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公开(公告)号：US20150266897A1
公开(公告)日：2015-09-24
申请号：US14638733
申请日：2015-04-03
Applicant: Merck Sharp & Dohme Corp. , MSD Italia S.R.L.
Inventor： Nigel J. Liverton , Vincenzo Summa , Maria Emilia Di Francesco , Marco Ferrara , Kevin F. Gilbert , Steven Harper , John A. McCauley , Charles J. McIntyre , Alessia Petrocchi , Marco Pompei , Joseph J. Romano , Michael T. Rudd , John W. Butcher , M. Katharine Holloway
IPC: C07D498/22 , A61K31/437 , A61K31/439 , C07D498/08 , A61K31/407 , A61K31/4192 , C07D498/18 , A61K45/06
CPC classification number: C07D498/22 , A61K31/407 , A61K31/4192 , A61K31/437 , A61K31/439 , A61K38/00 , A61K45/06 , C07D498/08 , C07D498/18 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/0812
Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS3蛋白酶抑制剂及其合成及其用于治疗或预防HCV感染的用途的式（I）的大环化合物。
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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
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: C07D471/04 , C07D401/14 , C07D413/14 , C07D409/14 , C07D403/14 , C07D403/12
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：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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Patent Agency Ranking
公开(公告)号：US09096598B2
公开(公告)日：2015-08-04
申请号：US14349377
申请日：2012-09-28
Applicant: Merck Sharp & Dohme Corp.
Inventor： John W. Butcher , David Witter , Christopher Dinsmore , June Kim , John Hendrix , Raksha Archarya , Sean P. Ahearn , Joon Jung , Alexey Rivkin , Philip Jones
IPC: C07D401/10 , A61K31/437 , C07D471/04 , C07D519/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD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
Applicant: 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.
Inventor： 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: C07D417/12 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538
CPC classification number: C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
Abstract: 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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6.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
Applicant: 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.
Inventor： 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: C07D417/14 , C07D417/12 , A61K31/5377 , A61K31/506 , A61K31/538
CPC classification number: C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
Abstract: 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).
Abstract translation: 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：US20140303142A1
公开(公告)日：2014-10-09
申请号：US14349377
申请日：2012-09-28
Applicant: MERCK SHARP & DOHME CORP
Inventor： John W. Butcher , David Witter , Christopher Dinsmore , June Kim , John Hendrix , Raksha Acharya , Sean P. Ahearn , Joon Jung , Alexey Rivkin , Philip Jones
IPC: C07D471/04
CPC classification number: C07D471/04 , C07D519/00
Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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8.发明申请2-Pyridyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors 有权含2-吡啶基羧酰胺的脾脏酪氨酸激酶（SYK）抑制剂公开(公告)号：US20140243336A1
公开(公告)日：2014-08-28
申请号：US14349551
申请日：2012-10-01
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Michael D. Altman , Corey E. Bienstock , John W. Butcher , Kaleen Konrad Childers , Maria Emilia Di Francesco , Anthony Donofrio , John Michael Ellis , Christian Fischer , Andrew M. Haidle , James P. Jewell , Sandra Lee Knowles , Alan B. Northrup , Ryan D. Otte , Scott L. Peterson , Graham Frank Smith
IPC: C07D401/14 , A61K31/444 , C07D405/14 , C07D487/04 , A61K31/506 , C07D409/14 , A61K31/5377 , A61K31/519 , A61K31/496 , A61K31/4439 , C07D213/81 , A61K31/5025
CPC classification number: A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D213/81 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B 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: 本发明提供了具有式（I）的某些含2-吡啶甲酰胺的化合物或其药学上可接受的盐，其中A和B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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