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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
Applicant: Merck Sharp & Dohme Corp. , Merck Canada Inc.
Inventor： 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: A61K31/4439 , A61K31/53 , A61K31/501 , A61K31/497 , A61K31/506 , C07D417/12 , C07D417/14
CPC classification number: C07D417/14 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D417/12
Abstract: 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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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：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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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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Patent Agency Ranking
公开(公告)号：US09969749B2
公开(公告)日：2018-05-15
申请号：US15515383
申请日：2015-09-25
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Michael D. Altman , Brian M. Andresen , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. MacLean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Luis Torres
IPC: C07D498/04 , A61K45/06 , A61K31/517 , C07D403/04 , C07D239/94 , C07D401/04 , A61K31/5377 , C07D405/14 , C07D401/14 , C07D413/04 , C07D405/04 , C07D471/04 , A61K31/5383 , C07D491/048 , C07D417/04 , C07D409/04
CPC classification number: C07D498/04 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K45/06 , A61P37/00 , C07D239/94 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/048 , A61K2300/00
Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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7.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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公开(公告)号：US09932350B2
公开(公告)日：2018-04-03
申请号：US15515377
申请日：2015-09-25
Applicant: MERCK SHARP & DOHME CORP. , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
Inventor： Michael D. Altman , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
IPC: C07D491/08 , C07D239/94 , A61K31/517 , A61K45/06 , C07D239/88 , A61K31/5377 , C07D403/12 , C07D401/12 , C07D413/12 , A61K31/538 , C07D491/052 , A61K31/5386 , C07D491/048 , A61K31/55 , C07D405/12
CPC classification number: C07D491/08 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5386 , A61K31/55 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D491/048 , C07D491/052 , C07D498/08 , A61K2300/00
Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：US09926330B2
公开(公告)日：2018-03-27
申请号：US15515396
申请日：2015-09-25
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Michael D. Altman , Jason D. Brubaker , Matthew L. Childers , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Solomon D. Kattar , Charles A. Lesburg , Jongwon Lim , John K. F. MacLean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith
IPC: C07D491/107 , A61K31/517 , C07D239/94 , A61K31/5377 , C07D403/12 , C07D401/12 , C07D405/12 , C07D409/12 , A61K31/541 , C07D417/12
CPC classification number: C07D491/107 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , A61P19/00 , A61P29/00 , A61P35/00 , C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K2300/00
Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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公开(公告)号：US09943516B2
公开(公告)日：2018-04-17
申请号：US15515388
申请日：2015-09-25
Applicant: MERCK SHARP & DOHME CORP.
Inventor： Michael D. Altman , Brian M. Andresen , Jason D. Brubaker , Anthony Donofrio , Thierry Fischmann , Craig R. Gibeau , Charles A. Lesburg , Jongwon Lim , John K. F. Maclean , Umar F. Mansoor , Alan B. Northrup , John M. Sanders , Graham F. Smith , Luis Torres
IPC: A61K31/517 , C07D405/04 , A61K45/06 , C07D239/94
CPC classification number: A61K31/517 , A61K45/06 , A61P29/00 , A61P35/00 , C07D239/94 , C07D405/04 , A61K2300/00
Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
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