Azahexane derivatives as substrate isosters of retroviral...

C - Chemistry – Metallurgy – 07 – C

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C07C 271/22 (2006.01) A61K 31/27 (2006.01) A61K 31/275 (2006.01)

Patent

CA 2237016

The invention relates to compounds of formula (I): wherein R1 and R10 are each independently of the other lower alkoxycarbonyl; either R2, R3 and R4 are each independently of the other C1-C4alkyl and R7, R8 and R9 are each selected from hydrogen 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 and R4 are each selected from hydrogen and C1-C4alkyl, with 1 or 2 of the radicals being hydrogen; R5 is phenyl or cyclohexyl; and R6 is phenyl or cyanophenyl; or salts thereof; those compounds are inhibitors of retroviral aspartate proteases and are effective, for example, against HIV.

L'invention concerne des composés de la formule (I) ou des sels de ceux-ci. Dans cette formule, R¿1? et R¿10? représentent chacun indépendamment alcoxycarbonyle inférieur, soit R¿2?, R¿3? et R¿4? représentent chacun indépendamment alkyle C¿1?-C¿4?, et R¿7?, R¿8? et R¿9? représentent chacun hydrogène ou alkyle C¿1?-C¿4?, deux de ces radicaux au maximum représentant hydrogène, soit R¿7?, R¿8? et R¿9? représentent chacun indépendamment alkyle C¿1?-C¿4? et R¿2?, R¿3? et R¿4? représentent chacun hydrogène ou alkyle C¿1?-C¿4?, 1 ou 2 de ces radicaux représentant hydrogène, R¿5? représente phényle ou cyclohexyle, et R¿6? représente phényle ou cyanophényle. Ces composés sont des inhibiteurs des aspartates protéases rétrovirales et ils sont efficace, par exemple, contre le VIH.

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