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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:US07750151B2
公开(公告)日:2010-07-06
申请号:US11547113
申请日:2005-04-05
申请人: Mark T. Bilodeau , Chixu Chen , Nicholas D. P. Cosford , Brian W. Eastman , John C. Hartnett , Essa H. Hu , Peter J. Manley , Lou Anne Neilson , Lida R. Tehrani , Zhicai Wu
发明人: Mark T. Bilodeau , Chixu Chen , Nicholas D. P. Cosford , Brian W. Eastman , John C. Hartnett , Essa H. Hu , Peter J. Manley , Lou Anne Neilson , Lida R. Tehrani , Zhicai Wu
IPC分类号: C07D471/04 , C07D413/12 , C07D521/00 , C07D401/14 , C07D487/08 , A61P35/00
CPC分类号: C07D471/04 , C07D519/00
摘要: The present invention is directed to compounds which contain substituted napthyridines 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.
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。
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公开(公告)号:US07544677B2
公开(公告)日:2009-06-09
申请号:US11659606
申请日:2005-08-19
申请人: Mark T. Bilodeau , Nicholas D. P. Cosford , John C. Hartnett , Yiwei Li , Jun Liang , Peter J. Manley , Lou Anne Neilson , Tony Siu , Zhicai Wu
发明人: Mark T. Bilodeau , Nicholas D. P. Cosford , John C. Hartnett , Yiwei Li , Jun Liang , Peter J. Manley , Lou Anne Neilson , Tony Siu , Zhicai Wu
IPC分类号: A61K31/541 , A61K31/5355 , A61K31/519 , C07D471/04 , C07D519/00 , A61P35/00
CPC分类号: C07D471/04
摘要: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties 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.
摘要翻译: 本发明涉及含有抑制Akt(丝氨酸/苏氨酸蛋白激酶)活性的取代的5-取代哌啶部分的化合物。 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。
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公开(公告)号:US20080280899A1
公开(公告)日:2008-11-13
申请号:US11547113
申请日:2005-04-05
申请人: Mark T. Bilodeau , Chixu Chen , Nicholas D.P. Cosford , Brian W. Eastman , John C. Hartnett , Essa H. Hu , Peter J. Manley , Lou Anne Neilson , Lida R. Tehrani , Zhicai Wu
发明人: Mark T. Bilodeau , Chixu Chen , Nicholas D.P. Cosford , Brian W. Eastman , John C. Hartnett , Essa H. Hu , Peter J. Manley , Lou Anne Neilson , Lida R. Tehrani , Zhicai Wu
IPC分类号: A61K31/519 , C07D471/04 , A61K31/4375 , A61P35/00 , A61K31/5377 , C07D413/12
CPC分类号: C07D471/04 , C07D519/00
摘要: The present invention is directed to compounds which contain substituted napthyridines 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.
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。
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公开(公告)号:US07115597B2
公开(公告)日:2006-10-03
申请号:US10677687
申请日:2003-10-02
申请人: Mark T. Bilodeau , George D. Hartman , Jacob M. Hoffman, Jr. , John T. Sisko , Peter J. Manley , Anthony M. Smith , Thomas J. Tucker , William C. Lumma, Jr. , Leonard Rodman
发明人: Mark T. Bilodeau , George D. Hartman , Jacob M. Hoffman, Jr. , John T. Sisko , Peter J. Manley , Anthony M. Smith , Thomas J. Tucker , William C. Lumma, Jr. , Leonard Rodman
IPC分类号: C07D417/12 , A61K31/427 , C07D241/04
CPC分类号: C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08
摘要: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号:US08389720B2
公开(公告)日:2013-03-05
申请号:US13127898
申请日:2009-11-03
申请人: James C. Barrow , Mark T. Bilodeau , Christopher D. Cox , John C. Hartnett , Nathan R. Kett , Yiwei Li , Peter J. Manley , Jeffrey Melamed , William D. Shipe , B. Wesley Trotter , Amy Zartman
发明人: James C. Barrow , Mark T. Bilodeau , Christopher D. Cox , John C. Hartnett , Nathan R. Kett , Yiwei Li , Peter J. Manley , Jeffrey Melamed , William D. Shipe , B. Wesley Trotter , Amy Zartman
IPC分类号: A61K31/551 , A61K31/5355 , A61K31/497 , A61K31/519 , A61K31/4412 , A61K31/4704 , C07D243/08 , C07D413/14 , C07D471/04 , C07D401/14 , C07D401/12 , C07D405/14
CPC分类号: A61K31/47 , C07D401/12 , C07D405/12
摘要: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
摘要翻译: 本发明涉及作为神经肽S受体的拮抗剂的喹诺酮化合物,其可用于治疗或预防神经和精神疾病以及涉及神经肽S受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及神经肽S受体的疾病中的用途。
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公开(公告)号:US20110212946A1
公开(公告)日:2011-09-01
申请号:US13127898
申请日:2009-11-03
申请人: James C. Barrow , Mark T. Bilodeau , Christopher D. Cox , John C. Hartnett , Nathan R. Kett , Yiwei Li , Peter J. Manley , Jeffrey Melamed , William D. Shipe , B. Wesley Trotter , Amy Zartman
发明人: James C. Barrow , Mark T. Bilodeau , Christopher D. Cox , John C. Hartnett , Nathan R. Kett , Yiwei Li , Peter J. Manley , Jeffrey Melamed , William D. Shipe , B. Wesley Trotter , Amy Zartman
IPC分类号: A61K31/4704 , C07D405/14 , A61K31/496 , A61K31/55 , C07D401/12 , A61K31/4709 , C07D413/12 , A61K31/5377 , C07D215/227 , A61P25/00
CPC分类号: A61K31/47 , C07D401/12 , C07D405/12
摘要: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
摘要翻译: 本发明涉及作为神经肽S受体的拮抗剂的喹诺酮化合物,其可用于治疗或预防神经和精神疾病以及涉及神经肽S受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及神经肽S受体的疾病中的用途。
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公开(公告)号:US06586423B2
公开(公告)日:2003-07-01
申请号:US10061817
申请日:2002-02-01
IPC分类号: C07D41312
CPC分类号: C07D417/12 , C07D417/14
摘要: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号:US07879839B2
公开(公告)日:2011-02-01
申请号:US11658114
申请日:2005-07-27
申请人: Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
发明人: Christopher J. Dinsmore , Jeffrey M. Bergman , Douglas C. Beshore , B. Wesley Trotter , Kausik K. Nanda , Richard Isaacs , Linda S. Payne , Lou Anne Neilson , Zhicai Wu , Mark T. Bilodeau , Peter J. Manley , Adrienne E. Balitza
IPC分类号: C07D401/14 , A61K31/438
CPC分类号: C07D213/36 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/40 , C07D213/42 , C07D213/55 , C07D213/56 , C07D213/64 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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