专利检索 ap:("Hengmiao (Henry) Cheng" OR "Rajesh Devraj" OR "Gary A Decresenzo" OR "Xiao Hu" OR "Kevin D. Jerome" OR "Mark Obukowicz" OR "Lisa Olson" OR "Paul V. Rucker" OR "Ronald Keith Webber") AND inv:"Rajesh Devraj" 第 1 页

1.

发明授权
Tricyclic compound, compositions, and methods 有权
标题翻译：三环化合物，组合物和方法

公开(公告)号：US07598231B2

公开(公告)日：2009-10-06

申请号：US12023362

申请日：2008-01-31

申请人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

发明人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

IPC分类号： A61K31/675 , C07F9/58

CPC分类号： C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886

摘要： 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.

摘要翻译： 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。

2.

发明授权
Tricyclic compounds, compositions and methods 有权
标题翻译：三环化合物，组合物和方法

公开(公告)号：US07786097B2

公开(公告)日：2010-08-31

申请号：US12506825

申请日：2009-07-21

申请人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

发明人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

IPC分类号： A61K31/675 , A61K31/44

CPC分类号： C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886

摘要： 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.

摘要翻译： 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。

3.

发明申请
Tricyclic Compound, Compositions, and Methods 有权
标题翻译：三环化合物，组合物和方法

公开(公告)号：US20080188443A1

公开(公告)日：2008-08-07

申请号：US12023362

申请日：2008-01-31

申请人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

发明人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. DeCresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Paul V. Rucker , Ronald Keith Webber

IPC分类号： A61K31/675 , C07D213/72 , A61K31/44 , A61P1/00 , A61P17/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P11/06 , C07K14/72 , C07F9/09

CPC分类号： C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886

摘要： 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.

摘要翻译： 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。

4.

发明申请
TRICYCLIC COMPOUNDS, COMPOSITIONS AND METHODS 有权
标题翻译：三元化合物，组合物和方法

公开(公告)号：US20090281148A1

公开(公告)日：2009-11-12

申请号：US12506825

申请日：2009-07-21

申请人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Ronald Keith Webber

发明人： Hengmiao (Henry) Cheng , Rajesh Devraj , Gary A. Decresenzo , Xiao Hu , Kevin D. Jerome , Mark Obukowicz , Lisa Olson , Ronald Keith Webber

IPC分类号： A61K31/44

CPC分类号： C07D213/89 , A61K31/44 , C07D213/72 , C07F9/58 , Y10S514/886

摘要： 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.

摘要翻译： 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。

5.

发明授权
Diaryl substituted pyridinones 失效
标题翻译：二芳基取代的吡啶酮

公开(公告)号：US07629363B2

公开(公告)日：2009-12-08

申请号：US11226556

申请日：2005-09-14

申请人： 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

发明人： 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分类号： A61K31/44 , C07D211/02

CPC分类号： 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

摘要： 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.

摘要翻译： 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。

6.

发明授权
Substituted pyridinones 有权
标题翻译：取代的吡啶酮

公开(公告)号：US07067540B2

公开(公告)日：2006-06-27

申请号：US10367987

申请日：2003-02-14

申请人： 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

发明人： 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分类号： A61K31/44 , C07D213/02 , C07D401/02

CPC分类号： 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

摘要： 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.

摘要翻译： 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＆gt;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。

7.

发明授权
Substituted pyrazoles as p38 kinase inhibitors 失效

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.

8.

发明授权
Brefeldin A derivatives 失效
标题翻译： Brefeldin A衍生物

公开(公告)号：US06362218B1

公开(公告)日：2002-03-26

申请号：US09581773

申请日：2000-06-16

申请人： Mark S. Cushman , Ankush B. Argade , Rudiger D. Haugwitz , Rajesh Devraj

发明人： Mark S. Cushman , Ankush B. Argade , Rudiger D. Haugwitz , Rajesh Devraj

IPC分类号： A61K31365

CPC分类号： C07D315/00

摘要： 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.

摘要翻译： 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。