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公开(公告)号：US08697685B2
公开(公告)日：2014-04-15
申请号：US13130368
申请日：2009-11-18
申请人： Jeffrey Michael Axten , Charles William Blackledge, Jr. , Gerald Patrick Brady, Jr. , Yanhong Feng , Seth W. Grant , Jesus Raul Medina , William H. Miller , Stuart P. Romeril
发明人： Jeffrey Michael Axten , Charles William Blackledge, Jr. , Gerald Patrick Brady, Jr. , Yanhong Feng , Seth W. Grant , Jesus Raul Medina , William H. Miller , Stuart P. Romeril
IPC分类号： A61K31/33 , A61K31/54 , A61K31/505 , A61K31/55 , C07D401/08 , C07D417/02 , C07D413/06 , C07D239/02
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要： The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明涉及6-（4-嘧啶基）-1H-吲唑衍生物。 具体地，本发明涉及式（I）的化合物，其中R 1 -R 4在本文中定义。 本发明的化合物可以用于治疗由组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）特征的免疫和代谢疾病和病症的治疗。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号：US07982053B2
公开(公告)日：2011-07-19
申请号：US11996994
申请日：2006-07-28
IPC分类号： C07D207/00 , C07D295/00 , C07D207/06
CPC分类号： C07D207/16 , A61K38/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D491/056
摘要： Novel PDF inhibitors and novel methods for their use are provided.
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公开(公告)号：US20100081650A1
公开(公告)日：2010-04-01
申请号：US12620129
申请日：2009-11-17
申请人： Jeffrey Michael Axten , Robert A. Daines , David Thomas Davies , Timothy Francis Gallagher , Graham Elgin Jones , William Henry Miller , Neil David Pearson , Israil Pendrak
发明人： Jeffrey Michael Axten , Robert A. Daines , David Thomas Davies , Timothy Francis Gallagher , Graham Elgin Jones , William Henry Miller , Neil David Pearson , Israil Pendrak
IPC分类号： A61K31/542 , C07D513/02 , C07D498/02 , A61K31/5383 , C07D491/02 , A61K31/436 , A61P31/04
CPC分类号： C07D493/04 , C07D417/12 , C07D513/04
摘要： Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译： 环己烷和环己烯衍生物及其药学上可接受的衍生物可用于治疗哺乳动物，特别是人的细菌感染的方法。
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公开(公告)号：US07622481B2
公开(公告)日：2009-11-24
申请号：US10518653
申请日：2003-06-25
申请人： Jeffrey Michael Axten , Robert A Daines , David Thomas Davies , Timothy Francis Gallagher , Graham Elgin Jones , William Henry Miller , Neil David Pearson , Israil Pendrak
发明人： Jeffrey Michael Axten , Robert A Daines , David Thomas Davies , Timothy Francis Gallagher , Graham Elgin Jones , William Henry Miller , Neil David Pearson , Israil Pendrak
IPC分类号： C07D513/04 , C07D471/04 , A61K31/542 , A61K31/4375
CPC分类号： C07D493/04 , C07D417/12 , C07D513/04
摘要： Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译： 环己烷和环己烯衍生物及其药学上可接受的衍生物可用于治疗哺乳动物，特别是人的细菌感染的方法。
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公开(公告)号：US08383635B2
公开(公告)日：2013-02-26
申请号：US13058251
申请日：2009-08-12
申请人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人： Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译： 本发明涉及吡啶并[4,3-d]嘧啶-5（6H） - 酮衍生物。 具体地，本发明涉及式I化合物：其中R1，R2，R3和R4定义如下。 本发明的化合物是PDK1的抑制剂，可用于治疗特征在于组成型激活的ACG激酶（例如癌症，更特别是乳腺癌，结肠癌和肺癌）的病症。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号：US07648984B2
公开(公告)日：2010-01-19
申请号：US11570600
申请日：2005-07-13
IPC分类号： A61K31/542
CPC分类号： C07D471/04
摘要： Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.
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公开(公告)号：US20090239866A1
公开(公告)日：2009-09-24
申请号：US11996994
申请日：2006-07-28
IPC分类号： A61K31/5377 , C07D207/12 , A61K31/40 , C07D401/12 , A61K31/4439 , C07D403/12 , A61K31/4155 , C07D413/12 , A61K31/422 , C07D405/12 , A61K31/4025 , A61K31/4178 , C07D409/12 , A61K31/436 , A61K31/496 , C07C235/88 , A61K31/16 , A61K31/454 , A61K31/497 , A61K31/404 , A61K31/437 , A61P31/04
CPC分类号： C07D207/16 , A61K38/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D491/056
摘要： Novel PDF inhibitors and novel methods for their use are provided.
摘要翻译： 提供了新的PDF抑制剂及其使用的新方法。
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18.发明授权Quinolines and nitrogenated derivatives thereof and their use as antibacterial agents 失效喹啉和其氮化衍生物及其作为抗菌剂的用途公开(公告)号：US07491714B2
公开(公告)日：2009-02-17
申请号：US10537034
申请日：2003-12-03
申请人： Jeffrey Michael Axten , Catherine Genevieve Yvette Dartois , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
发明人： Jeffrey Michael Axten , Catherine Genevieve Yvette Dartois , Guy Marguerite Marie Gerard Nadler , Neil David Pearson
IPC分类号： C07D413/02 , A61K31/421
CPC分类号： C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
摘要翻译： 喹啉和萘啶衍生物可用于治疗哺乳动物，特别是人的细菌感染。
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公开(公告)号：US07232832B2
公开(公告)日：2007-06-19
申请号：US10533502
申请日：2003-11-04
IPC分类号： C07D401/06 , A61K31/47
CPC分类号： C07D471/04
摘要： Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
摘要翻译： 喹啉和萘啶衍生物可用于治疗哺乳动物，特别是人的细菌感染。
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