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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: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: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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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:US07211597B2
公开(公告)日:2007-05-01
申请号:US10247028
申请日:2002-09-19
申请人: Suzanne Metz , Michael Clare , Joyce Z. Crich , Timothy J. Hagen , Gunnar J. Hanson , He Huang , Stephen C. Houdek , Michael A. Stealey , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu
发明人: Suzanne Metz , Michael Clare , Joyce Z. Crich , Timothy J. Hagen , Gunnar J. Hanson , He Huang , Stephen C. Houdek , Michael A. Stealey , Michael L. Vazquez , Richard M. Weier , Xiangdong Xu
IPC分类号: C07D491/052 , C07D471/04 , A61K31/4162 , A61K31/437 , A61K29/00
CPC分类号: C07D231/56 , C07D471/04 , C07D491/04 , C07D495/04 , C07D495/14
摘要: The present invention relates to compounds of Formula I: wherein A is (CH2)m-Q-(CH2)n, wherein each CH2 may be independently substituted with one or more substitution selected from the group consisting of: hydroxy, halo, alkoxy, lower alkyl, amino, aminoalkyl, alkylamino, alkenyl, and alkynyl; B is a 5 or 6 membered heteroaryl, or aryl, optionally saturated, or optionally substituted with R1, R2, or R12; X is selected from the group consisting of: N and C; and Y and Z are independently selected from the group consisting of: N, C, CH, CR3, S, and O; compositions comprising such compounds, intermediates thereof, methods of making such compounds, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.
摘要翻译: 本发明涉及式I的化合物:其中A是(CH 2)2 - (CH 2 CH 2)n 其中每个CH 2可以独立地被一个或多个选自以下的取代基取代:羟基,卤素,烷氧基,低级烷基,氨基,氨基烷基,烷基氨基,烯基和 炔基; B是任选被饱和或任选被R 1,R 2或R 12取代的5或6元杂芳基或芳基; X选自:N和C; 且Y和Z独立地选自:N,C,CH,CR 3,S和O; 包含这些化合物的组合物,其中间体,制备此类化合物的方法,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:US20050256180A1
公开(公告)日:2005-11-17
申请号:US11113926
申请日:2005-04-25
申请人: Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge Wolfson
发明人: Arija Bergmanis , Michael Clare , Joyce Crich , Lifeng Geng , Timothy Hagen , Gunnar Hanson , Stephen Houdek , He Huang , Donna Iula , Francis Koszyk , Shuyuan Liao , Scott Mohler , Maria Nguyen , Richard Partis , Michael Stealey , Michael Tollefson , Richard Weier , Xiangdong Xu , Dominique Bonafoux , Theresa Fletcher , Bruce Hamper , Patrick Lennon , Subo Liao , Suzanne Metz , David Oburn , Thomas Owen , Angela Scates , Michael Vazquez , Serge 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 , A61K31/4162
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:US20070078146A1
公开(公告)日:2007-04-05
申请号:US10840734
申请日:2004-05-05
申请人: Ashok Naraian , Michael Clare , Paul Collins , Joyce Crich , Rajesh Devraj , Daniel Flynn , Lifeng Geng , Matthew Graneto , Cathleen Hanau , Gunnar Hanson , Susan Hartmann , Michael Hepperle , He Huang , Ish Khanna , Francis Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard Partis , Thao Perry , Shashidhar Rao , Shaun Selness , Michael South , Michael Stealey , John Talley , Michael Vazquez , John Walker , Richard Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
发明人: Ashok Naraian , Michael Clare , Paul Collins , Joyce Crich , Rajesh Devraj , Daniel Flynn , Lifeng Geng , Matthew Graneto , Cathleen Hanau , Gunnar Hanson , Susan Hartmann , Michael Hepperle , He Huang , Ish Khanna , Francis Koszyk , Shuyuan Liao , Suzanne Metz , Win Naing , Richard Partis , Thao Perry , Shashidhar Rao , Shaun Selness , Michael South , Michael Stealey , John Talley , Michael Vazquez , John Walker , Richard Weier , Xiangdong Xu , Syaulan Yang , Yi Yu
IPC分类号: A61K31/506 , A61K31/4439 , C07D43/02
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 medicated 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激酶药物障碍。 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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