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公开(公告)号:US08722692B2
公开(公告)日:2014-05-13
申请号:US13386645
申请日:2010-07-30
申请人: Jianwei Che , Qiang Ding , Xiaohui He , Hong Liu , Yahua Liu , Pierre-Yves Michellys , Barun Okram , Xu Wu , Kunyong Yang , Xuefeng Zhu
发明人: Jianwei Che , Qiang Ding , Xiaohui He , Hong Liu , Yahua Liu , Pierre-Yves Michellys , Barun Okram , Xu Wu , Kunyong Yang , Xuefeng Zhu
IPC分类号: A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00
CPC分类号: C07D471/04
摘要: Provided herein are a novel class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.
摘要翻译: 本文提供了一类新的式(I)化合物,包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的Syk激酶活性相关的疾病或病症的方法。
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公开(公告)号:US20120184526A1
公开(公告)日:2012-07-19
申请号:US13386645
申请日:2010-07-30
申请人: Jianwei Che , Qiang Ding , Xiaohui He , Hong Liu , Yahua Liu , Pierre-Yves Michellys , Barun Okram , Xu Wu , Kunyong Yang , Xuefeng Zhu
发明人: Jianwei Che , Qiang Ding , Xiaohui He , Hong Liu , Yahua Liu , Pierre-Yves Michellys , Barun Okram , Xu Wu , Kunyong Yang , Xuefeng Zhu
IPC分类号: A61K31/5377 , A61K31/519 , A61P35/00 , A61P37/08 , A61P29/00 , A61P19/02 , C07D471/04 , A61K31/496
CPC分类号: C07D471/04
摘要: Provided herein are a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.
摘要翻译: 本文提供了一类新颖的化合物,包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的Syk激酶活性相关的疾病或病症的方法。
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公开(公告)号:US20110190264A1
公开(公告)日:2011-08-04
申请号:US12936193
申请日:2009-04-03
申请人: Tao Jiang , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Xuefeng Zhu
发明人: Tao Jiang , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Xuefeng Zhu
IPC分类号: A61K31/5377 , C07D403/14 , A61K31/53 , C12N9/99 , C07D413/14 , A61P35/00
CPC分类号: C07D471/04
摘要: The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.
摘要翻译: 本发明涉及具有式(1)或(2)的三嗪和嘧啶衍生物以及使用这些化合物的方法。 例如,本发明的化合物可用于治疗,改善或预防响应于间变性淋巴瘤激酶(ALK)活性,c-ros致癌基因(ROS),胰岛素样生长因子(IGF-1R) ,和/或胰岛素受体(InsR)或其组合。
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公开(公告)号:US08518931B2
公开(公告)日:2013-08-27
申请号:US12936193
申请日:2009-04-03
申请人: Tao Jiang , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Xuefeng Zhu
发明人: Tao Jiang , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Xuefeng Zhu
IPC分类号: C07D401/12 , C07D487/04 , A61K31/53 , A61P35/00
CPC分类号: C07D471/04
摘要: The invention relates to triazine and pyrimidine derivatives having Formula (1) or (2), and methods for using such compounds. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) or a combination thereof.
摘要翻译: 本发明涉及具有式(1)或(2)的三嗪和嘧啶衍生物以及使用这些化合物的方法。 例如,本发明的化合物可用于治疗,改善或预防响应于间变性淋巴瘤激酶(ALK)活性,c-ros致癌基因(ROS),胰岛素样生长因子(IGF-1R) ,和/或胰岛素受体(InsR)或其组合。
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公开(公告)号:US08592432B2
公开(公告)日:2013-11-26
申请号:US12936199
申请日:2009-04-03
申请人: Bei Chen , Tao Jiang , Thomas H. Marsilje , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Zhaobo Gao , Yonghui Ge , Chen Huang , Yuncheng Li , Xuefeng Zhu
发明人: Bei Chen , Tao Jiang , Thomas H. Marsilje , Pierre-Yves Michellys , Truc Ngoc Nguyen , Wei Pei , Baogen Wu , Zhaobo Gao , Yonghui Ge , Chen Huang , Yuncheng Li , Xuefeng Zhu
IPC分类号: A61K31/506 , A61K31/5377 , C07D239/42 , C07D239/30 , C07D295/108 , C07D487/04 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号: C07D239/48 , C07D403/12 , C07D403/14 , C07D487/04
摘要: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.
摘要翻译: 本发明提供新颖的嘧啶衍生物及其药物组合物,以及使用这些化合物的方法。 例如,本发明的嘧啶衍生物可用于治疗,改善或预防对间变性淋巴瘤激酶(ALK)活性,c-ros致癌基因(ROS),胰岛素样生长因子(IGF-1R )和/或胰岛素受体(InsR)或其组合。
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公开(公告)号:US20120165310A1
公开(公告)日:2012-06-28
申请号:US13394534
申请日:2010-09-10
申请人: Bei Chen , Robin Alec Fairhurst , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Jiang Songchun , Wenshuo Lu , Thomas H. Marsilje, III , Clive McCarthy , Pierre-Yves Michellys , Frederic Stauffer , Stefan Stutz , Andrea Vaupel
发明人: Bei Chen , Robin Alec Fairhurst , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Jiang Songchun , Wenshuo Lu , Thomas H. Marsilje, III , Clive McCarthy , Pierre-Yves Michellys , Frederic Stauffer , Stefan Stutz , Andrea Vaupel
IPC分类号: A61K31/519 , A61K31/541 , C07D493/08 , A61K31/5377 , A61K31/554 , A61P19/00 , A61K31/5386 , C07D495/08 , A61P35/00 , A61P11/00 , A61P1/16 , C07D487/04 , C07D487/08
CPC分类号: C07D487/04 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2059 , A61K9/4858
摘要: The invention relates to compounds of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; such compounds as a medicament; such compounds for the treatment of a proliferative disease.
摘要翻译: 本发明涉及式I化合物,其中取代基如说明书中所定义; 制备这些化合物的方法; 包含这些化合物的药物组合物; 诸如药物的化合物; 这种化合物用于治疗增殖性疾病。
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公开(公告)号:US20110224185A1
公开(公告)日:2011-09-15
申请号:US13113988
申请日:2011-05-23
申请人: Phillip B. Alper , Mihai Azimioara , Christopher Cow , Robert Epple , Songchun Jiang , Gerald Lelais , Pierre-Yves Michellys , Daniel Mutnick , Victor Nikulin , Lucas Westcott-Baker
发明人: Phillip B. Alper , Mihai Azimioara , Christopher Cow , Robert Epple , Songchun Jiang , Gerald Lelais , Pierre-Yves Michellys , Daniel Mutnick , Victor Nikulin , Lucas Westcott-Baker
IPC分类号: A61K31/397 , C07D405/14 , A61K31/506 , C07D401/14 , C07D401/12 , A61K31/4545 , A61K31/497 , A61K31/496 , A61K31/551 , C07D487/04 , A61K31/4985 , A61K31/501 , C07D413/14 , A61K31/5377 , A61P3/10 , A61P9/00 , A61P19/00 , A61P13/12 , A61P3/06 , A61P17/00 , C12N5/02
CPC分类号: C07D401/10 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/14 , C07D487/04 , C07D491/048
摘要: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.
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公开(公告)号:US20110190259A1
公开(公告)日:2011-08-04
申请号:US13048636
申请日:2011-03-15
申请人: Pierre-Yves Michellys , Wei Pei , Thomas H. Marsilje , Bei Chen , Tetsuo Uno , Yunho Jin , Tao Jiang
发明人: Pierre-Yves Michellys , Wei Pei , Thomas H. Marsilje , Bei Chen , Tetsuo Uno , Yunho Jin , Tao Jiang
IPC分类号: A61K31/506 , C07D401/14 , C12N9/99 , C07D239/24 , C07D413/14 , A61K31/5377 , C07D403/02 , A61P25/00 , A61P37/06
CPC分类号: A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/74 , C07D239/48 , C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D451/02 , C07D453/02 , C07D471/04 , C07D473/16 , C07D487/04 , C07D487/08
摘要: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
摘要翻译: 本发明提供新颖的嘧啶和吡啶衍生物及其药物组合物,以及使用这些化合物的方法。 例如,本发明的嘧啶和吡啶衍生物可用于治疗,改善或预防响应于间变性淋巴瘤激酶(ALK)活性,粘着斑激酶(FAK),ζ-链相关蛋白激酶70 (ZAP-70),胰岛素样生长因子(IGF-1R)或其组合。
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公开(公告)号:US20060166983A1
公开(公告)日:2006-07-27
申请号:US10541555
申请日:2003-12-31
申请人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz , Pierre-Yves Michellys
发明人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz , Pierre-Yves Michellys
IPC分类号: A61K31/5377 , A61K31/454 , A61K31/4439 , A61K31/405 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号: C07D209/08 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in (I) are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及一种通过使用结构式(I)的化合物调节过氧化物酶体增殖物激活受体的治疗方法。 (I)中的变量在本文中定义。 还包括化合物,制备化合物的方法和药物组合物。 据信本发明的化合物在治疗和预防X综合征,II型糖尿病,高血糖症,高脂血症,肥胖,凝血病,高血压,动脉粥样硬化以及与X综合征和心血管疾病相关的其它疾病方面是有效的。
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公开(公告)号:US06825222B2
公开(公告)日:2004-11-30
申请号:US10434425
申请日:2003-05-07
申请人: Dawn A. Brooks , Christopher J. Rito , Anthony J. Shuker , Samuel J. Dominianni , Alan M. Warshawsky , Lynn S. Gossett , Donald P. Matthews , David A. Hay , Robert J. Ardecky , Pierre-Yves Michellys , John S. Tyhonas
发明人: Dawn A. Brooks , Christopher J. Rito , Anthony J. Shuker , Samuel J. Dominianni , Alan M. Warshawsky , Lynn S. Gossett , Donald P. Matthews , David A. Hay , Robert J. Ardecky , Pierre-Yves Michellys , John S. Tyhonas
IPC分类号: A61K31425
CPC分类号: C07D413/10 , C07D263/32 , C07D277/24
摘要: The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and R6 is H, a C1-C4 alkyl, or an aminoalkyl.
摘要翻译: 本发明涉及由结构式I表示的化合物及其药学上可接受的盐,溶剂合物和水合物及其制备方法,使用方法和具有由结构式I表示的化合物的药物组合物及其药学上可接受的盐,溶剂化物和水合物: 在结构式Ⅰ中,n为2,3或4; V为O或S; W是O,S或SO 2; R1是H,C1-C4烷基,苯基或三氟甲基; R 2各自独立地为H,C 1 -C 6烷基,芳基-C 1 -C 6烷基,环烷基-C 1 -C 4烷基,芳基,环烷基,或与它们所连接的苯基一起形成萘基或1 ,2,3,4-四氢萘基; R 3各自独立地为H,C 1 -C 6烷基,芳基-C 1 -C 6烷基,环烷基-C 1 -C 4烷基,芳基或环烷基; R 4各自独立地为H,C 1 -C 4烷基,芳基或苄基; R5各自独立地为H,取代或未取代的芳基或杂芳基,条件是至少一个R 5为取代或未取代的芳基或取代或未取代的杂芳基; 并且R 6是H,C 1 -C 4烷基或氨基烷基。
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