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1.发明申请公开(公告)号：US20160311813A1
公开(公告)日：2016-10-27
申请号：US15105411
申请日：2014-12-15
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Alan B. NORTHUP , Michael D. ALTMAN , MERCK SHARP & DOHME CORP.
IPC分类号： C07D417/12 , A61K31/5377 , A61K31/433 , A61K31/427 , A61K45/06
CPC分类号： C07D417/12 , A61K31/427 , A61K31/433 , A61K31/5377 , A61K45/06
摘要： The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, 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).
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公开(公告)号：US08735417B2
公开(公告)日：2014-05-27
申请号：US13515941
申请日：2010-12-16
申请人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号： A61K31/506 , C07D417/02
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
摘要： The present invention provides novel pyrimidine amines 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 and rheumatoid arthritis.
摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，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和类风湿性关节炎。
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公开(公告)号：US20130090309A1
公开(公告)日：2013-04-11
申请号：US13704484
申请日：2012-04-30
申请人： Eric Thomas Romeo , Michelle R. Machacek , Benjamin Wesley Trotter , Thomas Allen Miller , Brian Michael Andresen , Neville John Anthony , Brandon M. Taoka , Yuan Liu
发明人： Eric Thomas Romeo , Michelle R. Machacek , Benjamin Wesley Trotter , Thomas Allen Miller , Brian Michael Andresen , Neville John Anthony , Brandon M. Taoka , Yuan Liu
IPC分类号： A61K31/444 , A61K31/496 , A61K45/06 , A61K31/675 , C07F5/02 , A61K31/69 , C07D417/14 , C07F9/6558
CPC分类号： A61K31/444 , A61K31/496 , A61K31/675 , A61K31/69 , A61K45/06 , C07D277/04 , C07D417/14 , C07F5/025 , C07F9/65583
摘要： The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n 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： 本发明提供某些含有氨基 - 吡啶的式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和n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：US20110166129A1
公开(公告)日：2011-07-07
申请号：US12988705
申请日：2009-04-09
IPC分类号： A61K31/4439 , C07D417/12 , C07D417/14 , A61K31/5377 , A61K31/541 , C07D471/04 , A61K31/437 , A61K31/501 , A61P35/00
CPC分类号： C07D417/14 , C07D417/12 , C07D471/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗骨髓增生性疾病或癌症的患者来抑制JAK1，JAK2，JAK3，TYK2和PDK1的活性的方法。
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公开(公告)号：US09586931B2
公开(公告)日：2017-03-07
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： A61K9/10 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D498/04 , C07D413/14 , C07D239/42 , A61K9/00 , A61K9/20 , A61K9/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives 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： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物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：US20150239866A1
公开(公告)日：2015-08-27
申请号：US14431895
申请日：2013-09-24
申请人： Michelle R. MACHACEK , Eric T. ROMEO , Solomon D. KATTAR , Matthew CHRISTOPHER , Michael D. ALTMAN , Alan B. NORTHRUP , John Michael ELLIS , Brendan O BOYLE , Anthony DONOFRIO , Jonathan GRIMM , Michael H. REUTERSHAN , Kaleen Konrad CHILDERS , Ryan D. OTTE , Brandon CASH , Yves DUCHARME , Andrew M. HAIDLE , Kerrie SPENCER , Dilrukshi VITHARANA , Lingyun WU , Li ZHANG , Peng ZHANG , Christian BEAULIEU , Daniel GUAY
发明人： Michelle R. Machacek , Eric T. Romeo , Solomon D. Kattar , Matthew Christopher , Michael D. Altman , Alan B. Northrup , John Michael Ellis , Brendan O'Boyle , Anthony Donofrio , Jonathan Grimm , Michael H. Reutershan , Kaleen Konrad Childers , Ryan D. Otte , Brandon Cash , Yves Ducharme , Andrew M. Haidle , Kerrie Spencer , Dilrukshi Vitharana , Lingyun Wu , Li Zhang , Peng Zhang , Christian Beaulieu , Daniel Guay
IPC分类号： C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/04 , C07D409/14 , C07D417/14
CPC分类号： C07D401/14 , A61K9/0019 , A61K9/0073 , A61K9/0075 , A61K9/10 , A61K9/2027 , A61K9/4858 , C07D239/42 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D498/04
摘要： Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives 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： 提供式I的三唑衍生物，其是脾脏酪氨酸激酶和药物组合物的有效抑制剂。 三唑衍生物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：US08796310B2
公开(公告)日：2014-08-05
申请号：US13704484
申请日：2012-04-30
申请人： Eric Thomas Romeo , Michelle R. Machacek , Benjamin Wesley Trotter , Thomas Allen Miller , Brian Michael Andresen , Neville John Anthony , Brandon M. Taoka , Yuan Liu
发明人： Eric Thomas Romeo , Michelle R. Machacek , Benjamin Wesley Trotter , Thomas Allen Miller , Brian Michael Andresen , Neville John Anthony , Brandon M. Taoka , Yuan Liu
IPC分类号： A61K31/444 , C07D277/04
CPC分类号： A61K31/444 , A61K31/496 , A61K31/675 , A61K31/69 , A61K45/06 , C07D277/04 , C07D417/14 , C07F5/025 , C07F9/65583
摘要： The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n 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： 本发明提供某些含有氨基 - 吡啶的式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和n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：US08431569B2
公开(公告)日：2013-04-30
申请号：US12747030
申请日：2008-12-09
IPC分类号： C07D487/02 , A61K31/503
CPC分类号： C07D471/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：US20120309735A1
公开(公告)日：2012-12-06
申请号：US13515941
申请日：2010-12-16
申请人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
发明人： Michael D. Altman , Kenneth L. Arrington , Jason Burch , Bernard Cote , Jean-Francois Fournier , Jacques Yves Gauthier , Solomon Kattar , Sandra Lee Knowles , Jongwon Lim , Michelle R. Machacek , Alan B. Northrup , Michael H. Reutershan , Joel S. Robichaud , Adam J. Schell , Kerrie B. Spencer
IPC分类号： A61K31/506 , C07D417/12 , C07D417/14 , C07D471/04 , A61P19/02 , A61K31/551 , A61P11/06 , A61P11/00 , A61P29/00 , C07D471/10 , A61K31/5377
CPC分类号： C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10
摘要： The present invention provides novel pyrimidine amines 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 and rheumatoid arthritis.
摘要翻译： 本发明提供了新颖的式（I）嘧啶胺，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和类风湿性关节炎。
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10.发明申请Benzocycloheptapyridines as inhibitors of the receptor tyrosine kinase met 有权作为受体酪氨酸激酶抑制剂的苯并环庚三烯类化合物公开(公告)号：US20090197908A1
公开(公告)日：2009-08-06
申请号：US11921350
申请日：2006-06-22
申请人： Christopher J. Dinsmore , Ana Esther Gabarda Ortega , David J. Guerin , James P. Jewell , Jason D. Katz , Jongwon Lim , Michelle R. Machacek , Ryan D. Otte , Jonathan R. Young
发明人： Christopher J. Dinsmore , Ana Esther Gabarda Ortega , David J. Guerin , James P. Jewell , Jason D. Katz , Jongwon Lim , Michelle R. Machacek , Ryan D. Otte , Jonathan R. Young
IPC分类号： A61K31/4353 , C07D221/06 , A61P35/00
CPC分类号： C07D471/04 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D491/10 , C07D491/113 , C07F7/1804
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病和用于抑制受体酪氨酸激酶MET的5H-苯并[4,5]环庚并[1,2-b]吡啶化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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