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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：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：US08735417B2
公开(公告)日：2014-05-27
申请号：US13515941
申请日：2010-12-16
申请人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号： A61K31/506 , C07D417/02
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
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：US20120309735A1
公开(公告)日：2012-12-06
申请号：US13515941
申请日：2010-12-16
申请人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号： A61K31/506 , C07D417/12 , C07D417/14 , C07D471/04 , A61P19/02 , A61K31/551 , A61P11/06 , A61P11/00 , A61P29/00 , C07D471/10 , A61K31/5377
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
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：US09586931B2
公开(公告)日：2017-03-07
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20150239866A1
公开(公告)日：2015-08-27
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
摘要翻译： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。
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公开(公告)号：US20210309688A1
公开(公告)日：2021-10-07
申请号：US17266507
申请日：2019-08-05
申请人： Jongwon Lim , Michelle Machacek , Michael H. Reutershan , Sebastian Schneider , Merck Sharp & Dohme Corp.
IPC分类号： C07H19/167 , C07D473/34 , C07D471/04
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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公开(公告)号：US11993602B2
公开(公告)日：2024-05-28
申请号：US17266474
申请日：2019-08-05
申请人： Merck Sharp & Dohme LLC , David Witter , Shuhei Kawamura , Michelle Machacek , Ryan Quiroz , Michael H. Reutershan , Sebastian Schneider , Phieng Siliphaivanh , Yingchun Ye , Charles S. Yeung
发明人： David Witter , Shuhei Kawamura , Michelle Machacek , Ryan Quiroz , Michael H. Reutershan , Sebastian Schneider , Phieng Siliphaivanh , Yingchun Ye , Charles S. Yeung
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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