbonyl, C1-C20 cycloalkyl-oxy-carbonyl, C6-C20 aryloxycarbonyl, C2-C20 heteroaryloxycarbonyl, C1-C20 alkylaminocarbonyl, C1-C20 alkylsulfonyl, C3-C20 cycloalkylsulfonyl, C6-C20 arylsulfonyl, C1-C20 alkylamino sulfonyl, C3-C20 cycloalkylaminosulfonyl, and C6-C20 arylaminosulfonyl group; Z and Z1 are each, independently, selected from the group consisting of H, hydroxy, amino, C1-C20 alkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, C3-C20 cycloalkyl-oxy, C1-C20 alkylamino, C3-C20 cycloalkylamino, C2-C20 heterocyclo, C2-C20 heterocycloamino, C6-C20 aryl, C6-C20 aryloxy, C6-C20 arylamino, C3-C20 heteroaryloxy, C3-C20 heteroarylamino, C1-C20 alkylsulfonamido, C3-C20 cycloalkylsulfonamido, C6-C20 arylsulfonamido, C1-C20 alkoxysulfonamido, C3-C20 cycloalkyloxy-sulfonamido, C6-C20 aryloxysulfonamido, C1-C20 alkylaminosulfonamido, C3-C20 cycloalkylaminosulfonamido, and C6-C20 arylaminosulfonamido group; R1, R2, R3 and R4 are each, independently, selected from the group consisting of H, C1-C20 alkyl, C3-C20 cycloalkyl, C2-C20 heterocyclo, C6-C20 aryl, C2-C20 heteroaryl, C1-C20 alkoxycarbonyl, C6-C20 aryloxycarbonyl, C2-C20 heterocyclo-oxy carbonyl, C1-C20 alkylaminocarbonyl, C1-C20 alkylaminosulfonamido, C2-C20 heterocycloamino sulfonyl, and C6-C20 arylaminosulfonyl group; R5, R6, R7 and R8 are each, independently, selected from the group consisting of H, halogen, hydroxy, cyano, amino, C1-C20 alkyl, C3-C20 cycloalkyl, C2-C20 heterocyclo, C1-C20 alkoxy, C1-C20 alkylamino, C2-C20 heterocycloamino, C6-C20 aryl, C3-C20 heteroaryl, C6-C20 arylamino, C1-C20 alkoxycarbonylamino, C1-C20 alkylaminocarbonylamino, C1-C20 alkylsulfonamido, C2-C20 heterocyclosulfonamido, C6-C20 arylsulfonamido, and C1-C20 alkylaminosulfonamido, or R5 and R6 may be linked to each other to form a cyclo group, or R7 and R8 may be linked to each other to form a cyclo group; and R9, R10, R11 and R12 are each, independently, selected from the group consisting of H, halogen, hydroxy, cyano, amino, C1-C20 alkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, C1-C20 alkylamino, C2-C20 heterocycloamino, C6-C20 aryl, C3-C20 heteroaryl, C6-C20 arylamino, and C1-C20 alkoxycarbonylamino, or the R9 and R10 may be linked to each other to form a cyclo or spiro group, and the R11 and R12 may be linked to each other to form a cyclo or spiro group. |
