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公开(公告)号：US5846986A
公开(公告)日：1998-12-08
申请号：US978233
申请日：1997-11-25
IPC分类号： C07D257/04 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00 , A61K31/41
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： 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.
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公开(公告)号：US5721261A
公开(公告)日：1998-02-24
申请号：US693530
申请日：1996-08-02
IPC分类号： C07D257/04 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00 , A61K31/41
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US5552420A
公开(公告)日：1996-09-03
申请号：US242752
申请日：1994-05-13
IPC分类号： C07D257/04 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00 , A61K31/41
CPC分类号： C07D257/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/06 , C07D277/24 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula ##STR1## wherein Azo is alkyltetrazolyl, oxadiazolyl, imidazolyl, pyrazolyl, triazolyl, oxazolyl, triazinyl, thiazolyl, isothiazolyl;Y is an alkylene bridge of 3-9 carbon atoms;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 phenyl or substituted heterocyclyl is an effective antipicornaviral agents.
摘要翻译： 式I的化合物，其中偶氮是烷基四唑基，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; Y是3-9个碳原子的亚烷基桥; 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是有效的抗虫病毒药剂。
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公开(公告)号：US5356903A
公开(公告)日：1994-10-18
申请号：US52027
申请日：1993-04-22
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04
摘要： Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.
摘要翻译： 式
的化合物其中; R1是氢，低级烷基或三氟甲基; R2是低级烷基，三氟甲基或CH2X，其中X是羟基，氯代，低级烷基氨基或二氧代 - 烷基氨基; R3和R4各自为氢或氟; Z为NR5或CR6R7; R5是氢，芳基，芳硫基，芳基磺酰基，低级烷基，环烷基，杂环烷基，氨基 - 低级 - 烷基，低级 - 烷基氨基 - 低级 - 烷基，二 - 低级 - 烷基氨基 - 低级 - 烷基，低级 - 烷氧基，羟基或NR8R9; R6是氢，氰基，低级烷氧基羰基，低级烷酰基，硝基或低级烷基磺酰基; R7是氢，氰基，低级烷氧基羰基，低级烷酰基，硝基，芳基或低级烷基磺酰基; R8是氢，低级烷基，芳基，杂环烷基，氨基甲酰基，烷酰基，芳酰基，羟基 - 低级烷基; 并且R 9为氢，低级烷基或低级烷酰基或其药学上可接受的酸加成盐可用作抗癌剂。
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