| 主权项 |
1. A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein R1 is isopropenyl or isopropyl; X is selected from the group of C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, wherein X is substituted with A, and wherein A is —C1-6 alkyl-halo; Y is selected from the group of —COOR2, —C(O)NR2SO2R3, —C(O)NHSO2NR2R2, —NR2SO2R2, —SO2NR2R2, —C3-6 cycloalkyl-COOR2, —C2-6 alkenyl-COOR2, —C2-6 alkynyl-COOR2, —C1-6 alkyl-COOR2, -alkylsubstituted C1-6 alkyl, —CF2—COOR2, —NHC(O)(CH2)n—COOR2, —SO2NR2C(O)R2, -tetrazole, and —CONHOH, wherein n=1-6; R2 is —H, —C1-6 alkyl, -alkylsubstituted C1-6 alkyl or -arylsubstituted C1-6 alkyl; W is absent, or is —CH2 or —CO; R3 is —H, —C1-6 alkyl or -alkylsubstituted C1-6 alkyl; R4 is selected from the group of —H, —C1-6 alkyl, —C1-6alkyl-C3-6cycloalkyl, —C1-6 substituted —C1-6 alkyl, —C1-6 alkyl-Q1, —C1-6 alkyl-C3-6 cycloalkyl-Q1, aryl, heteroaryl, substituted heteroaryl, —COR6, —SO2R7, —SO2NR2R2, and wherein G is selected from the group of −O—, —SO2— and —NR12; wherein Q1 is selected from the group of —C1-6 alkyl, —C1-6 fluoroalkyl, heteroaryl, substituted heteroaryl, halogen, —CF3, —OR2, —COOR2, —NR8R9, —CONR8R9 and —SO2R7; R5 is selected from the group of —H, —C1-6 alkyl, —C3-6 cycloalkyl, —C1-6 alkylsubstituted alkyl, —C1-6alkyl-NR8R9, —COR3, —SO2R7 and —SO2NR2R2; with the proviso that R4 or R5 cannot be —COR6 when W is —CO; with the further proviso that only one of R4 or R5 can be selected from the group of —COR6, —COCOR6, —SO2R7 and —SO2NR2R2; or when W is absent or is —CH2, then R4 and R5 can be taken together with the adjacent N to form R6 is selected from the group of —H, —C1-6 alkyl, —C1-6 alkyl-substituted alkyl, —C3-6 cycloalkyl, —C3-6 substituted cycloalkyl-Q2, —C1-6 alkyl-Q2, —C1-6 alkyl-substituted alkyl-Q2, —C3-6 cycloalkyl-Q2, aryl-Q2, —NR13R14, and —OR15; wherein Q2 is selected from the group of aryl, heteroaryl, substituted heteroaryl, —OR2, —COOR2, —NR8R9, SO2R7, —CONHSO2R3, and —CONHSO2NR2R2; R7 is selected from the group of —H, —C1-6 alkyl, —C1-6 substituted alkyl, —C3-6 cycloalkyl, —CF3, aryl, and heteroaryl; R8 and R9 are independently selected from the group of —H, —C1-6 alkyl, —C1-6 substituted alkyl, aryl, heteroaryl, substituted aryl, substituted heteroaryl, —C1-6 alkyl-Q2, and —COOR3, or R8 and R9 are taken together with the adjacent N to form a cycle selected from the group of: M is selected from the group of —R15, —SO2R2, —SO2NR2R2, —OH and —NR2R12; V is selected from the group of —CR10R11—, —SO2—, —O— and —NR12—; with the proviso that only one of R8 or R9 can be —COOR3; R10 and R11 are independently selected from the group of —H, —C1-6 alkyl, —C1-6 substituted alkyl and —C3-6 cycloalkyl; R12 is selected from the group of —H, —C1-6 alkyl, -alkylsubstituted C1-6 alkyl, —CONR2R2, —SO2R3, —SO2NR2R2; R13 and R14 are independently selected from the group of —H, —C1-6 alkyl, —C3-6 cycloalkyl, —C1-6 substituted alkyl, —C1-6 alkyl-Q3, C1-6 substituted alkyl-Q3 and Q3 is selected from the group of heteroaryl, substituted heteroaryl, —NR2R12, —CONR2R2, —COOR2, —OR2, and —SO2R3; R15 is selected from the group of —C1-6 alkyl, —C3-6 cycloalkyl, —C1-6 substituted alkyl, —C1-6 alkyl-Q3, —C1-6 alkyl-C3-6 cycloalkyl-Q3 and —C1-6 substituted alkyl-Q3, R16 is selected from the group of —H, —C1-6 alkyl, —NR2R2, and —COOR2; with the proviso that when V is —NR12—; R16 cannot be —NR2R2; and R17 is selected from the group of —H, —C1-6 alkyl, —COOR3, and aryl. |
