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公开(公告)号：US09822107B2
公开(公告)日：2017-11-21
申请号：US15105713
申请日：2014-12-18
申请人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier , MERCK SHARP & DOHME CORP.
发明人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier
IPC分类号： C07D417/12 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r 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).
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2.发明申请公开(公告)号：US20160340351A1
公开(公告)日：2016-11-24
申请号：US15105713
申请日：2014-12-18
申请人： Brian M. ANDRESEN , Kenneth L. ARRINGTON , Ryan D. OTTE , John Michael ELLIS , John W. BUTCHER , Alan B. NORTHRUP , Joel S. ROBICHAUD , Jacques Yves GAUTHIER , Jean-Francois FOURNIER , MERCK SHARP & DOHME CORP.
发明人： Brian M. Andresen , Kenneth L. Arrington , Ryan D. Otte , John Michael Ellis , John W. Butcher , Alan B. Northrup , Joel S. Robichaud , Jacques Yves Gauthier , Jean-Francois Fournier
IPC分类号： C07D417/14 , C07D417/12 , A61K31/5377 , A61K31/506 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r 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： 本发明提供了式（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R1，R2，R3，R4，环B和下标r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：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：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：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：US20100298347A1
公开(公告)日：2010-11-25
申请号：US12743610
申请日：2008-12-01
申请人： Michel Belley , Denis Deschenes , Rejean Fortin , Jean-Francois Fournier , Sebastien Gagne , Yves Gareau , Jacques Yves Gauthier , Lianhai Li , Joel Robichaud , Michel Therien , Geoffrey K. Tranmer , Zhaoyin Wang
发明人： Michel Belley , Denis Deschenes , Rejean Fortin , Jean-Francois Fournier , Sebastien Gagne , Yves Gareau , Jacques Yves Gauthier , Lianhai Li , Joel Robichaud , Michel Therien , Geoffrey K. Tranmer , Zhaoyin Wang
IPC分类号： A61K31/519 , C07C63/72 , C07D333/34 , C07D333/22 , C07C63/42 , C07D317/54 , C07D409/12 , C07D487/04 , C07D249/08 , C07D211/94 , C07D211/32 , A61K31/192 , A61K31/381 , A61K31/194 , A61K31/36 , A61K31/4436 , A61K31/4196 , A61K31/451 , A61P3/10 , A61P5/50 , A61P3/04 , A61P3/00
CPC分类号： C07D211/34 , C07C65/24 , C07C65/30 , C07C65/40 , C07C69/76 , C07C69/94 , C07C317/44 , C07C317/46 , C07C323/62 , C07D211/52 , C07D249/08 , C07D317/60 , C07D333/16 , C07D333/24 , C07D333/34 , C07D487/04
摘要： Substituted 2-naphthoic acids of structural formula are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabetes, particularly, Type 2 diabetes, insulin resistance, hyperglycemia, lipid disorders, obesity, atherosclerosis, and conditions associated with the Metabolic Syndrome.
摘要翻译： 结构式的取代的2-萘甲酸作为GPR105蛋白的生物活性的拮抗剂是有效的。 它们可用于治疗，控制或预防对该受体的拮抗作用有响应的病症，例如糖尿病，特别是2型糖尿病，胰岛素抵抗，高血糖症，脂质障碍，肥胖症，动脉粥样硬化和与代谢综合征有关的病症。
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公开(公告)号：US09353066B2
公开(公告)日：2016-05-31
申请号：US14422419
申请日：2013-08-15
发明人： Andrew M. Haidle , Jason Burch , Daniel Guay , Jacques Yves Gauthier , Joel Robichaud , Jean Francois Fournier , John Michael Ellis , Matthew Christopher , Solomon D. Kattar , Graham F. Smith , Alan B. Northrup
IPC分类号： C07D239/42 , C07D403/12 , A61K31/506 , A61K31/505 , C07D401/12 , C07D239/47
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t 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： 本发明提供某些取代的式（I）的苯基化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy和t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：US20150232428A1
公开(公告)日：2015-08-20
申请号：US14422419
申请日：2013-08-15
发明人： Andrew M. Haidle , Jason Burch , Daniel Guay , Jacques Yves Gauthier , Joel Robichaud , Jean Francois Fournier , John Michael Ellis , Matthew Christopher , Solomon D. Kattar , Graham F. Smith , Alan B. Northrup
IPC分类号： C07D239/42 , C07D239/47 , A61K31/506 , C07D403/12 , A61K31/505 , C07D401/12
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
摘要： The invention provides certain substituted phenyl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, and t 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： 本发明提供某些取代的式（I）的苯基化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy和t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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