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21. 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。

22. 发明授权

US5763461A Therapeutic phenoxyalkylheterocycles 失效
标题翻译：治疗苯氧基烷基杂环
公开(公告)号：US5763461A
公开(公告)日：1998-06-09
申请号：US822995
申请日：1997-03-21
申请人： David J. Aldous , Thomas R. Bailey , Guy Dominic Diana , Gee-Hong Kuo , Theodore J. Nitz
发明人： David J. Aldous , Thomas R. Bailey , Guy Dominic Diana , Gee-Hong Kuo , Theodore J. Nitz
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。

23. 发明授权

US5750527A Thiadiazoles and their use as antipicornaviral agents 失效
标题翻译：噻二唑及其作为止痛药物的用途
公开(公告)号：US5750527A
公开(公告)日：1998-05-12
申请号：US863388
申请日：1997-05-27
申请人： David J. Aldous , Thomas R. Bailey , Guy Dominic Diana , Theodore J. Nitz
发明人： David J. Aldous , Thomas R. Bailey , Guy Dominic Diana , Theodore J. Nitz
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。

24. 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。

25. 发明授权

US5453433A Thiadiazoles and antipicornaviral compositions 失效
标题翻译：噻二唑类和反爪骨病毒组合物
公开(公告)号：US5453433A
公开(公告)日：1995-09-26
申请号：US242529
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： 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 , C07D417/02 , C07D413/02
CPC分类号： C07D417/12
摘要： Compounds 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 alkoxycarbonyl, phenyl, alkyltetrazolyl, or heterocyclyl; 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; 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是烷氧基羰基，苯基，烷基四唑基或杂环基; 或其药学上可接受的盐是有效的抗虫病毒药剂。

26. 发明授权

US5175177A 1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents 失效
标题翻译： 1,2,4-氧杂唑并 - 苯氧基甲基咪唑和它们作为抗病毒剂的用途
公开(公告)号：US5175177A
公开(公告)日：1992-12-29
申请号：US731569
申请日：1991-07-17
申请人： Guy D. Diana , Thomas R. Bailey
发明人： Guy D. Diana , Thomas R. Bailey
IPC分类号： A61K31/42 , A61K31/4245 , A61P31/12 , C07D413/12
CPC分类号： C07D413/10
摘要： Compounds of the formula ##STR1## wherein: Y is alkylene of 3 to 9 carbon atoms;R.sub.1 is lower-alkyl, lower-alkoxy-(C.sub.1-3 -alkyl), lower-alkoxycarbonyl, cyclopropyl or trifluoromethyl;R.sub.2 and R.sub.3 independently are hydrogen, lower-alkyl, halogen, lower-alkoxy, nitro, trifluoromethyl or hydroxy; andR.sub.4 is hydrogen or lower-alkyl; where lower-alkyl and lower-alkoxy, each occurrence, have from 1-5 carbon atoms;with the proviso that when R.sub.1 is lower-alkyl, at least one of R.sub.2 and R.sub.3 is hydroxy; or pharmaceutically acceptable acid-addition salts thereof are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.

27. 发明申请

US20110288075A1 Pyridazinone Derivatives 有权
标题翻译：哒嗪酮衍生物
公开(公告)号：US20110288075A1
公开(公告)日：2011-11-24
申请号：US13197243
申请日：2011-08-03
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
IPC分类号： A61K31/55 , A61K31/502 , A61K31/5025 , A61P25/00 , A61K31/50 , A61P25/28 , A61P25/18 , A61K31/501 , A61K31/5377
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
摘要翻译：本发明涉及介导酶活性的新的哒嗪酮衍生物。特别地，这些化合物可有效治疗与组胺H3受体活性相关的疾病或疾病状态，包括例如神经变性疾病，睡眠/觉醒障碍，注意缺陷多动障碍和认知/认知障碍。

28. 发明申请

US20100273779A1 Pyridazinone Derivatives 有权
标题翻译：哒嗪酮衍生物
公开(公告)号：US20100273779A1
公开(公告)日：2010-10-28
申请号：US12815813
申请日：2010-06-15
申请人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
发明人： Edward R. Bacon , Thomas R. Bailey , Nadine C. Becknell , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Kurt A. Josef , Lars J.S. Knutsen , Ming Tao , Allison L. Zulli
IPC分类号： A61K31/55 , C07D403/12 , A61K31/501 , A61K31/502 , C07D495/04 , A61P3/04 , A61P9/10 , A61P11/00 , A61P25/08 , A61P25/18 , A61P25/24 , A61P25/28 , A61P1/00 , A61P29/00
CPC分类号： C07D498/04 , C07D237/14 , C07D237/26 , C07D237/32 , C07D237/36 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D495/04
摘要： The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
摘要翻译：本发明涉及介导酶活性的新型吡哒嗪酮衍生物。特别地，这些化合物可有效治疗与组胺H3受体活性相关的疾病或疾病状态，包括例如神经变性疾病，睡眠/觉醒障碍，注意力缺陷多动障碍和认知。

29. 发明申请

US20100227892A1 Compounds, Compositions and Methods for Treatment and Prevention of Orthopoxvirus Infections and Associated Diseases 有权
标题翻译：用于治疗和预防正痘病毒感染和相关疾病的化合物，组合物和方法
公开(公告)号：US20100227892A1
公开(公告)日：2010-09-09
申请号：US12752462
申请日：2010-04-01
申请人： Robert Jordan , Thomas R. Bailey , Susan R. Rippin
发明人： Robert Jordan , Thomas R. Bailey , Susan R. Rippin
IPC分类号： A61K31/4439 , A61K31/343 , C07D307/77 , A61K31/403 , C07D209/56 , C07D401/12 , C07D209/48 , A61K31/4178 , C07D277/593 , A61P31/12
CPC分类号： A61K31/403 , A61K31/407 , A61K31/4439
摘要： Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
摘要翻译：使用二，三和四环酰肼衍生物和类似物的方法以及含有它们的药物组合物用于治疗或预防病毒感染和与之相关的疾病，特别是由正痘病毒引起的那些病毒感染和相关疾病。

30. 发明授权

US07666863B2 Benzofuran compounds, compositions and methods for treatment and prophylaxis of hepatitis C viral infections and associated diseases 失效
标题翻译：苯并呋喃化合物，用于治疗和预防丙型肝炎病毒感染和相关疾病的组合物和方法
公开(公告)号：US07666863B2
公开(公告)日：2010-02-23
申请号：US11753145
申请日：2007-05-24
申请人： Ashis K. Saha , Christopher J Burns , Alfred M. Del Vecchio , Thomas R. Bailey , Jason A. Reinhardt , Bheemashankar A. Kulkarni , Thomas H. Faitg , Hao Feng , Susan R. Rippin , Charles W. Blackledge , David J. Rys , Thomas A. Lessen , John Swestock , Yijun Deng , Theodore J. Nitz
发明人： Ashis K. Saha , Christopher J Burns , Alfred M. Del Vecchio , Thomas R. Bailey , Jason A. Reinhardt , Bheemashankar A. Kulkarni , Thomas H. Faitg , Hao Feng , Susan R. Rippin , Charles W. Blackledge , David J. Rys , Thomas A. Lessen , John Swestock , Yijun Deng , Theodore J. Nitz
IPC分类号： A61K31/54 , A61K31/53 , C07D307/00 , C07D401/00 , C07D417/00
CPC分类号： C07D405/04 , C07D307/84 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.
摘要翻译：本发明涉及苯并呋喃衍生物和类似物，以及含有它们的组合物及其用于治疗或预防与其相关的病毒感染和疾病的用途，特别是由丙型肝炎病毒引起的那些病毒感染和相关疾病。

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