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公开(公告)号：US11230547B2
公开(公告)日：2022-01-25
申请号：US16764448
申请日：2018-12-12
Applicant: Merck Sharp & Dohme Corp.
Inventor： Meredeth A. McGowan , Jason D. Katz , Matthew Christopher , Hua Zhou , David James Witter , Chaomin Li , John Lampe , Joey L. Methot , Abdelghani A. Achab , Xavier Fradera , Shimin Xu
IPC: C07D487/08 , C07D519/00 , C07D403/14
Abstract: The instant invention provides compounds of formulas Ia and Ib 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：US09353066B2
公开(公告)日：2016-05-31
申请号：US14422419
申请日：2013-08-15
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: C07D239/42 , C07D403/12 , A61K31/506 , A61K31/505 , C07D401/12 , C07D239/47
CPC classification number: C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
Abstract: 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).
Abstract translation: 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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3.发明授权Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors 有权取代的二嗪和三嗪脾脏酪氨酸激酶（Syk）抑制剂公开(公告)号：US09416111B2
公开(公告)日：2016-08-16
申请号：US14409200
申请日：2013-06-17
Applicant: Merck Sharp & Dohme Corp.
Inventor： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC: A61K31/506 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D417/14 , C07D239/42 , A61K45/06 , C07D413/14 , C07D409/14 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , C07D239/47 , C07D239/48 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/12
CPC classification number: C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
Abstract: The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, 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) kinase.
Abstract translation: 本发明提供了式（I）（I）的某些取代的二嗪和三嗪化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy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）激酶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
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: C07D239/42 , C07D239/47 , A61K31/506 , C07D403/12 , A61K31/505 , C07D401/12
CPC classification number: C07D239/42 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/47 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/10
Abstract: 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).
Abstract translation: 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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5.发明申请SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINEASE (SYK) INHIBITORS 有权取代的DIAZINE和TRIAZINE SPLEEN TYROSINE KINEASE（SYK）抑制剂公开(公告)号：US20150166486A1
公开(公告)日：2015-06-18
申请号：US14409200
申请日：2013-06-17
Applicant: Merck Sharp & Dohme Corp.
Inventor： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC: C07D239/42 , C07D239/47 , C07D239/48 , C07D403/04 , C07D403/12 , A61K31/55 , C07D405/12 , A61K31/541 , C07D401/12 , C07D413/12 , A61K31/5377 , A61K31/551 , A61K31/506 , C07D409/12
CPC classification number: C07D239/42 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K45/06 , C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
Abstract: The invention provides certain substituted diazine and triazine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, 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) kinase.
Abstract translation: 本发明提供了式（I）（I）的某些取代的二嗪和三嗪化合物或其药学上可接受的盐，其中R1，R2，R3，R4，Rcy，Cy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）激酶介导的疾病或病症的方法。
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Patent Agency Ranking
公开(公告)号：US20150148327A1
公开(公告)日：2015-05-28
申请号：US14409151
申请日：2013-06-17
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Andrew M. Haidle , Sandra Lee Knowles , Solomon D. Kattar , Denis Deschenes , Jason Burch , Joel Robichaud , Matthew Christopher , Michael D. Altman , James P. Jewell , Alan B. Northrup , Marc Blouin , John Michael Ellis , Hua Zhou , Christian Fischer , Adam J. Schell , Michael H. Reutershan , Brandon M. Taoka , Anthony Donofrio , Joel Robichaud
IPC: C07D401/12 , A61K31/506 , C07D471/04 , C07D498/04 , A61K31/5383 , A61K31/551 , C07D405/14 , C07D401/14 , C07D471/10 , C07D491/107 , C07D491/113 , C07D417/14 , C07D413/14 , C07D487/04 , A61K31/5377
CPC classification number: C07D401/12 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04 , A61K2300/00
Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, 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) kinase.
Abstract translation: 本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy，Cy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）激酶介导的疾病或病症的方法。
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公开(公告)号：US09376418B2
公开(公告)日：2016-06-28
申请号：US14409151
申请日：2013-06-17
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Andrew M. Haidle , Sandra Lee Knowles , Solomon D. Kattar , Denis Deschenes , Jason Burch , Joel Robichaud , Matthew Christopher , Michael D. Altman , James P. Jewell , Alan B. Northrup , Marc Blouin , John Michael Ellis , Hua Zhou , Christian Fischer , Adam J. Schell , Michael H. Reutershan , Brandon M. Taoka , Anthony Donofrio
IPC: C07D401/12 , C07D401/14 , A61K31/506 , A61K31/505 , A61K45/06 , A61K31/5377 , A61K31/5383 , A61K31/551 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/107 , C07D491/113 , C07D498/04 , C07D491/08 , C07D409/14 , C07D487/10
CPC classification number: C07D401/12 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/551 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D491/08 , C07D491/107 , C07D491/113 , C07D498/04 , A61K2300/00
Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, 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) kinase.
Abstract translation: 本发明提供了式（I）的某些取代的吡啶或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Rcy，Cy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）激酶介导的疾病或病症的方法。
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公开(公告)号：US09242984B2
公开(公告)日：2016-01-26
申请号：US14409133
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： Michelle R. Machacek , Michael D. Altman , Eric T. Romeo , Dilrukshi Vitharana , Brandon Cash , Tony Siu , Hua Zhou , 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: C07D401/00 , A61K31/00 , C07D471/04 , C07D403/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D403/14 , C07D409/14
CPC classification number: C07D471/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
Abstract: 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.
Abstract translation: 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：US09487504B2
公开(公告)日：2016-11-08
申请号：US14409147
申请日：2013-06-18
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: C07D403/12 , C07D403/14 , C07D401/14
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14
Abstract: 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.
Abstract translation: 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
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: C07D403/12 , C07D401/14
CPC classification number: C07D403/12 , C07D401/14 , C07D403/14
Abstract: 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.
Abstract translation: 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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