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    • 9. 发明授权
    • Therapeutic phenoxyalkylazoles and phenoxyalkylazines
    • 治疗性苯氧基烷基唑和苯氧基烷基嗪
    • US5721261A
    • 1998-02-24
    • US693530
    • 1996-08-02
    • David J. AldousThomas R. BaileyGuy Dominic DianaTheodore J. NitzGee-Hong Kuo
    • David J. AldousThomas R. BaileyGuy Dominic DianaTheodore J. NitzGee-Hong Kuo
    • C07D257/04C07D271/06C07D277/24C07D403/12C07D405/12C07D413/12C07D417/12C07D521/00A61K31/41
    • C07D257/04C07D231/12C07D233/56C07D249/08C07D271/06C07D277/24C07D403/12C07D405/12C07D413/12C07D417/12
    • Compounds of the formula ##STR1## wherein Azo is alkyltetrazolyl or is chosen from the group consisting of oxadiazolyl, imidazolyl, pyrazolyl, triazolyl, oxazolyl, triazinyl, thiazolyl, isothiazolyl or any of these substituted with a member of the group consisting of alkyl, alkylthio, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkanoyl, fluoroalkyl or the N-oxide of any of the preceding; Y is an alkylene bridge of 3-9 carbon atoms; R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano; R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or substituted phenylor substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl or fluoroalkyl; the N-oxide thereof; or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agents.
    • 式I的化合物,其中偶氮是烷基四唑基或选自恶二唑基,咪唑基,吡唑基,三唑基,恶唑基,三嗪基,噻唑基,异噻唑基或其中任何一个被烷基取代的基团 ,烷硫基,烷氧基,羟基,卤素,氰基,硝基,羟基烷基,烷氧基烷基,烷氧基羰基,烷酰基,氟代烷基或任何前述的N-氧化物; Y是3-9个碳原子的亚烷基桥; R 1和R 2各自独立地选自氢,卤素,烷基,烯基,氨基,烷硫基,羟基,羟基烷基,烷氧基烷基,烷硫基烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,烷氧基,硝基,羧基,烷氧基羰基,二烷基氨基烷基,烷基氨基烷基,氨基烷基,二氟甲基,三氟甲基或 氰基; R3是烷氧基羰基,烷基四唑基,苯基或选自苯并恶唑基,苯并噻唑基,噻二唑基,咪唑基,二氢咪唑基,恶唑基,噻唑基,恶二唑基,吡唑基,异恶唑基,异噻唑基,呋喃基,三唑基,四唑基,噻吩基,吡啶基,嘧啶基,吡嗪基,哒嗪基或 取代的苯基或取代的杂环基,其中取代为烷基,烷氧基烷基,环烷基,卤代烷基,羟基烷基,烷氧基,羟基,呋喃基,噻吩基或氟代烷基; 其N-氧化物; 或其药学上可接受的酸加成盐是有效的抗虫病毒药剂。