| 摘要 |
A succinimide or maleimide derivative has the formula (I) wherein: R1 is -CH2 -, -CH2CO- or -CO-; R2 and R3 taken together are (i) ethylene optionally substituted with alkyl or phenyl; (ii) vinylene substituted with two substituents each selected, independently of the other, from alkyl or phenyl or (iii) a divalent cycloalkyl of 5-10 carbon atoms optionally substituted with one or more substituents of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl optionally substituted with alkyl, acetoxy, carboxy, hydroxy, optionally substituted amino, alkyl, alkoxy, norbornyl, phenyl or halo; R4 is a 3,4-disubstituted phenyl substituted with two substituents each selected, independently of the other of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, optionally substituted amino, alkyl, alkoxy, cycloalkyl, bicycloalkyl, phenyl or halo; R5 is -CH2COX; X is NH2, OH, NHR, or OR6; R is alkyl and R6 is alkyl or benzyl. A pharmaceutical composition thereof is useful in inhibiting TNFa-activated retrovirus replication in a mammal or inhibiting phosphodiesterase.
|
