Patent ID: 6465433
Filing Date: 2002-10-15
Classification: A61K,A61P,C07F,C07K

Abstract:
A method for inhibiting HIV replication in an animal in need of said inhibiting, comprising administering to said animal an effective amount a proteasome inhibitor of formula (1a) or a pharmaceutically acceptable salt thereof; whereinP is R7â€”C(O)â€” or R7â€”SO2â€”, where R7 is pyrazinyl; X2 is â€”C(O)â€”NHâ€”, R is hydrogen or alkyl; R2 and R3 are independently hydrogen, alkyl, cycloalkyl, aryl, or â€”CH2â€”R5; R5, in each instance, is one of aryl, aralkyl, alkaryl, cycloalkyl, or â€”Wâ€”R6, where W is a chalcogen and R6 is alkyl; where the ring portion of any of said aryl, aralkyl, or alkaryl in R2, R3 and R5 can be optionally substituted by one or two substituents independently selected from the group consisting of C1-6 alkyl, C3-8 cycloalkyl, C1-6alkyl(C3-8)cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, cyano, amino, C1-6 alkylamino, di(C1-6)alkylamino, benzylamino, dibenzylamino, nitro, carboxy, carbo(C1-6)alkoxy, trifluoromethyl, halogen, C1-6 alkoxy, C6-10 aryl, C6-10 aryl(C1-6)alkyl, C6-10 aryl(C1-6)alkoxy, hydroxy, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C6-10 arylthio, C6-10 arylsulfinyl, C6-10 arylsulfonyl, C6-10 aryl, C1-6 alkyl(C6-10)aryl, and halo(C6-10)aryl; Z1 and Z2 are independently one of hydroxy, alkoxy, or aryloxy, or together Z1 and Z2 form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising carbon atoms and, optionally, a heteroatom or heteroatoms which can be N, S, or O; and A is zero.