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公开(公告)号：US5763461A
公开(公告)日：1998-06-09
申请号：US822995
申请日：1997-03-21
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , A61K31/44 , A61K31/415 , A61K31/47 , A61K31/505 , C07D213/16 , C07D239/26 , C07D401/10 , C07D403/10
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US5750527A
公开(公告)日：1998-05-12
申请号：US863388
申请日：1997-05-27
IPC分类号： C07D285/12 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/495 , A61K31/505 , A61P31/12 , A61P31/14 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/13 , C07D417/12 , A61K31/50
CPC分类号： C07D417/12
摘要： Described herein are compound of the formula: ##STR1## wherein: Thi is thiadiazolyl or substituted thiadiazolyl; Y is 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, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl, or cyano; R.sub.3 is a heterocyclyl chosen from pyrimidinyl, pyrazinyl, or pyridazinyl; or a pharmaceutically acceptable salt thereof which are effective antipicornaviral agents.
摘要翻译： 本文描述的是下式的化合物：其中：Thi是噻二唑基或取代的噻二唑基; 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， ，或氰基; R3是选自嘧啶基，吡嗪基或哒嗪基的杂环基; 或其药学上可接受的盐是有效的抗虫病毒药剂。
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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：US5665763A
公开(公告)日：1997-09-09
申请号：US706109
申请日：1996-08-30
IPC分类号： C07D237/08 , C07D307/42 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14 , A61K31/34 , A61K31/38 , C07D409/12
CPC分类号： C07D307/42 , C07D237/08 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14
摘要： Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification,Y is alkylene of 3 to 9 carbon atoms,R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, oxazolinyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or any of the above substituted with alkyl, alkoxyalkyl, cycloalkyl, halo alkyl, hydroxyalkyl, alkoxy, hydroxy, halo, furyl, thienyl, fluoroalkyl;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.
摘要翻译： 其中：R1，R2，R3和R4如说明书中所定义，Y是3至9个碳原子的亚烷基，R 5是烷氧基羰基，烷基四唑基，苯基或选自苯并恶唑基的杂环， 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，恶唑啉基，异恶唑基，异噻唑基，呋喃基，三唑基，噻吩基，吡啶基，嘧啶基，吡嗪基，哒嗪基或任何上述被烷基，烷氧基烷基，环烷基， ，羟基烷基，烷氧基，羟基，卤素，呋喃基，噻吩基，氟代烷基; 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。
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公开(公告)号：US5821257A
公开(公告)日：1998-10-13
申请号：US52178
申请日：1998-03-31
IPC分类号： C07D285/12 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/495 , A61K31/505 , A61P31/12 , A61P31/14 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/13 , C07D417/12
CPC分类号： C07D417/12
摘要： Compounds of the formula; ##STR1## wherein: Thi is thiadiazolyl or substituted thiadiazolyl alkoxy, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1-difluoroethyl, halo, alkyl, cycloalkyl, hydroxyalkyl, or Y is 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, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl, or cyano; R.sub.3 is a heterocyclyl chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, oxazolyl, thiazolyl, oxadiazolyl, isoxazolyl, isothiazolyl, or substituted heterocyclyl wherein the substitution is with alkyl, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl; or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.
摘要翻译： 式的化合物; 式I其中：Thi是噻二唑基或取代的噻二唑基烷氧基，氟甲基，二氟甲基，三氟甲基，1,1-二氟乙基，卤素，烷基，环烷基，羟烷基或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， ，或氰基; R3是选自苯并恶唑基，苯并噻唑基，噻二唑基，恶唑基，噻唑基，恶二唑基，异恶唑基，异噻唑基或取代的杂环基的杂环基，其中取代为烷基，烷氧基烷基，环烷基，卤代烷基，羟烷基，烷氧基，羟基，呋喃基，噻吩基或氟代烷基 ; 或其药学上可接受的盐是有效的抗虫病毒药剂。
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公开(公告)号：US5650419A
公开(公告)日：1997-07-22
申请号：US706108
申请日：1996-08-30
IPC分类号： C07D285/12 , A61K31/41 , A61K31/42 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/495 , A61K31/505 , A61P31/12 , A61P31/14 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/13 , C07D417/12
CPC分类号： C07D417/12
摘要： Described herein are compounds of the formula; ##STR1## wherein: Thi is a unsubstituted or substituted thiadiazolyl;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, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxylcarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, substituted or unsubstituted phenyl, alkyltetrazolyl or a substituted or unsubstituted imidazolyl, dihydroimidazolyl, pyrazolyl, furyl, thiazolyl or thienyl or a pharmaceutically acceptable salt thereof are effective antipicornaviral agents.
摘要翻译： 本文描述的是式的化合物; 式I其中：Thi是未取代或取代的噻二唑基; 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， 氰基; R3是烷氧基羰基，取代或未取代的苯基，烷基四唑基或取代或未取代的咪唑基，二氢咪唑基，吡唑基，呋喃基，噻唑基或噻吩基或其药学上可接受的盐是有效的抗虫病毒剂。
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公开(公告)号：US5514692A
公开(公告)日：1996-05-07
申请号：US449463
申请日：1995-05-24
申请人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Gee-Hong Kuo , Theodore J. Nitz , Michael Reuman
发明人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Gee-Hong Kuo , Theodore J. Nitz , Michael Reuman
IPC分类号： C07D413/06 , C07D413/14 , A61K31/47 , C07D401/04
CPC分类号： C07D413/06 , C07D413/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US5514679A
公开(公告)日：1996-05-07
申请号：US242528
申请日：1994-05-13
IPC分类号： C07D237/08 , C07D307/42 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14 , A61K31/50 , C07D237/12
CPC分类号： C07D307/42 , C07D237/08 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US5618821A
公开(公告)日：1997-04-08
申请号：US451692
申请日：1995-05-26
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , A61K31/44 , A61K31/505 , C07D213/16 , C07D239/26
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： Compounds of the formula ##STR1## wherein Q is chosen from the group consisting of pyridyl, pyrazyl, pyrimidyl, quinolyl, indolyl and 7-azaindolyl or any of these substituted with one or two substituents;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, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.3 is alkoxycarbonyl, alkyltetrazolyl, substituted or unsubstituted phenyl or heterocyclyl, the N-oxide thereof, or a pharmaceutically acceptable acid addition salt thereof is an effective antipicornaviral agent.
摘要翻译： 式I的化合物，其中Q选自吡啶基，吡唑基，嘧啶基，喹啉基，吲哚基和7-氮杂吲哚基，或者被一个或两个取代基取代的那些; 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，取代或未取代的苯基或杂环基，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剂。
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