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公开(公告)号：US20140243290A1
公开(公告)日：2014-08-28
申请号：US14255480
申请日：2014-04-17
申请人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号： C07D417/12 , C07D495/04 , C07D451/06 , C07F9/6558 , C07D471/08 , C07D487/04 , C07D471/04 , C07D417/14 , C07D491/08
CPC分类号： C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎。
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公开(公告)号：US08367706B2
公开(公告)日：2013-02-05
申请号：US12665045
申请日：2008-06-16
申请人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
发明人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyun Chong Woo , Jonathan Young , Anna Zabierek
IPC分类号： A61K31/4436 , C07D409/12
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：US20120277192A1
公开(公告)日：2012-11-01
申请号：US13516455
申请日：2010-12-15
申请人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号： A61K31/506 , A61K31/55 , A61K31/554 , A61K31/551 , A61P35/00 , C07D417/14 , C07F9/6539 , C07D417/12 , A61P19/02 , A61P11/06 , A61K31/675 , A61K31/5377
CPC分类号： C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
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公开(公告)号：US20110245205A1
公开(公告)日：2011-10-06
申请号：US12968608
申请日：2010-12-15
申请人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号： A61K31/675 , C07D417/14 , A61K31/55 , C07D417/12 , A61K31/506 , C07F9/6558 , A61K31/397 , A61K31/551 , A61K31/553 , A61K31/541 , C07D413/14 , A61K31/5377 , A61P11/06 , A61P35/00 , A61P19/02
CPC分类号： C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
摘要： The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，其是脾脏酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD和类风湿性关节炎。
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公开(公告)号：US08937077B2
公开(公告)日：2015-01-20
申请号：US13880767
申请日：2011-10-17
申请人： David Joseph Guerin , Jason D. Brubaker , Michelle Martinez , Joon O. Jung , Neville J. Anthony , Mark E. Scott , Carolyn Michele Cammarano , Dawn Marie Mampreian Hoffman , Hyun Chong Woo , Christopher J. Dinsmore , Philip Jones
发明人： David Joseph Guerin , Jason D. Brubaker , Michelle Martinez , Joon O. Jung , Neville J. Anthony , Mark E. Scott , Carolyn Michele Cammarano , Dawn Marie Mampreian Hoffman , Hyun Chong Woo , Christopher J. Dinsmore , Philip Jones
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/519 , C07D519/00
摘要： The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为Jak抑制剂的式I化合物，因此可用于治疗Jak介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US20140235641A1
公开(公告)日：2014-08-21
申请号：US14345982
申请日：2012-09-21
申请人： Jason Brubaker , Joshua Close , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Zhongyong Wei , Feng Shi
发明人： Jason Brubaker , Joshua Close , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Zhongyong Wei , Feng Shi
IPC分类号： C07D401/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D405/04 , C07D413/14 , C07D401/14
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US20130225577A1
公开(公告)日：2013-08-29
申请号：US13880767
申请日：2011-10-17
申请人： David Joseph Guerin , Jason D. Brubaker , Michelle Martinez , Joon O. Jung , Neville J. Anthony , Mark E. Scott , Carolyn Michele Cammarano , Dawn Marie Mampreian Hoffman , Hyun Chong Woo , Christopher J. Dinsmore , Philip Jones
发明人： David Joseph Guerin , Jason D. Brubaker , Michelle Martinez , Joon O. Jung , Neville J. Anthony , Mark E. Scott , Carolyn Michele Cammarano , Dawn Marie Mampreian Hoffman , Hyun Chong Woo , Christopher J. Dinsmore , Philip Jones
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/519 , C07D519/00
摘要： The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为Jak抑制剂的式I化合物，因此可用于治疗Jak介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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8.发明申请公开(公告)号：US20160060255A1
公开(公告)日：2016-03-03
申请号：US14786464
申请日：2014-04-22
申请人： Neville J. ANTHONY , Brain M. ANDERSEN , Alan B. NORTHRUP , Kaleen K. CHILDERS , Anthony FRIO , Thomas A. MILLER , Yuan LIU , Michelle R. MACHACEK , Hyun Chong WOO , Kerrie B. SPENCER , John Michael ELLIS , Micheal D. ALTMAN , Eric T. ROMEO , Daniel GUAY , Jonathan GRIMM , Marie-Eve LEBRUN , Joel S. ROBICHAUD , Liping WANG , Byron DUBOIS , Qiaolin DENG , MERICK SHARP & DOHNE CORP. , MERCK CANADA INC.
发明人： Neville J. Anthony , Brian M. Andresen , Alan B. Northrup , Kaleen K. Childers , Anthony Donofrio , Thomas A. Miller , Yuan Liu , Michelle R. Machacek , Hyun Chong Woo , Kerrie B. Spencer , John Michael Ellis , Michael D. Altman , Eric T. Romeo , Daniel Guay , Jonathan Grimm , Marie-Eve Lebrun , Joel S. Robichaud , Liping Wang , Byron DuBois , Qiaolin Deng
IPC分类号： C07D417/14 , A61K31/53 , A61K31/4439 , A61K31/501 , A61K31/506 , A61K31/497
CPC分类号： C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, and R4 are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
摘要翻译： 本发明提供式（I）的某些噻唑取代的氨基杂芳基化合物或其药学上可接受的盐，其中X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和R 4如本文所定义。 本发明还提供包含这些化合物的药物组合物，以及使用该化合物治疗由脾脏酪氨酸激酶（Syk）介导的疾病或病症的方法。
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公开(公告)号：US09394282B2
公开(公告)日：2016-07-19
申请号：US14345982
申请日：2012-09-21
申请人： Jason Brubaker , Joshua Close , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Zhongyong Wei , Feng Shi
发明人： Jason Brubaker , Joshua Close , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Zhongyong Wei , Feng Shi
IPC分类号： C07D401/04 , C07D405/14 , C07D409/04 , C07D417/14 , C07D405/04 , C07D413/14 , C07D401/14 , C07D405/08 , C07D403/12 , C07D231/38 , C07D401/12 , C07D403/08 , C07D405/12 , C07D409/12 , C07D413/12 , C07D403/04 , C07D401/06 , C07D403/06 , C07D405/06
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US09328099B2
公开(公告)日：2016-05-03
申请号：US14345978
申请日：2012-09-21
申请人： Jason Brubaker , Matthew Lloyd Childers , Matthew Christopher , Joshua T. Close , Jason David Katz , Joon Jung , Scott Peterson , Phieng Siliphaivanh , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Hongjun Zhang
发明人： Jason Brubaker , Matthew Lloyd Childers , Matthew Christopher , Joshua T. Close , Jason David Katz , Joon Jung , Scott Peterson , Phieng Siliphaivanh , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Hongjun Zhang
IPC分类号： C07D231/38 , C07D405/04 , C07D401/14 , C07D401/04 , C07D403/04 , C07D405/08 , C07D403/12 , C07D401/12 , C07D403/08 , C07D405/12 , C07D409/12 , C07D413/12 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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