Antiviral proteaz inhibitörleri

Bu bulus yeni proteaz inhibitörlerine ve özelliklerine ve özellikle de bazi retrovirüslerin, öncelikle de HIV'nin sahip oldugu aspartat proteaz inhibitörlerine iliskin bir bulustur. Bulus ayrica bu tür proteaz inhibitörlerinin retrovirüslerin neden oldugu durumlarin tedavisinde ve bu amaca yönelik ilaçlarin hazirlanmasinda kullanimlarina iliskindir. Bulus proteaz inhibitörlerinin ve benzeri kimyasal yapilarin kolay hazirlanmasina yönelik yeni sentez metodoljisine de iliskindir. Compounds of the formula I : wherein: A' and A" are independently the same or different group of the formula II : wherein: R' is H, CH 3 , C(CH 3 ) 2 , -OR a , -N(R a ) 2 , -N(R a )OR a or -DP R''' is H or CH 3 ; R a is H, C 1 -C 3 alkyl; D is a bond, alkylene, -C(=O)-, -S(O)- or -S(O) 2 - ; P is an optionally substituted, mono or bicyclic carbo- or heterocycle; R" is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH 2 ) n DP; M is a bond or -C(=O)N(R''')-; Q is absent, a bond, -CH(OH)- or -CH 2 -; or R" together with Q , M and R' define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R' is -OR a , -N(R a ) 2 , -N(R a )OR a or -DP, if M is a bond and Q is absent; X is H, OH, OCH 3 ; Y is H, OH, OCH 3 , but X and Y are not both H; Z' and Z" are independently -(CH 2 ) m P where P is as defined above; n and m are independently 0,1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.