Antiviral ethers of aspartate protease substrate isosteres

Details Antiviral ethers of aspartate protease substrate isosteres Antiviral ethers of aspartate protease substrate isosteres

C - Chemistry, Metallurgy

07

C

C07C 271/10 (2006.01) A61K 31/27 (2006.01) A61K 31/33 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) C07C 255/60 (2006.01) C07C 271/22 (2006.01) C07C 311/19 (2006.01) C07C 311/41 (2006.01) C07C 311/42 (2006.01) C07C 317/50 (2006.01) C07D 207/26 (2006.01) C07D 207/263 (2006.01) C07D 207/28 (2006.01) C07D 209/42 (2006.01) C07D 211/46 (2006.01) C07D 211/62 (2006.01) C07D 213/30 (2006.01) C07D 213/56 (2006.01) C07D 213/82 (2006.01) C07D 277/06 (2006.01) C07D 277/40 (2006.01) C07D 295/155 (2006.01) C07D 30

Patent

CA 2160763

Antiretroviral compounds (which are effective, for example, against HIV) of the formula I Image (I) in which R1 is an acyl radical lower-alkoxy-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amino, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl; or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals); R2 and R3 are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy,carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen; R4 is lower alkyl, cyclohexyl or phenyl; and R5 is lower alkyl; and n is 1 or 2,or salts thereof, are novel.

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