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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
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 Xu , 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 Xu , Ish K. Khanna , Yi Yu
IPC: A61K31454
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.
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公开(公告)号:US06362218B1
公开(公告)日:2002-03-26
申请号:US09581773
申请日:2000-06-16
Applicant: Mark S. Cushman , Ankush B. Argade , Rudiger D. Haugwitz , Rajesh Devraj
Inventor: Mark S. Cushman , Ankush B. Argade , Rudiger D. Haugwitz , Rajesh Devraj
IPC: A61K31365
CPC classification number: C07D315/00
Abstract: Cytotoxic Michael addition derivatives of brefeldin A are described. Oxidation of thiol addition products of brefeldin A provides the corresponding sulfoxides and sulfones. The sulfoxides exhibited more cytotoxic activity than the corresponding sulfides and sulfones in a variety of human cancer cell lines. Pharmaceutical formulations of the disclosed cytotoxic derivatives are also described.
Abstract translation: 描述了布雷菲德菌素A的细胞毒性迈克尔加成衍生物。 布雷菲尔德A的硫醇加成产物的氧化提供相应的亚砜和砜。 亚砜在各种人类癌细胞系中表现出比相应的硫化物和砜更多的细胞毒性活性。 还描述了所公开的细胞毒性衍生物的药物制剂。
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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
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 Xu , Ish K. Khanna , Yi Yu , Win Naing , John Walker , Syaulan Yang
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 Xu , Ish K. Khanna , Yi Yu , Win Naing , John Walker , Syaulan Yang
IPC: A61K31/496 , A61K31/501 , A61K31/5355 , C07D211/06 , C07D413/04
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.
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
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 Xu , 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 Xu , Ish K. Khanna , Yi Yu
IPC: A61K31506
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, R 2, 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:US20090281148A1
公开(公告)日:2009-11-12
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 , Ronald Keith Webber
Inventor: Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Ronald Keith Webber
IPC: 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:US07598231B2
公开(公告)日:2009-10-06
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 , C07F9/58
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:US20050020594A1
公开(公告)日:2005-01-27
申请号:US10893073
申请日:2004-07-16
Applicant: Michael Hepperle , Kevin Jerome , John Walker , Shaun Selness , Rajesh Devraj
Inventor: Michael Hepperle , Kevin Jerome , John Walker , Shaun Selness , Rajesh Devraj
IPC: A61K31/501 , C07D237/14 , C07D237/16 , C07D237/18 , C07D237/22 , C07D405/12 , C07
CPC classification number: C07D405/12 , C07D237/14 , C07D237/16 , C07D237/18 , C07D237/22
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.
Abstract translation: 公开了可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加剧的疾病和病症的取代哒嗪酮。 还公开了含有哒嗪酮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:US20070088033A1
公开(公告)日:2007-04-19
申请号:US11531492
申请日:2006-09-13
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 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 , A61K31/497 , A61K31/4439 , A61K31/4545 , A61K31/4709 , C07D417/02 , C07D403/02 , 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:US20070078146A1
公开(公告)日:2007-04-05
申请号:US10840734
申请日:2004-05-05
Applicant: 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
Inventor: 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: A61K31/506 , A61K31/4439 , C07D43/02
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 medicated 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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公开(公告)号:US07153959B2
公开(公告)日:2006-12-26
申请号:US10374781
申请日:2003-02-25
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 Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
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 Xu , Ish K. Khanna , Yi Yu , Win Naing , Syaulan Yang
IPC: C07D401/04 , C07D401/14 , C07D413/02
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R 1,R 2,R 3和R 4是 如说明书中所述。
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