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1. 发明授权

US5514692A Substituted quinoline derivatives useful as antipiconaviral agents 失效
标题翻译：可用作抗病毒药物的取代喹啉衍生物
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。

2. 发明授权

US5514679A Therapeutic phenoxyalklpyridazines and intermediates therefor 失效
标题翻译：治疗性苯氧亚胺idaz嗪及其中间体
公开(公告)号：US5514679A
公开(公告)日：1996-05-07
申请号：US242528
申请日：1994-05-13
申请人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Theodore J. Nitz
发明人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Theodore J. Nitz
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。

3. 发明授权

US5821243A Compounds compositions and methods for treating influenza 失效
标题翻译：用于治疗流感的化合物组合物和方法
公开(公告)号：US5821243A
公开(公告)日：1998-10-13
申请号：US858649
申请日：1997-05-19
申请人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
发明人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
IPC分类号： C07D237/02 , A61K31/50 , A61K31/501 , A61P31/16 , C07D237/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/495 , C07D401/00
CPC分类号： C07D403/10 , C07D237/14 , C07D407/10
摘要： A compound of the formula: ##STR1## wherein R.sub.1 represents a lower alkyl (C.sub.1 --C.sub.6) substituent which may be straight or branched; R.sub.2 represents an aryl substituent of the formula: ##STR2## and Q, V, W, X, Y and Z are as set forth in the accompanying specification. These compounds are useful in prophylaxis and treatment of influenza virus infection.
摘要翻译：下式化合物：其中R 1表示可以是直链或支链的低级烷基（C1-C6）取代基; R2表示下式的芳基取代基：其中Q，V，W，X，Y和Z如所附说明书所述。这些化合物可用于预防和治疗流感病毒感染。

4. 发明授权

US5567717A Heterocycle substituted phenoxyalkylheterocycles and their use as antiviral agents 失效
标题翻译：杂环取代的苯氧基烷基杂环和它们作为抗病毒剂的用途
公开(公告)号：US5567717A
公开(公告)日：1996-10-22
申请号：US461285
申请日：1995-06-05
申请人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Theodore J. Nitz
发明人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Theodore J. Nitz
IPC分类号： C07D237/08 , C07D307/42 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14 , A61K31/34 , C07D407/12 , C07D409/12 , C07D417/12
CPC分类号： C07D307/42 , C07D237/08 , C07D403/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D413/12 , C07D413/14
摘要： A compound of the formula ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification.
摘要翻译：其中Y，R1，R2，R3，R4和R5如本说明书中所定义的式IMA化合物。

5. 发明授权

US5523312A Antipicornaviral agents 失效
标题翻译：止痒病毒药
公开(公告)号：US5523312A
公开(公告)日：1996-06-04
申请号：US312724
申请日：1994-09-27
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 , A61K31/41 , C07D261/08 , C07D263/32 , C07D271/06
CPC分类号： C07D413/06 , C07D413/14
摘要： 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.
摘要翻译：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。

6. 发明授权

US06271373B1 Compounds, compositions and methods for treating influenza 失效
标题翻译：用于治疗流感的化合物，组合物和方法
公开(公告)号：US06271373B1
公开(公告)日：2001-08-07
申请号：US09654209
申请日：2000-09-01
申请人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
发明人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
IPC分类号： C07D40100
CPC分类号： C07D403/10 , C07D237/14 , C07D407/10
摘要： A compound produced by the process comprising the step of reacting a starting compound of the formula: with FeCl3 in the presence of acetic acid, wherein the reaction mixture is heated and the temperature of the reaction mixture is about 85° C.to about reflux temperature, R1 and R2 in the above formula being as defined in the present specification.
摘要翻译：通过该方法制备的化合物包括使下式的起始化合物与FeCl 3在乙酸存在下反应的步骤，其中将反应混合物加热并将反应混合物的温度为约85℃至约回流温度上述式中的R 1和R 2如本说明书中所定义。

7. 发明授权

US06180628B2 Compounds, compositions and methods for treating influenza 失效
标题翻译：用于治疗流感的化合物，组合物和方法
公开(公告)号：US06180628B2
公开(公告)日：2001-01-30
申请号：US09371057
申请日：1999-08-09
申请人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
发明人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
IPC分类号： A61P3116
CPC分类号： C07D403/10 , C07D237/14 , C07D407/10
摘要： Compounds of the formula: wherein R1 represents a lower alkyl (C1-C6) substituent which may be straight or branched; R2 represents an aryl substituent of the formula: and Q, V, W, X, Y and Z are as set forth in the accompanying specification, are useful in prophylaxis of influenza virus infection.
摘要翻译：下式的化合物：其中R 1表示可以是直链或支链的低级烷基（C1-C6）取代基; R2表示下式的芳基取代基：Q，V，W，X，Y和Z如所附说明书所述，可用于预防流感病毒感染。

8. 发明授权

US6127384A Compounds, compositions and methods for treatment of hepatitis C 失效
标题翻译：用于治疗丙型肝炎的化合物，组合物和方法
公开(公告)号：US6127384A
公开(公告)日：2000-10-03
申请号：US84538
申请日：1998-05-26
申请人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz
发明人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz
IPC分类号： C07D211/58 , C07D211/62 , C07D401/14 , A01N43/40
CPC分类号： C07D401/14 , C07D211/58 , C07D211/62
摘要： Derivatives of piperidine are useful in prophylaxis and treatment of hepatitis C virus infections.
摘要翻译：哌啶的衍生物可用于预防和治疗丙型肝炎病毒感染。

9. 发明授权

US5935957A Compounds, compositions and methods for treating influenza 失效
标题翻译：用于治疗流感的化合物，组合物和方法
公开(公告)号：US5935957A
公开(公告)日：1999-08-10
申请号：US82656
申请日：1998-05-21
申请人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
发明人： Guy D. Diana , Thomas R. Bailey , Theodore J. Nitz , Dorothy C. Young , William P. Gorczyca
IPC分类号： C07D237/02 , A61K31/50 , A61K31/501 , A61P31/16 , C07D237/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K43/60
CPC分类号： C07D403/10 , C07D237/14 , C07D407/10
摘要： Compounds of the formula: ##STR1## wherein R1 represents a lower alkyl (C1-C6) substituent which may be straight or branched; R2 represents an aryl substituent of the formula: ##STR2## and Q, V, W, X, Y and Z are as set forth in the accompanying specification, are useful in prophylaxis of influenza virus infection.
摘要翻译：下式的化合物：其中R 1表示可以是直链或支链的低级烷基（C1-C6）取代基; R2表示下式的芳基取代基：Q，V，W，X，Y和Z如所附说明书所述，可用于预防流感病毒感染。

10. 发明授权

US5618821A Therapeutic phenoxyalkylheterocycles 失效
标题翻译：治疗苯氧基烷基杂环
公开(公告)号：US5618821A
公开(公告)日：1997-04-08
申请号：US451692
申请日：1995-05-26
申请人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Gee-Hong Kuo , Theodore J. Nitz
发明人： David J. Aldous , Thomas R. Bailey , Guy D. Diana , Gee-Hong Kuo , Theodore J. Nitz
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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