Antipicornaviral agents

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 413/14 (2006.01) A61K 31/41 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) C07D 401/14 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/06 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2199275

Compounds of formula (A), wherein, Het1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyridazyl or pyrazyl; Y is an alkylene bridge of 3 to 9 carbon atoms. Het2 is a substituted or unsubstituted quinolyl, benzofuranyl, indolyl, benzothiazolyl or benzoxazolyl; R1 and R2 are hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano; R3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a substituted or unsubstituted heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, or pyridazinyl, the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof are effective antipicornaviral agents.

Les composés de la formule (A) constituent des agents antipicornaviraux efficaces. Dans ladite formule Het¿1? est choisi dans le groupe constitué de furyle, oxazolyle, isoxasolyle, oxadiazolyle, tétrazolyle, thiadiazolyle, pyridyle, pyridimidyle, pyridazyle ou pyrazyle substitués ou non substitués; Y représente un pont alkylène de 3 à 9 atomes de carbone; Het¿2? représente quinolyle, benzofuranyle, indolyle, benzothiazolyle ou benzoxazolyle substitués ou non substitués; R¿1? et R¿2? représentent hydrogène, halo, alkyle, alcényle, amino, alkylthio, hydroxy, hydroxyalkyle, alcoxyalkyle, alkylthioalkyle, alkylsulfinylalkyle, alkylsulfonylalkyle, alcoxy, nitro, carboxy, alcoxycarboxycarbonyle, dialkylaminoalkyle, alkylaminoalkyle, aminoalkyle, difluorométhyle, trifluorométhyle ou cyano; R¿3? représente alcoxycarbonyle, alkyltétrazolyle, phényle ou un hétérocyclyle substitué ou non substitué choisis parmi benzoxazolyle, benzothiazolyle, thiadiazolyle, imidazolyle, dihydroimidazolyle, oxazolyle, thiazolyle, oxadiazolyle, pyrazolyle, isoxazolyle, isothiazolyle, furyle, triazolyle, tétrazolyle, thiophényle, pyridyle, pyrimidinyle, pyrazinyle ou pyridazinyle, leur N-oxyde ou un sel d'addition d'acide acceptable sur le plan pharmaceutique de ceux-ci.

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