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公开(公告)号:US20080214455A1
公开(公告)日:2008-09-04
申请号:US11912969
申请日:2006-05-03
申请人: Kevin Duffy , Deping Chai , Mirela Colon , Duke M. Fitch , Sarah Rae King , Antony N. Shaw , Rosanna Tedesco , Kenneth Wiggall , Michael N. Zimmerman , Neil W. Johnson , Jiri Kasparec
发明人: Kevin Duffy , Deping Chai , Mirela Colon , Duke M. Fitch , Sarah Rae King , Antony N. Shaw , Rosanna Tedesco , Kenneth Wiggall , Michael N. Zimmerman , Neil W. Johnson , Jiri Kasparec
IPC分类号: C07D417/02 , C07D417/14 , A61K31/5377 , A61K31/498 , A61K31/496 , A61K31/4709 , A61K38/22 , A61P7/00
CPC分类号: C07D417/06
摘要: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.
摘要翻译: 本发明涉及新鉴定的用于抑制hYAK3蛋白的化合物和用于治疗与hYAK3活性相关的疾病的方法。
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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:US20140018393A1
公开(公告)日:2014-01-16
申请号:US14007035
申请日:2012-03-26
申请人: Neil W. Johnson , Jiri Kasparec
发明人: Neil W. Johnson , Jiri Kasparec
IPC分类号: C07D211/26
CPC分类号: A61K31/445 , C07C211/35 , C07C211/36 , C07C271/24 , C07C2601/02 , C07C2601/14 , C07D207/09 , C07D211/26 , C07D211/62 , C07D211/96 , C07D223/04 , C07D265/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D413/06 , C07F5/02 , C07F5/025 , C07F9/59
摘要: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
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公开(公告)号:US08853408B2
公开(公告)日:2014-10-07
申请号:US14007035
申请日:2012-03-26
申请人: Neil W. Johnson , Jiri Kasparec
发明人: Neil W. Johnson , Jiri Kasparec
IPC分类号: C07D211/32 , A01N43/40 , A61K31/445 , C07D401/04 , C07D223/04 , C07D265/30 , C07D211/96 , C07C271/24 , C07D413/06 , C07D211/26 , C07D401/06 , C07D401/10 , C07C211/35 , C07D211/62 , C07F9/59 , C07D207/09 , C07F5/02 , C07C211/36
CPC分类号: A61K31/445 , C07C211/35 , C07C211/36 , C07C271/24 , C07C2601/02 , C07C2601/14 , C07D207/09 , C07D211/26 , C07D211/62 , C07D211/96 , C07D223/04 , C07D265/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D413/06 , C07F5/02 , C07F5/025 , C07F9/59
摘要: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
摘要翻译: 本发明涉及环丙胺衍生物用于调节,特别是赖氨酸特异性脱甲基酶1(LSD1)的活性的抑制。 适宜地,本发明涉及环丙胺在治疗癌症中的应用。
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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:US20100311736A1
公开(公告)日:2010-12-09
申请号:US12739176
申请日:2008-10-22
申请人: Nicholas D. Adams , Michael Gerard Darcy , Neil W. Johnson , Jiri Kasparec , Steven David Knight , Kenneth Allen Newlander , Xin Peng , Lance H. Ridgers
发明人: Nicholas D. Adams , Michael Gerard Darcy , Neil W. Johnson , Jiri Kasparec , Steven David Knight , Kenneth Allen Newlander , Xin Peng , Lance H. Ridgers
IPC分类号: A61K31/536 , A61K31/44 , C07D213/72 , A61K31/444 , C07D213/22 , A61K31/4439 , C07D401/02 , A61K31/5377 , C07D413/14 , A61K31/506 , C07D401/04 , A61K31/4709 , C07D413/02 , A61K31/498 , A61P35/00 , A61P37/06 , A61P29/00 , A61P9/00 , A61P25/00
CPC分类号: C07D213/76 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.
摘要翻译: 本发明是使用吡啶磺酰胺衍生物抑制PI3激酶的活性/功能的方法。 还发明了一种治疗选自以下的一种或多种疾病状态的方法:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,变态反应,哮喘,胰腺炎,多器官功能衰竭,肾脏疾病,血小板聚集,癌症,精子活力,移植排斥反应, 通过施用吡啶磺酰胺衍生物的移植排斥和肺损伤。
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公开(公告)号:US20070249599A1
公开(公告)日:2007-10-25
申请号:US10590623
申请日:2005-02-24
申请人: Kevin Duffy , Duke Fitch , Steven Goodman , Masaichi Hasegawa , Neil Johnson , Jiri Kasparec , Antony Shaw
发明人: Kevin Duffy , Duke Fitch , Steven Goodman , Masaichi Hasegawa , Neil Johnson , Jiri Kasparec , Antony Shaw
IPC分类号: A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5355 , C07D277/04 , C07D417/10
CPC分类号: C07D417/06 , C07D417/14
摘要: This invention relates to the newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.
摘要翻译: 本发明涉及新鉴定的用于抑制hYAK3蛋白的化合物和用于治疗与hYAK3蛋白的不平衡或不适当活性相关的疾病的方法。
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公开(公告)号:US07759486B2
公开(公告)日:2010-07-20
申请号:US11839830
申请日:2007-08-16
申请人: Jerry L. Adams , Jeffrey C. Boehm , Ralph Hall , Qi Jin , Jiri Kasparec , Domingos J. Silva , John J. Taggart
发明人: Jerry L. Adams , Jeffrey C. Boehm , Ralph Hall , Qi Jin , Jiri Kasparec , Domingos J. Silva , John J. Taggart
IPC分类号: C07D239/02
CPC分类号: C07D239/47 , C07D471/04
摘要: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
摘要翻译: 新型取代的2,4,8-三取代-8H-吡啶并[2,3-d]嘧啶-7-酮化合物和用作CSBP / p38激酶抑制剂治疗的组合物。
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公开(公告)号:US20090012309A1
公开(公告)日:2009-01-08
申请号:US11928101
申请日:2007-10-30
IPC分类号: C07D231/06
CPC分类号: C07D233/90 , C07D405/12
摘要: Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.
摘要翻译: 吡唑衍生物在本文中描述。 所述的发明还包括制备这种吡唑衍生物的方法以及使用它们在治疗疾病中的方法。
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公开(公告)号:US20080268044A1
公开(公告)日:2008-10-30
申请号:US12093191
申请日:2006-11-15
申请人: John Robert George Appleby , Philip Blatcher , Ann M. Diederich , Lesley Anne Humphries , Jiri Kasparec , As'ad Abu Khalil , Richard S. Lloyd , Paul G. Spoors , John J. Taggart , Lois E. Vernon
发明人: John Robert George Appleby , Philip Blatcher , Ann M. Diederich , Lesley Anne Humphries , Jiri Kasparec , As'ad Abu Khalil , Richard S. Lloyd , Paul G. Spoors , John J. Taggart , Lois E. Vernon
IPC分类号: C07D487/04 , A61K31/519 , A61K9/20 , A61P1/00 , A61P9/00 , A61P11/00
CPC分类号: A61K31/513 , A61K9/2054 , A61K9/2077 , C07D471/04 , Y02A50/401 , Y02A50/409 , Y02A50/411
摘要: The present invention provides for a novel process of making 6-carboxylic acid derivatives of pyrido[2,3-d]pyrimidin-7-one's, as well as a novel process for making 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxy-1-(hydroxymethyl)ethyl]-amino}pyrido[2,3-d]pyrimidin-7(8H)-one, and salts thereof.
摘要翻译: 本发明提供了制备吡啶并[2,3-d]嘧啶-7-酮的6-羧酸衍生物的新方法,以及制备8-(2,6-二氟苯基)-4- (4-氟-2-甲基苯基)-2 - {[2-羟基-1-(羟甲基)乙基] - 氨基}吡啶并[2,3-d]嘧啶-7(8H) - 酮及其盐。
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