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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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公开(公告)号：US20090270511A1
公开(公告)日：2009-10-29
申请号：US12439323
申请日：2007-09-07
IPC分类号： A61K31/165 , C07C255/46
CPC分类号： C07C317/48 , C07C2601/02
摘要： The present invention provides compounds of formula (I) which are prodrugs of inhibitors of cathepsin S and as such are useful in the prevention and treatment of cathepsin S dependent diseases and conditions including, but not limited to, chronic obstructive pulmonary disease (COPD) and pain.
摘要翻译： 本发明提供式（I）化合物，其为组织蛋白酶S抑制剂的前药，因此可用于预防和治疗组织蛋白酶S依赖性疾病和病症，包括但不限于慢性阻塞性肺病（COPD）和 疼痛。
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13.发明授权Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) 失效作为蛋白酪氨酸磷酸酶1B（PTP-1B）的抑制剂的膦酸联芳衍生物公开(公告)号：US06486141B2
公开(公告)日：2002-11-26
申请号：US09745199
申请日：2000-12-21
申请人： Cheuk Kun Lau , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Chun Sing Li , Patrick Roy , Michel Therien , Zhaoyin Wang
发明人： Cheuk Kun Lau , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Chun Sing Li , Patrick Roy , Michel Therien , Zhaoyin Wang
IPC分类号： A61K31663
CPC分类号： C07F9/65583 , C07F9/65188
摘要： The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.
摘要翻译： 本发明包括作为PTP-1B酶抑制剂的由式I表示的新一类化合物。本发明还包括治疗或预防PTP-1B介导的疾病的药物组合物和方法，包括糖尿病，肥胖症和糖尿病相关病症 。
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公开(公告)号：US5767291A
公开(公告)日：1998-06-16
申请号：US738144
申请日：1996-10-25
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
摘要： The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
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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
申请人： 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.
发明人： 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分类号： C07D417/12 , C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： 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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16.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
申请人： 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.
发明人： 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分类号： C07D417/14 , C07D417/12 , A61K31/5377 , A61K31/506 , A61K31/538
CPC分类号： C07D417/14 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D417/12
摘要： 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).
摘要翻译： 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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17.发明授权Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) 失效作为蛋白酪氨酸磷酸酶1B（PTP-1B）抑制剂的膦酸衍生物公开(公告)号：US06486142B2
公开(公告)日：2002-11-26
申请号：US09745211
申请日：2000-12-21
申请人： Yves Leblanc , Claude Dufresne , Jacques Yves Gauthier , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michel Therien , John Scheigetz , Zhaoyin Wang
发明人： Yves Leblanc , Claude Dufresne , Jacques Yves Gauthier , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michel Therien , John Scheigetz , Zhaoyin Wang
IPC分类号： C07F938
CPC分类号： C07F9/6539 , C07F9/3882 , C07F9/4075 , C07F9/4087 , C07F9/65188 , C07F9/65318
摘要： The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
摘要翻译： 本发明包括由式I表示的新型化合物，其是PTP-1B酶的抑制剂。本发明还包括治疗或预防PTP-1B介导的疾病的药物组合物和方法，包括糖尿病，肥胖症和与 糖尿病。
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18.发明授权Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates 失效含有两个邻位取代的芳族膦酸酯的蛋白酪氨酸磷酸酶1B（PTP-1B）抑制剂公开(公告)号：US06448429B1
公开(公告)日：2002-09-10
申请号：US09745220
申请日：2000-12-21
IPC分类号： C07F940
CPC分类号： C07F9/3856
摘要： The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
摘要翻译： 本发明包括由式I表示的新型化合物，其是PTP-1B酶的抑制剂。本发明还包括药物组合物和治疗或预防PTP-1B介导的疾病的药物组合物和方法，包括糖尿病，肥胖症和糖尿病相关 疾病
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19.发明授权Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases 失效使用环氧合酶抑制剂治疗神经变性疾病
公开(公告)号：US5840746A
公开(公告)日：1998-11-24
申请号：US926291
申请日：1997-09-05
申请人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
发明人： Yves Ducharme , Jacques Yves Gauthier , Petpiboon Prasit , Yves Leblanc , Zhaoyin Wang , Serge Leger , Michel Therien
IPC分类号： A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/08 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C323/49 , C07D209/26 , C07D275/02 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , A61K31/38 , A61K31/27 , A61K31/34
CPC分类号： C07D275/02 , A61K31/10 , A61K31/341 , A61K31/381 , A61K31/425 , A61K31/426 , C07C311/08 , C07C311/29 , C07C311/46 , C07C311/49 , C07C317/24 , C07C323/49 , C07D209/26 , C07D277/26 , C07D307/38 , C07D307/58 , C07D333/18 , C07D333/38 , C07D405/04 , C07C2101/08 , C07C2102/08
摘要： The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: ##STR1##
摘要翻译： 本发明提供治疗神经变性疾病，特别是阿尔茨海默病的方法，其包括向有需要的人施用治疗有效量的非类固醇COX-II抑制剂。 尽管可以使用大范围的COX-II抑制剂，但优选使用式I的化合物：
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公开(公告)号：US20140243290A1
公开(公告)日：2014-08-28
申请号：US14255480
申请日：2014-04-17
申请人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
发明人： Michael D. Altman , Brian M. Andresen , Kenneth L. Arrington , Sathesh Bhat , Jason Burch , Kaleen Konrad Childers , Bernard Cote , Maria Emilia Di Francesco , Anthony Donofrio , Kristina Dupont-Gaudet , John Michael Ellis , Christian Fischer , Jean-Francois Fournier , Jacques Yves Gauthier , Jonathan Grimm , Daniel Guay , David Joseph Guerin , Andrew M. Haidle , Solomon D. Kattar , Sandra Lee Knowles , Chaomin Li , Jongwon Lim , Michelle R. Machacek , Matthew L. Maddess , Alan B. Northrup , Brendan M. O'Boyle , Ryan D. Otte , Alessia Petrocchi , Michael H. Reutershan , Joel S. Robichaud , Eric T. Romeo , Adam J. Schell , Tony Siu , Kerrie B. Spencer , Brandon M. Taoka , B. Wesley Trotter , Hyun Chong Woo , Hua Zhou
IPC分类号： C07D417/12 , C07D495/04 , C07D451/06 , C07F9/6558 , C07D471/08 , C07D487/04 , C07D471/04 , C07D417/14 , C07D491/08
CPC分类号： C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D491/08 , C07D495/04 , C07F9/65583
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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