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公开(公告)号:US20110118245A1
公开(公告)日:2011-05-19
申请号:US12933402
申请日:2009-03-17
申请人: Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人: Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号: A61K31/517 , C07D413/12 , C07D491/056 , A61K31/519 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , C07D403/12 , C07D239/88 , C07D401/12 , A61P19/10 , A61P29/00 , A61P3/10 , A61P1/00 , A61P19/02 , A61P37/00 , A61P35/04
CPC分类号: C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译: 提供根据式(I)的化合物,组合物和方法用于调节RAF激酶(包括BRAF激酶)的活性,并用于治疗,预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式(I):或其药学上可接受的盐,溶剂合物,其水合物的包合物,其中X为O或S(O)t; Ra是O或S.
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公开(公告)号:US08618289B2
公开(公告)日:2013-12-31
申请号:US12933402
申请日:2009-03-17
申请人: Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人: Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号: C07D239/70 , A01N43/54
CPC分类号: C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译: 提供根据式(I)的化合物,组合物和方法用于调节RAF激酶(包括BRAF激酶)的活性,并用于治疗,预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。 式(I):或其药学上可接受的盐,溶剂合物,其水合物的包合物,其中X为O或S(O)t; Ra是O或S.
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公开(公告)号:US07910561B2
公开(公告)日:2011-03-22
申请号:US11792121
申请日:2005-12-09
申请人: Jeannie M. Arruda , Brian T. Campbell , Nicholas D. P. Cosford , Jacob M. Hoffman , Essa H. Hu , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Tony Siu , Brian A. Stearns , Lida R. Tehrani , Mark T. Bilodeau , Peter J. Manley
发明人: Jeannie M. Arruda , Brian T. Campbell , Nicholas D. P. Cosford , Jacob M. Hoffman , Essa H. Hu , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Tony Siu , Brian A. Stearns , Lida R. Tehrani , Mark T. Bilodeau , Peter J. Manley
IPC分类号: A01N43/04 , A01N43/58 , A01N43/42 , A61K31/541 , A61K31/70 , A61K31/50 , A61K31/495 , A61K31/52 , C09B25/00 , C07D487/00 , C07D491/00 , C07H15/00
CPC分类号: C07D471/04
摘要: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
摘要翻译: 本发明涉及含有抑制Akt(丝氨酸/苏氨酸蛋白激酶)活性的取代萘啶的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法,包括施用本发明化合物。 与PCT公开WO2003 / 086394中报道的其它萘啶类相比,这些取代的萘啶具有意想不到的有利性质,这种意想不到的有利性质可包括增加的细胞效力/溶解度,更大的选择性,增强的药物动力学性质,缺乏目标活性等。
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公开(公告)号:US20080287457A1
公开(公告)日:2008-11-20
申请号:US11792121
申请日:2005-12-09
申请人: Jeannie M. Arruda , Brian T. Campbell , Nicholas D.P. Cosford , Jacob M. Hoffman , Essa H. Hu , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Tony Siu , Brian A. Stearns , Lida R. Tehrani , Mark T. Bilodeau , Peter J. Manley
发明人: Jeannie M. Arruda , Brian T. Campbell , Nicholas D.P. Cosford , Jacob M. Hoffman , Essa H. Hu , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Tony Siu , Brian A. Stearns , Lida R. Tehrani , Mark T. Bilodeau , Peter J. Manley
IPC分类号: A61K31/496 , C07D487/04 , A61P35/04 , A61K31/4375
CPC分类号: C07D471/04
摘要: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
摘要翻译: 本发明涉及含有抑制Akt(丝氨酸/苏氨酸蛋白激酶)活性的取代萘啶的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法,包括施用本发明化合物。 与PCT公开WO2003 / 086394中报道的其它萘啶类相比,这些取代的萘啶具有意想不到的有利性质,这种意想不到的有利性质可包括增加的细胞效力/溶解度,更大的选择性,增强的药物动力学性质,缺乏目标活性等。
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公开(公告)号:US07087601B2
公开(公告)日:2006-08-08
申请号:US10497452
申请日:2002-11-26
申请人: Jeannie Arruda , Celine Bonnefous , Brian T. Campbell , Rowena V. Cube , Benito Munoz , Brian Stearns , Jean-Michel Vernier , Bowei Wang , Xiumin Zhao
发明人: Jeannie Arruda , Celine Bonnefous , Brian T. Campbell , Rowena V. Cube , Benito Munoz , Brian Stearns , Jean-Michel Vernier , Bowei Wang , Xiumin Zhao
IPC分类号: A61K31/5383 , A61K31/437 , C07D413/14 , C07D491/048
CPC分类号: C07D263/57 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/10
摘要: Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.
摘要翻译: 苯基化合物在1-位上被一个稠合的双环自由基组成,它由与六元碳环稠合的五元杂环,六元芳基或六元杂芳基形成,并进一步任选地被取代在3位上 ,4个位置是mGluR5调节剂,可用于治疗精神病和情绪障碍,例如精神分裂症,焦虑,抑郁和恐慌,以及治疗疼痛和其他疾病。
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