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公开(公告)号:US07495102B2
公开(公告)日:2009-02-24
申请号:US11855183
申请日:2007-09-14
申请人: Martha A. Sarpong , Nicholas D. Adams , Jeffrey Michael Axten , Amita M. Chaudhari , Dashyant Dhanak , Toshihiro Hamajima , Kenneth Allen Newlander , Cynthia A. Parrish , Jerry Leroy Adams , Domingos J. Silva , Jun Tang
发明人: Martha A. Sarpong , Nicholas D. Adams , Jeffrey Michael Axten , Amita M. Chaudhari , Dashyant Dhanak , Toshihiro Hamajima , Kenneth Allen Newlander , Cynthia A. Parrish , Jerry Leroy Adams , Domingos J. Silva , Jun Tang
IPC分类号: C07D453/02
CPC分类号: C07D471/04
摘要: The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.
摘要翻译: 本发明涉及由式(I)表示的化合物及其药学上可接受的盐。 本发明的化合物抑制Aurora激酶,使其特别适用于治疗许多疾病,包括实体瘤癌症和血液癌症。
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公开(公告)号:US20100016318A1
公开(公告)日:2010-01-21
申请号:US12524009
申请日:2008-01-25
申请人: Jeffrey Michael Axten , Deborah L. Bryan , David Harold Drewry , Thomas H. Faitg , Timothy Francis Gallagher , Neil W. Johnson , Jiri Kasparec , Jeffrey M. Ralph , Domingos J. Silva
发明人: Jeffrey Michael Axten , Deborah L. Bryan , David Harold Drewry , Thomas H. Faitg , Timothy Francis Gallagher , Neil W. Johnson , Jiri Kasparec , Jeffrey M. Ralph , Domingos J. Silva
IPC分类号: A61K31/5355 , A61K31/541 , A61K31/505 , A61K31/506 , C07D279/12 , C07D403/02 , C07D239/24 , C07D413/02
CPC分类号: C07D403/12 , C07D241/20 , C07D413/12
摘要: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1′ R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.
摘要翻译: 本发明涉及由下式表示的化合物或其药学上可接受的盐; 其中R1,R1'R2,R3,R4,R5,r和s如本文所定义。 本发明的化合物可用于治疗与极光激酶活性相关的疾病如癌症。
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公开(公告)号:US07884098B2
公开(公告)日:2011-02-08
申请号:US12524009
申请日:2008-01-25
申请人: Jeffrey Michael Axten , Deborah L. Bryan , David Harold Drewry , Thomas H Faitg , Timothy Francis Gallagher , Neil W Johnson , Jiri Kasparec , Jeffrey M Ralph , Domingos J. Silva
发明人: Jeffrey Michael Axten , Deborah L. Bryan , David Harold Drewry , Thomas H Faitg , Timothy Francis Gallagher , Neil W Johnson , Jiri Kasparec , Jeffrey M Ralph , Domingos J. Silva
IPC分类号: A61K31/5355 , A61K31/541 , A61K31/505 , A61K31/506 , C07D279/12 , C07D403/02 , C07D239/24 , C07D413/02
CPC分类号: C07D403/12 , C07D241/20 , C07D413/12
摘要: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1′ R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.
摘要翻译: 本发明涉及由下式表示的化合物或其药学上可接受的盐; 其中R1,R1'R2,R3,R4,R5,r和s如本文所定义。 本发明的化合物可用于治疗与极光激酶活性相关的疾病如癌症。
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公开(公告)号:US20120077828A1
公开(公告)日:2012-03-29
申请号:US13069569
申请日:2011-03-23
申请人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Raul Medina , Stuart Paul Romeril , Jun Tang
发明人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Raul Medina , Stuart Paul Romeril , Jun Tang
IPC分类号: A61K31/519 , A61P35/00 , A61P25/28 , A61P25/00 , A61P3/10 , A61P25/16 , A61P25/14 , A61P9/10 , A61P9/00 , A61P9/06 , A61P27/02 , A61P35/04 , A61P35/02 , A61P27/10 , C07D487/04
CPC分类号: C07D487/04 , A61K31/405 , A61K45/06 , C07D403/04 , C07D491/04 , C07D495/04 , A61K2300/00
摘要: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein.The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, 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 PERK 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: 本发明涉及取代的二氢吲哚衍生物。 具体地,本发明涉及式I化合物:其中R1,R2和R3如本文所定义。 本发明的化合物是PERK的抑制剂,可用于治疗癌症,眼部疾病和与活化的未折叠蛋白反应途径相关的疾病,例如阿尔茨海默氏病,中风,1型糖尿病帕金森病,亨廷顿舞蹈病,肌萎缩性侧索 硬化症,心肌梗死,心血管疾病,动脉粥样硬化和心律失常,更具体地说是乳腺癌,结肠癌,胰腺癌和肺癌。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。
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公开(公告)号:US20130018038A1
公开(公告)日:2013-01-17
申请号:US13637127
申请日:2011-03-23
申请人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Rual Medina , Stuart Paul Romeril , Jun Tang
发明人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Rual Medina , Stuart Paul Romeril , Jun Tang
IPC分类号: A61K31/519 , C07D495/04 , C07D403/10 , C07D491/048 , C07D471/04 , A61K31/4365 , A61K31/416 , A61K31/4355 , A61P35/00 , A61P25/28 , A61P3/10 , A61P25/16 , A61P9/00 , A61P9/10 , A61P9/06 , A61P27/02 , A61P35/04 , A61P35/02 , C07D487/04
CPC分类号: C07D487/04 , A61K31/405 , A61K45/06 , C07D403/04 , C07D491/04 , C07D495/04 , A61K2300/00
摘要: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein.The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, 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 PERK 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: 本发明涉及取代的二氢吲哚衍生物。 具体地,本发明涉及式I化合物:其中R1,R2和R3如本文所定义。 本发明的化合物是PERK的抑制剂,可用于治疗癌症,眼部疾病和与活化的未折叠蛋白反应途径相关的疾病,例如阿尔茨海默氏病,中风,1型糖尿病帕金森病,亨廷顿舞蹈病,肌萎缩性侧索 硬化症,心肌梗死,心血管疾病,动脉粥样硬化和心律失常,更具体地说是乳腺癌,结肠癌,胰腺癌和肺癌。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。
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公开(公告)号:US08598156B2
公开(公告)日:2013-12-03
申请号:US13637127
申请日:2011-03-23
申请人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Rual Medina , Stuart Paul Romeril , Jun Tang
发明人: Jeffrey Michael Axten , Seth Wilson Grant , Dirk A. Heerding , Jesus Rual Medina , Stuart Paul Romeril , Jun Tang
CPC分类号: C07D487/04 , A61K31/405 , A61K45/06 , C07D403/04 , C07D491/04 , C07D495/04 , A61K2300/00
摘要: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, 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 PERK 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: 本发明涉及取代的二氢吲哚衍生物。 具体地,本发明涉及式I化合物:其中R1,R2和R3如本文所定义。 本发明的化合物是PERK的抑制剂,可用于治疗癌症,眼部疾病和与活化的未折叠蛋白反应途径相关的疾病,例如阿尔茨海默氏病,中风,1型糖尿病帕金森病,亨廷顿舞蹈病,肌萎缩性侧索 硬化症,心肌梗死,心血管疾病,动脉粥样硬化和心律失常,更具体地说是乳腺癌,结肠癌,胰腺癌和肺癌。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。
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公开(公告)号:US20110275611A1
公开(公告)日:2011-11-10
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: A61K31/506 , C07D417/14 , C07D413/14 , C07D401/14 , A61K31/541 , A61K31/5377 , C07D403/14 , A61K31/55 , C07D471/04 , A61P35/00 , A61P35/02 , A61P3/10 , A61P37/06 , A61P17/06 , A61P1/00 , C07D403/10
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。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PDK1活性和与之相关疾病的治疗方法
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公开(公告)号:US20110136838A1
公开(公告)日:2011-06-09
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: A61K31/519 , C07D471/04 , A61P35/00
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:US07618959B2
公开(公告)日:2009-11-17
申请号:US10533501
申请日:2003-11-04
IPC分类号: C07D513/04 , A61K31/542
CPC分类号: C07D471/04 , C07D413/12 , C07D513/04
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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公开(公告)号:US07498326B2
公开(公告)日:2009-03-03
申请号:US10518655
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: C07D471/04 , A61K31/4375
CPC分类号: C07D491/04 , A61K31/03 , A61K31/535 , A61K31/54 , C07D513/04
摘要: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. The piperidine derivatives include compounds of formula (I): wherein RA, AB, n, R3, R2 and R4 are defined herein. For example, RA is an optionally substituted bicyclic carbocyclic or heterocyclic ring system, and R4 is a group U-R5 in which R5 is an optionally substituted bicyclic heterocyclic ring system as defined herein (e.g. optionally substituted pyrido [3,2, -b][1,4] thiazin-yl).
摘要翻译: 哌啶衍生物及其药学上可接受的衍生物可用于哺乳动物,特别是人的细菌感染治疗方法。 哌啶衍生物包括式(I)的化合物:其中RA,AB,n,R 3,R 2和R 4在本文中定义。 例如,RA是任选取代的双环碳环或杂环系统,并且R 4是基团U-R 5,其中R 5是如本文所定义的任选取代的双环杂环体系(例如任选取代的吡啶并[3,2-b] [1,4]噻嗪基)。
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