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    • 35. 发明授权
    • Antipicornaviral agents
    • 止痒病毒药
    • US5523312A
    • 1996-06-04
    • US312724
    • 1994-09-27
    • David J. AldousThomas R. BaileyGuy D. DianaGee-Hong KuoTheodore J. NitzMichael Reuman
    • David J. AldousThomas R. BaileyGuy D. DianaGee-Hong KuoTheodore J. NitzMichael Reuman
    • C07D413/06C07D413/14A61K31/41C07D261/08C07D263/32C07D271/06
    • C07D413/06C07D413/14
    • Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.
    • 本文公开了用于对抗小核糖核酸病毒和预防或治疗小RNA病毒感染的化合物和药物组合物。 化合物具有下式:其中Het1选自恶唑基,异恶唑基,恶二唑基; Y是3〜9个碳原子的亚烷基桥; Het2是苯并呋喃基或吲哚基; R 1和R 2各自独立地选自氢,卤素,乙酰基,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; 并且R 3是恶唑基,恶二唑基,异恶唑基或被烷基,卤素,烷氧基烷基,环烷基,卤代烷基,羟基烷基,烷氧基,羟基,呋喃基,噻吩基或氟代烷基取代的任何一个。 其N-氧化物或其药学上可接受的酸加成盐。
    • 39. 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。