AZAHEXANE DERIVATIVES AS SUBSTRATE ISOSTERS OF RETROVIRAL ASPARATE PROTEASES

摘要

The invention relates to compounds of formula (I): wherein R1 and R10 are eachindependently of the other lower alkoxycarbonyl; either R2, R3 and R4 are eachindependently of the other C1-C4alkyl and R7, R8 and R9 are each selected fromhydrogen and C1-C4alkyl, with not more than 2 of the radicals being hydrogen;or R7, R8 and R9 are each independently of the other C1-C4alkyl and R2, R3 andR4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicalsbeing hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl;or salts thereof; those compounds are inhibitors of retroviral aspartateproteases and are effective, for example, against HIV.