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    • 6. 发明授权
    • Substituted quinoline derivatives useful as antipiconaviral agents
    • 可用作抗病毒药物的取代喹啉衍生物
    • US5514692A
    • 1996-05-07
    • US449463
    • 1995-05-24
    • David J. AldousThomas R. BaileyGuy D. DianaGee-Hong KuoTheodore J. NitzMichael Reuman
    • David J. AldousThomas R. BaileyGuy D. DianaGee-Hong KuoTheodore J. NitzMichael Reuman
    • C07D413/06C07D413/14A61K31/47C07D401/04
    • C07D413/06C07D413/14
    • The invention discloses compounds of the formula ##STR1## wherein, Het.sub.1 is chosen from the group consisting of substituted or unsubstituted furyl, oxazolyl, isoxazolyl, oxadiazolyl, tetrazolyl, thiadiazolylY is an alkylene bridge of 3 to 9 carbon atoms.Het.sub.2 is quinolyl quinolyl substituted by R.sub.1 and R.sub.2 ;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkyltetrazolyl, or substituted or unsubstituted heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, tetrazolyl, thiophenyl the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof are effective antipicornaviral agents.
    • 本发明公开了下式化合物:其中Het1选自取代或未取代的呋喃基,恶唑基,异恶唑基,恶二唑基,四唑基,噻二唑基,Y为3至9个碳原子的亚烷基桥。 Het2是被R1和R2取代的喹啉基喹啉基; 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, 或氰基; R3是烷基四唑基,或者是取代或未取代的选自苯并恶唑基,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,噻唑基,恶唑基,呋喃基,三唑基,四唑基,噻吩基,其N-氧化物或其药学上可接受的酸 其加成盐是有效的抗虫病毒药剂。
    • 7. 发明授权
    • Therapeutic phenoxyalklpyridazines and intermediates therefor
    • 治疗性苯氧亚胺idaz嗪及其中间体
    • US5514679A
    • 1996-05-07
    • US242528
    • 1994-05-13
    • David J. AldousThomas R. BaileyGuy D. DianaTheodore J. Nitz
    • David J. AldousThomas R. BaileyGuy D. DianaTheodore J. Nitz
    • C07D237/08C07D307/42C07D403/12C07D405/04C07D405/12C07D407/04C07D413/12C07D413/14A61K31/50C07D237/12
    • C07D307/42C07D237/08C07D403/12C07D405/04C07D405/12C07D407/04C07D413/12C07D413/14
    • Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.
    • 其中:R1和R2独立地是氢,卤素,烷基,烯基,烷氧基,羟基,羟基烷基,羟基卤代烷基,烷氧基烷基,烷基硫代炔基,羟基烷氧基,烷基硫代烷基,烷基亚磺酰基烷基,烷基磺酰基烷基,氨基,氨基烷基,烷基氨基烷基 ,二烷基氨基烷基,烷氧基羰基,羧基或氰基甲基,硝基,二氟甲基,三氟甲基或氰基; Y为3至9个碳原子的亚烷基; R3和R4独立地是氢,烷基,烷氧基,羟基,环烷基,羟基烷基,羟基卤代烷基,烷氧基烷基,羟基烷氧基,烷硫基烷基,烷酰基,烷酰氧基,烷基亚磺酰基烷基,烷基磺酰基烷基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,烷氧基羰基,羧基,氰基甲基,氟代烷基, ,炔基,烯烃或卤素; R5是烷氧基羰基,烷基四唑基,苯基或杂环; 或其药学上可接受的酸加成盐; 其N-氧化物可用作抗血管病毒药物。
    • 10. 发明授权
    • Therapeutic phenoxyalkylheterocycles
    • 治疗苯氧基烷基杂环
    • US5763461A
    • 1998-06-09
    • US822995
    • 1997-03-21
    • David J. AldousThomas R. BaileyGuy Dominic DianaGee-Hong KuoTheodore J. Nitz
    • David J. AldousThomas R. BaileyGuy Dominic DianaGee-Hong KuoTheodore J. Nitz
    • C07D401/12C07D403/12C07D405/12C07D413/12C07D471/04A61K31/44A61K31/415A61K31/47A61K31/505C07D213/16C07D239/26C07D401/10C07D403/10
    • C07D401/12C07D403/12C07D405/12C07D413/12C07D471/04
    • Compounds of the formula ##STR1## wherein Pyr is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substitutents chosen from alkyl, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkanoyl, fluoroalkyl or the N-oxide of any of these; Y is an alkylene bridge of 3-9 carbon atoms; R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylaikyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano; R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, phenyl or heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazlnyl, pyridazinyl or a substituted phenyl or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, halo alkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, or thienyl or fluoroalkyl, the N-oxide thereof, or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agents.
    • 下式的化合物其中Pyr选自吡啶基,吡唑基,嘧啶基,喹啉基,吲哚基和7-氮杂吲哚基,或者被一个或两个选自烷基,烷氧基,羟基,卤代的取代基取代的那些 氰基,硝基,羟基烷基,烷氧基烷基,烷酰基,氟代烷基或其中任何一种的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,异唑基,异噻唑基,呋喃基,三唑基,噻吩基,吡啶基,嘧啶基,吡嗪基,哒嗪基或取代苯基 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,呋喃基或噻吩基或氟代烷基,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。