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公开(公告)号：US20170114078A1
公开(公告)日：2017-04-27
申请号：US15318483
申请日：2015-06-09
申请人： Meredeth Ann MCGOWAN , Kin Chiu FONG , Neville John ANTHONY , Hua ZHOU , Jason D. KATZ , Lihu YANG , Chaomin LI , Yuan TIAN , Changwei MU , Baijun YE , Feng SHI , Xiaoli ZHAO , Jianmin FU , Yabin LI , Merck Sharp & Dohme Corp.
发明人： Meredeth Ann McGowan , Kin Chiu Fong , Neville John Anthony , Hua Zhou , Jason D. Katz , Lihu Yang , Chaomin Li , Yuan Tian , Changwei Mu , Baijun Ye , Feng Shi , Xiaoli Zhao , Jianmin Fu , Yabin Li
IPC分类号： C07D519/00 , C07D473/30 , C07D473/34 , A61K31/52
CPC分类号： C07D519/00 , A61K31/52 , C07D473/30 , C07D473/34
摘要： The instant invention provides compounds of formula (I) which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
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公开(公告)号：US08551984B2
公开(公告)日：2013-10-08
申请号：US12968608
申请日：2010-12-15
申请人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Michael H. Reutershan , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hua Zhou
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Michael H. Reutershan , Eric Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hua Zhou
IPC分类号： C07D417/12 , A61K31/497
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：US20120022044A1
公开(公告)日：2012-01-26
申请号：US13139830
申请日：2009-12-07
申请人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
发明人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
IPC分类号： A61K31/55 , C07D403/04 , C07D409/14 , A61P25/28 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D401/14 , C07D417/14
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱A＆bgr的产生42，因此可用于治疗阿尔茨海默病和相关病症。
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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：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：US08759579B2
公开(公告)日：2014-06-24
申请号：US12989131
申请日：2009-04-17
申请人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
发明人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
IPC分类号： C07C311/13 , C07C61/16 , A61K31/195 , A61K31/18
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的环丁基砜衍生物，它们通过推定的γ-分泌酶抑制APP的加工，同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。 还包括药物组合物和使用方法。
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公开(公告)号：US08575150B2
公开(公告)日：2013-11-05
申请号：US13139830
申请日：2009-12-07
申请人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
发明人： Christian Fischer , Joey Methot , Hua Zhou , Adam J. Schell , Benito Munoz , Alexey A. Rivkin , Sean P. Ahearn , Stephanie Chichetti , Rachel N. MacCoss , Sam Kattar , Matthew Christopher , Chaomin Li , Andrew Rosenau , William Colby Brown
IPC分类号： C07D249/14 , A61K31/4196
CPC分类号： A61K31/41 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.
摘要翻译： 根据本发明，提供式I化合物或其药学上可接受的盐或水合物; 其中变量如本文所定义。 这些化合物选择性地减弱Abeta42的产生，因此可用于治疗阿尔茨海默病和相关病症。
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公开(公告)号：US20110039925A1
公开(公告)日：2011-02-17
申请号：US12989131
申请日：2009-04-17
申请人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
发明人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
IPC分类号： C07C311/13 , A61K31/195 , A61K31/18 , C07C61/16 , A61K31/351 , C07D309/10 , A61P25/28
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括一类新的环丁基砜衍生物，它们通过推定的γ-分泌酶抑制APP的加工，同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。 还包括药物组合物和使用方法。
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