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公开(公告)号:US20060211694A1
公开(公告)日:2006-09-21
申请号:US11226556
申请日:2005-09-14
Applicant: Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
Inventor: Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
IPC: A61K31/53 , A61K31/506 , A61K31/498 , A61K31/497 , A61K31/501 , A61K31/4439 , A61K31/4747 , A61K31/4709 , A61K31/4412
CPC classification number: C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Abstract translation: 公开了式I化合物及其药学上可接受的盐,其中R 1,R 2,R 3,R 4, >和R 5>在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物,制备化合物的方法和使用该化合物的治疗方法。
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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
Applicant: 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
Inventor: 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: A61K31/506 , A61K31/4439 , C07D401/04
CPC classification number: 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
Abstract: 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:US07067540B2
公开(公告)日:2006-06-27
申请号:US10367987
申请日:2003-02-14
Applicant: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
Inventor: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
IPC: A61K31/44 , C07D213/02 , C07D401/02
CPC classification number: C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Abstract translation: 公开了式I化合物及其药学上可接受的盐,其中R 1,R 2,R 3,R 4, >和R 5>在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物,制备化合物的方法和使用该化合物的治疗方法。
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公开(公告)号:US20050176775A1
公开(公告)日:2005-08-11
申请号:US10918826
申请日:2004-08-13
Applicant: Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marrufo , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
Inventor: Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marrufo , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
IPC: A61K20060101 , A61K31/4412 , A61K31/4415 , A61K31/4439 , A61P29/00 , C07D211/86 , C07D213/64 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/84 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D417/04 , C07D41/02
CPC classification number: C07D213/69 , C04B35/632 , C07D213/64 , C07D213/70 , C07D213/73 , C07D213/80 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D417/04
Abstract: Disclosed are compounds of Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Abstract translation: 公开了式I的化合物及其药学上可接受的盐,其中R 1,R 2,R 3,R 4, SUB>和R 5>在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物,制备化合物的方法和使用该化合物的治疗方法。
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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
Applicant: 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
Inventor: 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: A61K31496
CPC classification number: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
Abstract: 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.
Abstract translation: 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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公开(公告)号:US07786097B2
公开(公告)日:2010-08-31
申请号:US12506825
申请日:2009-07-21
Applicant: Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber
Inventor: Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber
IPC: A61K31/675 , A61K31/44
CPC classification number: C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886
Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
Abstract translation: 本发明涉及式I化合物或其盐,它们是糖皮质激素受体的调节剂。 本发明的化合物和盐可用于治疗由糖皮质激素受体活性介导的病症。
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公开(公告)号:US07629363B2
公开(公告)日:2009-12-08
申请号:US11226556
申请日:2005-09-14
Applicant: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
Inventor: Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
IPC: A61K31/44 , C07D211/02
CPC classification number: C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3/R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Abstract translation: 公开了式I化合物及其药学上可接受的盐,其中R 1,R 2,R 3 / R 4和R 5在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物,制备化合物的方法和使用该化合物的治疗方法。
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公开(公告)号:US20080188443A1
公开(公告)日:2008-08-07
申请号:US12023362
申请日:2008-01-31
Applicant: Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber
Inventor: Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber
IPC: A61K31/675 , C07D213/72 , A61K31/44 , A61P1/00 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P11/06 , C07K14/72 , C07F9/09
CPC classification number: C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886
Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
Abstract translation: 本发明涉及式I化合物或其盐,它们是糖皮质激素受体的调节剂。 本发明的化合物和盐可用于治疗由糖皮质激素受体活性介导的病症。
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公开(公告)号:US20050256122A1
公开(公告)日:2005-11-17
申请号:US11069471
申请日:2005-03-01
Applicant: Michael Hepperle , Kevin Jerome , John Walker , Shaun Selness , Rajesh Devraj
Inventor: Michael Hepperle , Kevin Jerome , John Walker , Shaun Selness , Rajesh Devraj
IPC: C07D237/14 , A61K31/50 , A61K31/501 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/16 , A61P31/18 , A61P31/22 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P39/02 , A61P43/00 , C07D237/16 , C07D237/18 , C07D237/22 , C07D401/04 , C07D401/06 , C07D405/12 , C07D417/06
CPC classification number: C07D401/04 , C07D237/16 , C07D237/18 , C07D237/22 , C07D401/06 , C07D405/12 , C07D417/06
Abstract: Disclosed are substituted pyridazinones that are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical composition containing the pyridazinone compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
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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
Applicant: 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
Inventor: 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: A61K31496
CPC classification number: C07D409/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D471/04 , C07D473/00 , C07D487/04
Abstract: 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.
Abstract translation: 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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