Patent ID: 6503890
Filing Date: 2003-01-07
Classification: A61K,A61P,C07H,Y10S

Abstract:
A method for inhibiting HIV reverse transcriptase activity in cells infected with HIV, comprising administering to the infected cells an effective inhibitory amount of a compound of the formula: whereinY is oxygen or sulfur; R1 is aryl mono-substituted with Br, Cl, or I; R2 is a nucleoside of formula II or III: â€ƒwherein R6 is purine or pyrimidine; R7, R8, R9, R10, R11, and R12 are independently hydrogen, hydroxy, halo, azido, â€”NO2, â€”NR13R14, or â€”N(OR15)R16, wherein R13, R14, R15, and R16 are independently hydrogen, acyl, alkyl, or cycloalkyl; R3 is hydrogen, acyl, alkyl, or cycloalkyl; R4 is a side chain of an amino acid; or R3 and R4 may be taken together to form a proline or hydroxyproline side chain; and R5 is hydrogen, alkyl, cycloalkyl, or aryl; or a pharmaceutically acceptable salt or ester thereof.