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公开(公告)号：US20170071935A1
公开(公告)日：2017-03-16
申请号：US15125373
申请日：2015-03-09
申请人： Michael D. ALTMAN , Brandon CASH , John Michael ELLIS , Matthew L. MADDESS , Alan B. NORTHRUP , Ryan D. OTTE , Binyuan SUN , Merck Sharp & Dohme Corp.
发明人： Michael D. Altman , Brandon Cash , John Michael Ellis , Matthew L. Maddess , Alan B. Northrup , Ryan D. Otte , Binyuan Sun
IPC分类号： A61K31/497 , C07D405/04 , C07D403/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07D491/056 , A61K45/06 , C07D409/14
CPC分类号： A61K31/497 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X 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： 本发明提供了一些式（I）的吡嗪-2-甲酰胺化合物或其药学上可接受的盐，其中A，B和X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：US20160130659A1
公开(公告)日：2016-05-12
申请号：US14894705
申请日：2014-06-03
IPC分类号： C12Q1/68 , C07K16/28 , G01N33/574
CPC分类号： C12Q1/6886 , A61K31/00 , C07K16/2827 , C12Q2600/106 , C12Q2600/158 , G01N33/57426 , G01N2333/70532 , G01N2800/52
摘要： The instant invention relates to methods for the treatment of B-cell lymphomas and leukemia by administering a SYK inhibitor. In another embodiment, the invention relates to a method for treating a patient diagnosed with a B-cell lymphoma or leukemia, comprising administering a SYK inhibitor, wherein the B-cells of said patient to be treated are characterized by elevated expression levels of CD86.
摘要翻译： 本发明涉及通过施用SYK抑制剂治疗B细胞淋巴瘤和白血病的方法。 在另一个实施方案中，本发明涉及治疗诊断患有B细胞淋巴瘤或白血病的患者的方法，包括施用SYK抑制剂，其中所述待治疗患者的B细胞的特征在于CD86的表达水平升高。
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公开(公告)号：US20150191461A1
公开(公告)日：2015-07-09
申请号：US14409133
申请日：2013-06-18
发明人： Michelle R. Machacek , Michael D. Altman , Eric T. Romeo , Dilrukshi Vitharana , Brandon Cash , Tony Siu , Matthew Christopher , Solomon D. Kattar , Andrew M. Haidle , Kaleen Konrad Childers , Matthew L. Maddess , Michael H. Reutershan , Yves Ducharme , David J. Guerin , Kerrie Spencer , Christian Beaulieu , Vouy Linh Truong , Daniel Guay , Alan B. Northrup , Brandon M. Taoka , Jongwon Lim , Christian Fischer , John W. Butcher , Ryan D. Otte , Binyuan Sun , John Michael Ellis
IPC分类号： C07D471/04 , C07D401/14 , C07D413/14 , C07D409/14 , C07D403/14 , C07D403/12
CPC分类号： C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention provides novel pyrazole derivatives 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, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型吡唑衍生物，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，类风湿性关节炎和癌症。
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公开(公告)号：US09775839B2
公开(公告)日：2017-10-03
申请号：US15125373
申请日：2015-03-09
发明人： Michael D. Altman , Brandon Cash , John Michael Ellis , Matthew L. Maddess , Alan B. Northrup , Ryan D. Otte , Binyuan Sun
IPC分类号： A61K31/497 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , A61K45/06 , C07D401/14 , C07D471/04 , C07D491/056
CPC分类号： A61K31/497 , A61K45/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X 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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公开(公告)号：US09487504B2
公开(公告)日：2016-11-08
申请号：US14409147
申请日：2013-06-18
发明人： Jongwon Lim , Michael H. Reutershan , John Michael Ellis , Kaleen Konrad Childers , Anthony Donofrio , Michael D. Altman , Andrew M. Haidle , Anna Zabierek , Matthew Christopher , Jonathan Grimm , Jason Burch , Maria Emilia Di Francesco , Alessia Petrocchi , Christian Beaulieu , Vouy Linh Truong , Alan B. Northrup , Marc Blouin
IPC分类号： C07D403/12 , C07D403/14 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention provides novel imidazole analogs 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, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型咪唑类似物，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，类风湿性关节炎和癌症。
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公开(公告)号：US20150175575A1
公开(公告)日：2015-06-25
申请号：US14409147
申请日：2013-06-18
发明人： Jongwon Lim , Michael H. Reutershan , John Michael Ellis , Kaleen Konrad Childers , Anthony Donofrio , Michael D. Altman , Andrew M. Haidle , Anna Zabierek , Matthew Christopher , Jonathan Grimm , Jason Burch , Maria Emilia Di Francesco , Alessia Petrocchi , Christian Beaulieu , Vouy Linh Truong , Alan B. Northrup , Marc Blouin
IPC分类号： C07D403/12 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14
摘要： The present invention provides novel imidazole analogs 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, rheumatoid arthritis, and cancer.
摘要翻译： 本发明提供了式I的新型咪唑类似物，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，类风湿性关节炎和癌症。
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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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8.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：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：US09745295B2
公开(公告)日：2017-08-29
申请号：US14786464
申请日：2014-04-22
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： A61K31/4439 , A61K31/53 , A61K31/501 , A61K31/497 , A61K31/506 , C07D417/12 , C07D417/14
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).
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