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公开(公告)号:US5476944A
公开(公告)日:1995-12-19
申请号:US245780
申请日:1994-05-19
IPC分类号: C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07D213/40 , C07D307/18 , C07D307/20 , C07D493/04 , C07D213/02 , A61K31/38 , A61K31/44 , C07D335/02
CPC分类号: C07D213/40 , C07C323/17 , C07C323/20 , C07C323/22 , C07C323/52 , C07C323/60 , C07D307/18 , C07D307/20 , C07D493/04 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.
摘要翻译: 本发明涉及以下化学式的环状酚硫醚衍生物及其药学上可接受的盐,其为抑制剂或超氧化物产生的刺激剂,并且还可以将环氧合酶和/或5-脂氧合酶抑制于含有 这些化合物中的一种或多种与药学上可接受的载体组合,以及使用这些化合物的医疗治疗方法。
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公开(公告)号:US06617324B1
公开(公告)日:2003-09-09
申请号:US10114297
申请日:2002-04-02
申请人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号: A61K31496
CPC分类号: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要: A class of pyrazole derivatives described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译: 一类描述用于治疗p38激酶介导的病症的吡唑衍生物。 特别感兴趣的化合物由式IA定义,其中R1,R2,R3和R4如说明书中所述。
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公开(公告)号:US06956052B2
公开(公告)日:2005-10-18
申请号:US10247096
申请日:2002-09-19
申请人: Arija A. Bergmanis , Michael Clare , Joyce Z. Crich , Lifeng Geng , Timothy J. Hagen , Gunnar J. Hanson , Stephen C. Houdek , He Huang , Donna M. Iula , Francis J. Koszyk , Shuyuan Liao , Scott B. Mohler , Maria Nguyen , Richard A. Partis , Michael A. Stealey , Michael B. Tollefson , Richard M. Weier , Xiangdong Xu , Dominique Bonafoux , Theresa R. Fletcher , Bruce C. Hamper , Patrick J. Lennon , Subo Liao , Suzanne Metz , David S. Oburn , Thomas J. Owen , Angela M. Scates , Michael L. Vazquez , Serge G. Wolfson
发明人: Arija A. Bergmanis , Michael Clare , Joyce Z. Crich , Lifeng Geng , Timothy J. Hagen , Gunnar J. Hanson , Stephen C. Houdek , He Huang , Donna M. Iula , Francis J. Koszyk , Shuyuan Liao , Scott B. Mohler , Maria Nguyen , Richard A. Partis , Michael A. Stealey , Michael B. Tollefson , Richard M. Weier , Xiangdong Xu , Dominique Bonafoux , Theresa R. Fletcher , Bruce C. Hamper , Patrick J. Lennon , Subo Liao , Suzanne Metz , David S. Oburn , Thomas J. Owen , Angela M. Scates , Michael L. Vazquez , Serge G. Wolfson
IPC分类号: A61K31/416 , A61K31/4178 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P19/02 , A61P25/04 , A61P29/00 , A61P35/00 , C07D231/54 , C07D333/62 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
CPC分类号: C07D403/12 , C07D231/54 , C07D333/62 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
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公开(公告)号:US07220770B2
公开(公告)日:2007-05-22
申请号:US11183016
申请日:2005-07-15
申请人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
发明人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
IPC分类号: A61K31/44 , C07D213/53 , C07D401/04
CPC分类号: C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要: A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxy-carbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof
摘要翻译: 描述了一类咪唑基化合物用于治疗炎症。 特别感兴趣的化合物由式(V)定义,其中R 3是选自氢,烷基,卤代烷基,芳烷基,杂环烷基,杂芳烷基,酰基,氰基,烷氧基,烷硫基,烷硫基烷基,烷基磺酰基 环烷硫基,环烷硫基烷基,环烷基磺酰基,环烷基磺酰基烷基,卤代烷基磺酰基,芳基磺酰基,卤素,羟基烷基,烷氧基烷基,烷基羰基,芳基羰基,芳烷基羰基,杂环羰基,氰基烷基,氨基烷基,烷基氨基烷基,N-芳基氨基烷基,N-烷基-N-芳基氨基烷基,羧基烷基,烷氧基 - 烷氧基羰基,卤代烷基羰基,羧基,氨基羰基,烷基氨基羰基,烷基氨基羰基烷基,杂芳基烷氧基烷基,杂芳氧基烷基,杂芳硫基烷基,芳烷氧基,芳烷硫基,杂芳烷氧基,杂芳烷硫基,杂芳基烷硫基烷基,杂芳氧基,杂芳硫基,芳硫基烷基,芳氧基烷基,芳硫基,芳氧基,芳烷硫基烷基,芳烷氧基烷基,芳基和杂芳基。 其中R 4是选自氢,烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环,其中R 13和R 14是 任选地在可取代的位置被一个或多个独立地选自烷基磺酰基,氨基磺酰基,卤素,烷硫基,烷基,氰基,羧基,烷氧基羰基,卤代烷基,羟基,烷氧基,羟基烷基,烷氧基烷基,卤代烷氧基,氨基,烷基氨基,芳基氨基和硝基的基团取代。 只要R 13和R 14中的至少一个为被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐
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公开(公告)号:US07186743B2
公开(公告)日:2007-03-06
申请号:US11113926
申请日:2005-04-25
申请人: Arija A. Bergmanis , Michael Clare , Joyce Z. Crich , Lifeng Geng , Timothy J. Hagen , Gunnar J. Hanson , Stephen C. Houdek , He Huang , Donna M. Iula , Francis J. Koszyk , Shuyuan Liao , Scott B. Mohler , Maria Nguyen , Richard A. Partis , Michael A. Stealey , Michael B. Tollefson , Richard M. Weier , Xiangdong Xu , Dominique Bonafoux , Theresa R. Fletcher , Bruce C Hamper , Patrick J. Lennon , Subo Liao , Suzanne Metz , David S. Oburn , Thomas J. Owen , Angela M. Scates , Michael L. Vazquez , Serge G. Wolfson
发明人: Arija A. Bergmanis , Michael Clare , Joyce Z. Crich , Lifeng Geng , Timothy J. Hagen , Gunnar J. Hanson , Stephen C. Houdek , He Huang , Donna M. Iula , Francis J. Koszyk , Shuyuan Liao , Scott B. Mohler , Maria Nguyen , Richard A. Partis , Michael A. Stealey , Michael B. Tollefson , Richard M. Weier , Xiangdong Xu , Dominique Bonafoux , Theresa R. Fletcher , Bruce C Hamper , Patrick J. Lennon , Subo Liao , Suzanne Metz , David S. Oburn , Thomas J. Owen , Angela M. Scates , Michael L. Vazquez , Serge G. Wolfson
IPC分类号: A61K31/416 , A61K31/454 , A61K31/5395 , A61K31/429 , A61K31/433 , A61K31/506 , A61K31/496
CPC分类号: C07D403/12 , C07D231/54 , C07D333/62 , C07D401/12 , C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译: 本发明涉及取代的吡唑基衍生物,包含这些的组合物,中间体,制备取代的吡唑基衍生物的方法,以及用于治疗癌症,炎症和炎症相关疾病如关节炎的方法。
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公开(公告)号:US06514977B1
公开(公告)日:2003-02-04
申请号:US09196623
申请日:1998-11-20
申请人: Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu
发明人: Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu
IPC分类号: A61K31454
CPC分类号: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
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公开(公告)号:US07153959B2
公开(公告)日:2006-12-26
申请号:US10374781
申请日:2003-02-25
申请人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
发明人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
IPC分类号: C07D401/04 , C07D401/14 , C07D413/02
CPC分类号: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译: 描述了一类吡唑衍生物用于治疗p38激酶介导的病症。 特别感兴趣的化合物由式IA定义,其中R 1,R 2,R 3和R 4是 如说明书中所述。
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公开(公告)号:US07071198B1
公开(公告)日:2006-07-04
申请号:US10840734
申请日:2004-05-05
申请人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Ish K. Khanna , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , John Walker , Richard M. Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
发明人: Ashok S. Naraian , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Ish K. Khanna , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , John Walker , Richard M. Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
IPC分类号: A61K31/506 , A61K31/4439 , C07D401/04
CPC分类号: C07D401/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D473/00 , C07D487/04 , C07D491/10 , C07D495/04
摘要: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
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公开(公告)号:US06613789B2
公开(公告)日:2003-09-02
申请号:US10004944
申请日:2001-12-05
申请人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
发明人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk , Renee M. Huff
IPC分类号: A61K3144
CPC分类号: C07D233/64 , C07D233/32 , C07D233/90 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04
摘要: A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by Formula V: and pharmaceutically-acceptable salts thereof.
摘要翻译: 描述了一类咪唑基化合物用于治疗炎症。 特别感兴趣的化合物由式V定义:及其药学上可接受的盐。
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公开(公告)号:US06423713B1
公开(公告)日:2002-07-23
申请号:US09918481
申请日:2001-07-31
申请人: Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
发明人: Ashok Anantanarayan , Michael Clare , Paul W. Collins , Joyce Zuowu Crich , Rajesh Devraj , Daniel L. Flynn , Lifeng Geng , Matthew J. Graneto , Cathleen E. Hanau , Gunnar J. Hanson , Susan J. Hartmann , Michael Hepperle , He Huang , Francis J. Koszyk , Shuyuan Liao , Suzanne Metz , Richard A. Partis , Thao D. Perry , Shashidhar N. Rao , Shaun Raj Selness , Michael S. South , Michael A. Stealey , John Jeffrey Talley , Michael L. Vazquez , Richard M. Weier , Xiangdong Xi , Ish K. Khanna , Yi Yu
IPC分类号: A61K31496
CPC分类号: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
摘要: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R2, R3 and R4 are as described in the specification.
摘要翻译: 描述了一类吡唑衍生物用于治疗p38激酶介导的病症。 特别感兴趣的化合物由式IA定义,其中R1,R2,R3和R4如说明书中所述。
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