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公开(公告)号:US07601714B2
公开(公告)日:2009-10-13
申请号:US11175476
申请日:2005-07-06
申请人: Antonio J. M. Barbosa, Jr. , Steven Richard Brunette , Eugene Richard Hickey , Jin Mi Kim , Michael David Lawlor , René Marc Lemieux , Bryan McKibben , Matt Aaron Tschantz , Hui Yu
发明人: Antonio J. M. Barbosa, Jr. , Steven Richard Brunette , Eugene Richard Hickey , Jin Mi Kim , Michael David Lawlor , René Marc Lemieux , Bryan McKibben , Matt Aaron Tschantz , Hui Yu
IPC分类号: C07D239/48 , C07D403/12 , A61K31/505
CPC分类号: C07D239/48 , C07D401/12 , C07D403/12
摘要: Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译: 公开了式(I)的新化合物:其中X,Y,R 1,R 2和R 3如本文所定义,其可用作PKC-θ的抑制剂,因此可用于治疗介导的多种疾病和病症 通过PKC-θ的活性持续,包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物,使用这些化合物治疗各种疾病和病症的方法,制备这些化合物的方法和可用于这些方法的中间体。
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公开(公告)号:US20080318929A1
公开(公告)日:2008-12-25
申请号:US12158217
申请日:2006-12-12
申请人: Antonio J.M. Barbosa , Steven Richard Brunette , Eugene Richard Hickey , Michael David Lawlor , Matt Aaron Tschantz
发明人: Antonio J.M. Barbosa , Steven Richard Brunette , Eugene Richard Hickey , Michael David Lawlor , Matt Aaron Tschantz
IPC分类号: A61K31/506 , A61P37/00 , A61P29/00 , A61P3/10 , C07D239/50 , C07D401/12 , A61K31/5377 , A61K31/55 , C07D401/10 , C07D487/04 , C07D403/12 , A61K31/505
CPC分类号: C07D239/48 , C07D401/04 , C07D401/12 , C07D487/04
摘要: Disclosed are novel compounds of formula (I) wherein R1, R2, R3, and R4 and A are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译: 公开了式(I)的新化合物,其中R 1,R 2,R 3和R 4和A如本文所定义,其可用作PKC-θ的抑制剂,因此可用于治疗介导的多种疾病和病症 通过PKC-θ的活性持续,包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物,使用这些化合物治疗各种疾病和病症的方法,制备这些化合物的方法和可用于这些方法的中间体。
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3.
公开(公告)号:US08729114B2
公开(公告)日:2014-05-20
申请号:US13581829
申请日:2011-03-02
申请人: Michael J. Burke , Derek Cogan , Donghong Amy Gao , Alexander Heim-Riether , Eugene Richard Hickey , Matthew Russell Netherton , Philip Dean Ramsden , David Charles Thompson , Zhaoming Xiong
发明人: Michael J. Burke , Derek Cogan , Donghong Amy Gao , Alexander Heim-Riether , Eugene Richard Hickey , Matthew Russell Netherton , Philip Dean Ramsden , David Charles Thompson , Zhaoming Xiong
IPC分类号: A61K31/4164 , A61K31/4192 , C07D249/04 , C07D247/02 , C07D257/04
CPC分类号: C07D249/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
摘要翻译: 披露了可用于治疗自身免疫性疾病和其他疾病的式(I)的组织蛋白酶-S可逆抑制剂化合物。 还公开了含有该组合物的药物组合物及其制备和使用方法。
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4.
公开(公告)号:US20130158018A1
公开(公告)日:2013-06-20
申请号:US13581829
申请日:2011-03-02
申请人: Michael J. Burke , Derek Cogan , Donghong Amy Gao , Alexander Heim-Riether , Eugene Richard Hickey , Matthew Russell Netherton , Philip Dean Ramsden , David Charles Thompson , Zhaoming Xiong
发明人: Michael J. Burke , Derek Cogan , Donghong Amy Gao , Alexander Heim-Riether , Eugene Richard Hickey , Matthew Russell Netherton , Philip Dean Ramsden , David Charles Thompson , Zhaoming Xiong
IPC分类号: C07D249/04 , C07D401/06 , C07D409/14 , C07D513/04 , C07D417/06 , C07D471/04 , C07D487/04 , C07D409/12 , C07D403/04
CPC分类号: C07D249/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
摘要翻译: 披露了可用于治疗自身免疫性疾病和其他疾病的式(I)的组织蛋白酶-S可逆抑制剂化合物。 还公开了含有该组合物的药物组合物及其制备和使用方法。
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公开(公告)号:US20120142677A1
公开(公告)日:2012-06-07
申请号:US13141105
申请日:2009-12-15
申请人: Angela Berry , Rajashekhar Betageri , Eugene Richard Hickey , Someina Khok , Doris Riether , Lifen Wu , Renee M. Zindell
发明人: Angela Berry , Rajashekhar Betageri , Eugene Richard Hickey , Someina Khok , Doris Riether , Lifen Wu , Renee M. Zindell
IPC分类号: A61K31/4439 , C07D413/12 , A61K31/422 , C07D401/12 , C07D417/14 , A61K31/427 , A61K31/541 , A61K31/5377 , A61P11/00 , A61P29/00 , A61P37/00 , A61P19/00 , A61P37/08 , A61P7/00 , A61P17/00 , A61P13/12 , A61P1/16 , A61P1/00 , A61P25/28 , A61P27/16 , A61P11/02 , A61P11/04 , A61P27/02 , A61P25/00 , A61P35/00 , A61P5/00 , A61P37/06 , A61P1/06 , A61P9/10 , A61P9/04 , A61P43/00 , C07D413/14
CPC分类号: C07D417/12 , C07D207/16 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. (I)
摘要翻译: 公开了调节CB2受体的化合物。 根据本发明的化合物与CB2受体结合并且是激动剂,并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。 (一世)
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公开(公告)号:US08048899B2
公开(公告)日:2011-11-01
申请号:US12564132
申请日:2009-09-22
申请人: Alessandra Bartolozzi , Angela Berry , Eugene Richard Hickey , Markus Ostermeier , Doris Riether , Achim Sauer , David Smith Thomson , Lifen Wu , Renee M. Zindell , Patricia Amouzegh , Nigel James Blumire , Stephen Peter East , Monika Ermann , Someina Khor , Innocent Mushi
发明人: Alessandra Bartolozzi , Angela Berry , Eugene Richard Hickey , Markus Ostermeier , Doris Riether , Achim Sauer , David Smith Thomson , Lifen Wu , Renee M. Zindell , Patricia Amouzegh , Nigel James Blumire , Stephen Peter East , Monika Ermann , Someina Khor , Innocent Mushi
IPC分类号: A61K31/433 , A61K31/42 , A61K31/422 , A61K31/4196 , C07D285/135 , C07D413/12 , C07D261/14 , C07D249/16
CPC分类号: C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要: are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译: 被披露。 根据本发明的化合物结合并且是CB 2受体的激动剂,拮抗剂或反向激动剂,并且可用于治疗炎症。 作为激动剂的那些化合物另外可用于治疗疼痛。
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公开(公告)号:US20110190256A1
公开(公告)日:2011-08-04
申请号:US12867970
申请日:2009-02-19
申请人: Pier Francesco Cirillo , Eugene Richard Hickey , Doris Riether , Monika Ermann , Innocent Mushi
发明人: Pier Francesco Cirillo , Eugene Richard Hickey , Doris Riether , Monika Ermann , Innocent Mushi
IPC分类号: A61K31/397 , C07D413/12 , A61K31/422 , C07D403/12 , A61K31/4196 , C07D401/12 , A61K31/4439 , C07D413/10 , A61K31/5377 , C07D417/12 , A61K31/541 , A61K31/454 , C07D213/72 , A61K31/44 , A61K31/4545 , A61P29/00 , A61P11/00 , A61P9/00 , A61P19/02 , A61P13/12 , A61P1/00 , A61P5/00 , A61P7/00 , A61P17/00 , A61P37/08 , A61P35/00
CPC分类号: C07D261/16 , C07D213/75 , C07D405/12 , C07D413/12
摘要: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
摘要翻译: 公开了调节CB2受体的化合物。 该化合物可用于治疗CB2受体介导的疾病如疼痛。
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公开(公告)号:US20080161297A1
公开(公告)日:2008-07-03
申请号:US11856740
申请日:2007-09-18
申请人: Todd Bosanac , John David Ginn , Eugene Richard Hickey , Thomas Martin Kirrane , Weimin Liu , Anthony S. Prokopowicz , Sabine K. Schlyer , Cheng-Kon Shih , Roger John Snow , Michael Robert Turner , Frank Wu , Erick Richard Young
发明人: Todd Bosanac , John David Ginn , Eugene Richard Hickey , Thomas Martin Kirrane , Weimin Liu , Anthony S. Prokopowicz , Sabine K. Schlyer , Cheng-Kon Shih , Roger John Snow , Michael Robert Turner , Frank Wu , Erick Richard Young
IPC分类号: A61K31/4725 , A61P9/00 , A61P13/00 , A61P15/10 , A61P27/06 , A61P11/06 , A61K31/517 , A61K31/5377 , A61K31/496 , C07D239/88 , C07D217/24 , C07D401/02 , C07D417/02 , A61K31/541 , A61K31/472
CPC分类号: A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , C07D217/24 , C07D239/88 , C07D239/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D487/08
摘要: Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
摘要翻译: 公开了用作Rho激酶抑制剂的新型取代的2H-异喹啉-1-酮和3H-喹唑啉-4-酮衍生物,并用于治疗通过Rho激酶(包括心血管疾病)的活性介导或维持的多种疾病和病症 包含这些化合物的药物组合物,使用这些化合物的方法和制备这些化合物的方法。
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公开(公告)号:US07291733B2
公开(公告)日:2007-11-06
申请号:US10960550
申请日:2004-10-07
申请人: Charles Lawrence Cywin , Roman Wolfgang Fleck , Eugene Richard Hickey , Weimin Liu , Tina Marie Morwick , John Robert Proudfoot , Denice M. Spero
发明人: Charles Lawrence Cywin , Roman Wolfgang Fleck , Eugene Richard Hickey , Weimin Liu , Tina Marie Morwick , John Robert Proudfoot , Denice M. Spero
IPC分类号: C07D491/00 , C07D498/00 , C07D513/00 , C07D515/00
CPC分类号: C07D495/14
摘要: Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds
摘要翻译: 公开了以下所示的式(I),(II)和(III)的取代的三环杂环化合物,其中R 1,R 2,R 3, 本文描述了它们作为抗炎剂是有活性的。 还公开了使用和制备这些化合物的方法
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公开(公告)号:US08362039B2
公开(公告)日:2013-01-29
申请号:US13217480
申请日:2011-08-25
申请人: Alessandra Bartolozzi , Angela Berry , Eugene Richard Hickey , Markus Ostermeier , Doris Riether , Achim Sauer , David Smith Thomson , Lifen Wu , Renee M. Zindell , Patricia Amouzegh , Nigel James Blumire , Stephen Peter East , Monika Ermann , Someina Khor , Innocent Mushi
发明人: Alessandra Bartolozzi , Angela Berry , Eugene Richard Hickey , Markus Ostermeier , Doris Riether , Achim Sauer , David Smith Thomson , Lifen Wu , Renee M. Zindell , Patricia Amouzegh , Nigel James Blumire , Stephen Peter East , Monika Ermann , Someina Khor , Innocent Mushi
IPC分类号: A61K31/4525 , A61K31/4196 , A61K31/422 , A61K31/433
CPC分类号: C07D413/12 , C07D249/14 , C07D261/14 , C07D405/12 , C07D413/04 , C07D413/14
摘要: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
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