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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：US20180244712A1
公开(公告)日：2018-08-30
申请号：US15886568
申请日：2018-02-01
发明人： Michael D. Altman , Brian Andresen , Wonsuk Chang , Matthew Lloyd Childers , Jared N. Cumming , Andrew Marc Haidle , Timothy J. Henderson , James P. Jewell , Rui Liang , Jongwon Lim , Hong Liu , Min Lu , Alan B. Northrup , Ryan D. Otte , Tony Siu , Benjamin Wesley Trotter , Quang T. Truong , Shawn P. Walsh , Kake Zhao
IPC分类号： C07H21/04 , C07H21/02 , C07H21/00 , C07H19/23 , C07H19/20 , A61K39/39 , A61K31/7084 , A61K31/708 , A61K31/7076 , A61K31/7064 , A61K31/706
摘要： A class of polycyclic compounds of general formula (I), of general formula (I′), or of general formula (I″), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a 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：US09969749B2
公开(公告)日：2018-05-15
申请号：US15515383
申请日：2015-09-25
发明人： 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分类号： 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分类号： 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
摘要： 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：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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35.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
发明人： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC分类号： 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分类号： 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
摘要： 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.
摘要翻译： 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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36.发明申请公开(公告)号：US20150353535A1
公开(公告)日：2015-12-10
申请号：US14653488
申请日：2013-12-19
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Kaleen Konrad Childers , Maria Emilia Di Francesco , John Michael Ellis , Andrew M. Haidle , Yuan Liu , Alan B. Northrup , Brendan O'Boyle , Ryan D. Otte , Michael H. Reutershan , Dilrukshi Vitharana , Hyun Chong Woo
IPC分类号： C07D417/14 , A61K31/444
CPC分类号： C07D417/14 , A61K31/444 , A61K45/06
摘要： The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript 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： 本发明提供了式（I）（I）的某些噻唑取代的氨基吡啶化合物或其药学上可接受的盐，其中R1，R2，R3，R4，R5，R6，Cy和下标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：US20150232428A1
公开(公告)日：2015-08-20
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 , C07D239/47 , A61K31/506 , C07D403/12 , A61K31/505 , C07D401/12
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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38.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
发明人： Andrew M. Haidle , Michael D. Altman , Solomon D. Kattar , Matthew Christopher , John Michael Ellis , Christian Fischer , Alan B. Northrup , Kaleen Konrad Childers
IPC分类号： 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分类号： 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
摘要： 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.
摘要翻译： 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：US20150148327A1
公开(公告)日：2015-05-28
申请号：US14409151
申请日：2013-06-17
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译： 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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40.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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译： 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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