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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: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:US06979686B1
公开(公告)日:2005-12-27
申请号:US10021780
申请日:2001-12-07
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 , John Walker , 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 , John Walker , Syaulan Yang
IPC分类号: A61K31/496 , A61K31/501 , A61K31/5355 , C07D211/06 , C07D413/04
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.
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, SUP>如说明书中所述。
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公开(公告)号:US06525059B1
公开(公告)日:2003-02-25
申请号:US09513351
申请日:2000-02-24
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: A61K31506
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, R 2, 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如说明书中所述。
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8.1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation 失效
标题翻译: 用于治疗炎症的1,2-芳基和杂芳基取代的咪唑基化合物公开(公告)号:US5616601A
公开(公告)日:1997-04-01
申请号:US464154
申请日:1995-06-05
申请人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk
发明人: Ish K. Khanna , Richard M. Weier , Paul W. Collins , Yi Yu , Xiangdong Xu , Richard A. Partis , Francis J. Koszyk
IPC分类号: C07D233/30 , A61K31/415 , A61K31/4166 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P25/04 , A61P29/00 , A61P43/00 , C07D233/32 , C07D233/54 , C07D233/64 , C07D233/90 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D409/04 , C07D419/04 , C07D213/53
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 and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 -R.sup.6 are as described in the specification; 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和炎症相关疾病。 特别感兴趣的化合物由式I定义:其中R 1 -R 6如说明书中所述; 或其药学上可接受的盐。
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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: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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