| 主权项 |
1. A pharmaceutical composition which comprises an HIV ameliorating amount of one or more of the compounds which are selected from the group consisting of:
a compound of formula I a compound of formula IIand
a compound of formula III wherein R1 is isopropenyl or isopropyl; J and E are independently —H or —CH3, and E is absent when the double bond is present; X is a phenyl or heteroaryl ring substituted with A, wherein A is at least one member selected from the group of —H, -halo, -hydroxyl, —C1-6 alkyl, —C1-6 alkoxy, and —COOR2; R2 is —H, —C1-6 alkyl, -alkyl substituted C1-6 alkyl or -aryl substituted C1-6 alkyl; 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, —C1-6alkyl-COOR2, —NHC(O)(CH2)n—COOR2, —SO2NR2C(O)R2, -tetrazole, and —CONHOH, wherein n=1-6; R3 is —C1-6 alkyl or -alkyl substituted C1-6 alkyl; R4 is selected from the group of —H, —C1-6 alkyl, —C1-6alkyl-C(OR3)2—C3-6cycloalkyl, —C1-6 substituted alkyl, —C1-6alkyl-C3-6cycloalkyl, —C1-6 alkyl-Q1, —C1-6 alkyl-C3-6 cycloalkyl-Q1, aryl, heteroaryl, substituted heteroaryl, —COR6, —COCOR6, —SO2R2, —SO2NR2R2, wherein Q1 is selected from the group of heteroaryl, substituted heteroaryl, halogen, —CF3, —OR2, —COOR2, —NR8R9, —CONR10R11 and —SO2R7; R5 is selected from the group of —H, —C1-6 alkyl, —C3-6 cycloalkyl, —C1-6 alkyl substituted alkyl, —C1-6alkyl-NR8R9, —COR10, —COR6, —COCOR6, —SO2R2 and —SO2NR2R2; with the proviso that only one of R4 or R5 can be selected from the group of —COR6, —COCOR6, —SO2R7 and —SO2NR2R2; or R4 and R5 are 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, SO2R2, —CONHSO2R3, and —CONHSO2NR2R2; R7 is selected from the group of —C1-6 alkyl, —C1-6 substituted alkyl, —C3-6cycloalkyl, 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 independently selected from the group of or R8 and R9 are taken together with the adjacent N to form a cycle selected from the group of: with the proviso that only one of R8 or R9 is —COOR3; R10 and R11 are independently selected from the group of —H, alkyl, —C1-6 substituted alkyl and —C3-6 cycloalkyl, or R10 and R11 are taken together with the adjacent N to form the cycle R12 is selected from the group of —C1-6 alkyl, —NR2R2, —C1-6 alkyl-OH, —C1-6 alkyl, —C1-6 substituted alkyl, —C3-6 cycloalkyl, —COR7, —COONR22R23, —SOR7, and —SONR24R25; 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, alkyl-C3-6 cycloalkyl-Q3, C1-6 substituted alkyl-Q3 and or R13 and R14 are taken together with the adjacent N to form a cycle selected from the group of: Q3 is selected from the group of heteroaryl, substituted heteroaryl, —NR20R21, —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 —COOR3; R17 is selected from the group of —H, —C1-6 alkyl, —COOR3, and aryl; R18 is selected from the group of —COOR2 and —C1-6 alkyl-COOR2; R19 is selected from the group of —H, —C1-6 alkyl, —C1-6 alkyl-Q4, —COR3, —COOR3, wherein Q4 is selected from the group of —NR2R2 and —OR2; R20 and R21 are independently selected from the group of —H, —C1-6 alkyl, —C1-6 substituted alkyl, —C1-6 substituted alkyl-OR2, and —COR3, or R20 and R21 are taken together with the adjacent N to form a cycle selected from the group of with the proviso that only one of R20 or R21 can be —COR3, R22 and R23 are independently selected from the group of H, —C1-6 alkyl, —C1-6 substituted alkyl, and —C1-6cycloalkyl, or R22 and R23 are taken together with the adjacent N to form a cycle selected from the group of R24 and R25 are independently from the group of H, —C1-6 alkyl, —C1-6 substituted alkyl, —C1-6 alkyl-Q5, —C1-6cycloalkyl, aryl, substituted aryl, heteroaryl, and substituted heteroaryl, and Q5 is selected from the group of halogen and SO2R3; including pharmaceutically acceptable salts thereof; together with one or more pharmaceutically acceptable carriers, excipients or diluents. |
