Broadspectrum 2-amino-benzothiazole sulfonamide hiv protease...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 417/12 (2006.01) A61K 31/425 (2006.01) A61P 31/18 (2006.01) C07D 277/82 (2006.01) C07D 493/04 (2006.01)

Patent

CA 2492832

The present invention relates to the use of 2-amino-benzothiazoles, having the formula (I) wherein R1 is hexahydrofuro[2,3-b]furanyl, tetrahydrofuranyl, oxazolyl, thiazolyl, pyridinyl, or phenyl optionally substituted with one or more substituents independently selected from C1-6-alkyl, hydroxy, amino, halogen, aminoC1-4-alkyl and mono-or di(C1-4alkyl)amino; R2 is hydrogen or C1- 6alkyl; L is a direct bond, -0-, C1-6alkanediyl-O- or -O-C1-6alkanediyl; R3 is phenylC1-4alkyl; R4 is C1-6alkyl; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; in the manufacture of a medicament useful for inhibiting mutant HIV protease in a mammal infected with said mutant HIV protease. It also relates to novel compounds of formula (I).

La présente invention concerne l'utilisation de 2-amino-benzothiazoles, représentés par la formule (I) dans laquelle R¿1? est héxahydrofuro[2,3-b]furanyle, tétrahydrofuranyle, oxazolyle, thiazolyle, pyridinyle, ou phényle éventuellement substitué par un ou plusieurs substituants indépendamment sélectionnés parmi C¿1-6?alkyle, hydroxy, amino, halogène, aminoC¿1-4?alkyle et mono ou di(C¿1-4?alkyl)amino; R¿2? est hydrogène ou C¿1-6?alkyle; L est une liaison directe, -0-, C¿1-6?alkanediyl-O- ou -O-C¿1-6?alkanediyl; R¿3? est phénylC¿1-4?alkyle; R¿4? est C¿1-6?alkyle; R¿5? est hydrogène ou C¿1-6?alkyle; et R¿6? est hydrogène ou C¿1-6?alkyle. Ces composés sont utilisés dans la fabrication d'un médicament servant à inhiber la protéase du VIH mutant chez un mammifère infecté par ladite protéase du VIH mutant. L'invention concerne également de nouveaux composés représentés par la formule (I).

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