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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：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：US10208047B2
公开(公告)日：2019-02-19
申请号：US15538910
申请日：2015-12-17
申请人： Jian Liu , Joseph A. Kozlowski , Brian M. Andresen , Sobhana Babu Boga , Xiaolei Gao , Deodial Guy Guiadeen , Jiaqiang Cai , Shilan Liu , Dahai Wang , Hao Wu , Chundao Yang
发明人： Jian Liu , Joseph A. Kozlowski , Brian M. Andresen , Sobhana Babu Boga , Xiaolei Gao , Deodial Guy Guiadeen , Jiaqiang Cai , Shilan Liu , Dahai Wang , Hao Wu , Chundao Yang
IPC分类号： C07D487/04 , A61K31/4985 , A61K45/06
摘要： The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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公开(公告)号：US20210206796A1
公开(公告)日：2021-07-08
申请号：US16771814
申请日：2018-12-17
申请人： Brian M. ANDRESEN , Frank BENNETT , Wonsuk CHANG , Matthew Lloyd CHILDERS , Jared N. CUMMING , Jongwon LIM , Min LU , Benjamin Wesley TROTTER , Wen-Lian WU , Merck Sharp & Dohme Corp.
发明人： Brian M. Andresen , Frank Bennett , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Jongwon Lim , Min Lu , Benjamin Wesley Trotter , Wen-Lian Wu
摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.
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公开(公告)号：US09085536B2
公开(公告)日：2015-07-21
申请号：US13421809
申请日：2012-03-15
IPC分类号： A61K31/439 , C07D221/22
CPC分类号： C07D221/22 , A61K31/439 , A61K31/695
摘要： Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.
摘要翻译： 提供乌头碱的复合衍生物，特别是调节钠通道活性的衍生物。 还提供了包含本发明化合物和药学上可接受的载体的药物组合物。 主题化合物可用于治疗，包括调节神经元活动或引起肌肉松弛的治疗。 该化合物还可用于治疗患有电压门控钠通道增强性疾病或疼痛的受试者。 提供了用于制备乌头碱衍生物的其它方法。
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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：US20120238526A1
公开(公告)日：2012-09-20
申请号：US13421809
申请日：2012-03-15
IPC分类号： A61K31/439 , C07D405/12 , C07F7/18 , A61K31/695 , A61P25/00 , A61P21/02 , A61P29/00 , A61P1/00 , A61P19/02 , A61P25/06 , A61P35/00 , A61P9/06 , A61P25/08 , A61P21/00 , A61P13/10 , A61P17/00 , C07D221/22
CPC分类号： C07D221/22 , A61K31/439 , A61K31/695
摘要： Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.
摘要翻译： 提供乌头碱的复合衍生物，特别是调节钠通道活性的衍生物。 还提供了包含本发明化合物和药学上可接受的载体的药物组合物。 主题化合物可用于治疗，包括调节神经元活动或引起肌肉松弛的治疗。 该化合物还可用于治疗患有电压门控钠通道增强性疾病或疼痛的受试者。 提供了用于制备乌头碱衍生物的其它方法。
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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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