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公开(公告)号：US08163763B2
公开(公告)日：2012-04-24
申请号：US12533935
申请日：2009-07-31
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F. T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/519 , C07D471/04
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I化合物，其包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，其可用于调节PIKK相关激酶信号传导，例如mTOR和用于治疗疾病（例如癌症）， 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US20100069357A1
公开(公告)日：2010-03-18
申请号：US12533935
申请日：2009-07-31
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Cuong Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/5377 , C07D487/04 , C07D471/04 , A61K31/55 , A61K31/553 , A61K31/519 , A61P35/00
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，其可用于调节PIKK相关激酶信号传导，例如mTOR，以及用于治疗疾病（例如癌症） 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US20120165313A1
公开(公告)日：2012-06-28
申请号：US13410246
申请日：2012-03-01
申请人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Coung Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
发明人： Philippe Bergeron , Frederick Cohen , Anthony Estrada , Michael F.T. Koehler , Kevin Hon Luen Lau , Coung Ly , Joseph P. Lyssikatos , Daniel Ortwine , Zhonghua Pei , Xianrui Zhao
IPC分类号： A61K31/553 , A61K31/5377 , C07D491/048 , A61K31/519 , C07D471/04 , A61P35/02 , A61K31/55 , C07D471/14 , C07D491/08 , C07D471/18 , A61P35/00 , C07D487/04 , A61K31/5386
CPC分类号： C07D471/18 , C07D471/14
摘要： Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
摘要翻译： 公开了式I化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐，其可用于调节PIKK相关激酶信号传导，例如mTOR，以及用于治疗疾病（例如癌症） 至少部分地由PIKK信号通路的失调（例如mTOR）介导。
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公开(公告)号：US08618107B2
公开(公告)日：2013-12-31
申请号：US13102720
申请日：2011-05-06
申请人： Antonio J. M. Barbosa , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J. M. Barbosa , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/50 , A61K31/501 , C07D487/00
CPC分类号： C07D519/00 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K31/551 , A61K45/06 , C07C69/65 , C07D209/52 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07F5/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。
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![5-Substituted-4-[(substituted phenyl) amino]-2-pyridone derivatives](/abs-image/US/2005/02/03/US20050026964A1/abs.jpg.150x150.jpg)
5.发明申请5-Substituted-4-[(substituted phenyl) amino]-2-pyridone derivatives 有权5-取代的-4 - [（取代的苯基）氨基] -2-吡啶酮衍生物公开(公告)号：US20050026964A1
公开(公告)日：2005-02-03
申请号：US10876100
申请日：2004-06-24
申请人： Shannon Black , Michael Kaufman , Daniel Ortwine , Mark Plummer , John Quin , Gordon Rewcastle , Aurash Shahripour , Julie Spicer , Christopher Whitehead
发明人： Shannon Black , Michael Kaufman , Daniel Ortwine , Mark Plummer , John Quin , Gordon Rewcastle , Aurash Shahripour , Julie Spicer , Christopher Whitehead
IPC分类号： A61P35/00 , C07D213/78 , C07D213/80 , C07D213/82 , C07D213/87 , C07D401/12 , C07D413/04 , A61K31/4439 , A61K31/44 , C07D213/72
CPC分类号： C07D213/78 , C07D213/80 , C07D213/82 , C07D213/87 , C07D401/12 , C07D413/04
摘要： The present invention relates to 5-substituted-4-(substituted)phenylamino-2-pyridone derivatives, pharmaceutical compositions and methods of use thereof.
摘要翻译： 本发明涉及5-取代-4-（取代的）苯基氨基-2-吡啶酮衍生物，药物组合物及其使用方法。
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公开(公告)号：US20120010191A1
公开(公告)日：2012-01-12
申请号：US13102720
申请日：2011-05-06
申请人： Antonio J.M. BARBOSA , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J.M. BARBOSA , Peter A. Blomgren , Kevin S. Currie , Ravi Krishnamoorthy , Jeffrey E. Kropf , Seung H. Lee , Scott A. Mitchell , Daniel Ortwine , Aaron C. Schmitt , Xiaojing Wang , Jianjun Xu , Wendy Young , Honglu Zhang , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/397 , A61K31/501 , C07D495/04 , A61K31/5025 , C07D487/04 , A61K31/551 , A61K31/4365 , C07D413/14 , A61K31/5377 , A61P29/00 , A61P19/02 , A61P9/00 , A61P35/00 , A61P37/06 , A61P11/06 , A61P25/00 , A61P11/00 , A61P17/06 , A61P35/02 , C07D401/14
CPC分类号： C07D519/00 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/5386 , A61K31/551 , A61K45/06 , C07C69/65 , C07D209/52 , C07D471/14 , C07D487/04 , C07D495/04 , C07D498/04 , C07F5/04
摘要： Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
摘要翻译： 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。
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公开(公告)号：US20110301145A1
公开(公告)日：2011-12-08
申请号：US13128726
申请日：2009-11-12
申请人： Antonio J.M. Barbosa JR. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey Kropf , Scott A. Mithchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J.M. Barbosa JR. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey Kropf , Scott A. Mithchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/5377 , C07D487/04 , C07D495/04 , C07D413/14 , C07D401/14 , C07D403/14 , C07D403/12 , C07D417/14 , C07D405/14 , C07D498/04 , A61K31/506 , A61K31/501 , A61K31/5383 , A61K31/55 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/08 , A61P19/08 , C12N5/071 , C12Q1/70 , G01N33/573 , C07D409/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译： 本文描述了抑制Btk的式I化合物。 描述了包含至少一种式I化合物的药物组合物以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体。 描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。 描述了确定样品中Btk的存在的方法。
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8.发明申请Modified Wee1, crystals of peptide: inhibitor complexes containing such modified Wee1, and methods of use thereof 审中-公开修饰的Wee1，含有这种修饰的Wee1的肽的结晶：抑制剂复合物及其使用方法公开(公告)号：US20050037476A1
公开(公告)日：2005-02-17
申请号：US10837652
申请日：2004-05-04
申请人： Edward Baker , Richard Booth , Alan Kraker , Daniel Ortwine , James Dickson , Ivan Ivanovic , Christopher Squire
发明人： Edward Baker , Richard Booth , Alan Kraker , Daniel Ortwine , James Dickson , Ivan Ivanovic , Christopher Squire
CPC分类号： C12N9/1205 , C07K2299/00 , C12Q1/485 , G01N33/6803 , G01N2333/91215 , G01N2500/00 , G16B15/00 , G16C20/50
摘要： Modified Wee1 peptides, polynucleotides encoding those peptides, and methods for purifying the peptides and crystallizing them as peptide: inhibitor complexes have been discovered. The three-dimensional structure of Wee1, including the ATP substrate binding site, and uses of this information in the design and screening of compounds that may associate with Wee1, or peptides structurally related thereto, have also been discovered.
摘要翻译： 已经发现修饰的Wee1肽，编码这些肽的多核苷酸，以及纯化肽并将其结晶为肽：抑制剂复合物的方法。 还发现了Wee1的三维结构，包括ATP底物结合位点，以及该信息在可能与Wee1相关的化合物的设计和筛选中的用途，或与其结构相关的肽。
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9.发明申请Method of determining potential allosterically-binding matrix metalloproteinase inhibitors 审中-公开确定潜在的变构结合基质金属蛋白酶抑制剂的方法公开(公告)号：US20050004126A1
公开(公告)日：2005-01-06
申请号：US10835619
申请日：2004-04-29
IPC分类号： C07D239/90 , A61K31/00 , A61K31/36 , A61K31/444 , A61K31/517 , A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/04 , A61P29/00 , A61P35/00 , A61P43/00 , C07C69/76 , C07C69/92 , C07C205/57 , C07C229/62 , C07C235/60 , C07D213/30 , C07D213/40 , C07D239/96 , C07D285/14 , C07D285/24 , C07D285/32 , C07D317/54 , C07D317/58 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04 , A61K31/535 , A61K31/47 , A61K31/50
CPC分类号： C07D471/04 , A61K31/00 , C07C235/60 , C07D213/30 , C07D213/40 , C07D239/96 , C07D285/14 , C07D285/24 , C07D285/32 , C07D317/54 , C07D317/58 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D513/04
摘要： Compounds are provided that bind allosterically to the catalytic domain of MMP-13 and comprise a hydrophobic group, first and second hydrogen bond acceptors and at least one, and preferably both, of a third hydrogen bond acceptor and a second hydrophobic group. Cartesian coordinates for centroids of the above features are defined in the specification. When the ligand binds to MMP-13, the first, second and third (when present) hydrogen bond acceptors bond respectively with Thr245, Thr 247 and Met 253, the first hydrophobic group locates within the S1′ channel of MMP-13 and the second hydrophobic group (when present) is relatively open to solvent. The compounds specifically inhibit the matrix metalloproteinase-13 enzyme and thus are useful for treating diseases resulting from tissue breakdown, such as heart disease, multiple sclerosis, arthritis, atherosclerosis, and osteoporosis.
摘要翻译： 提供化合物，其以构象方式与MMP-13的催化结构域结合，并且包含疏水基团，第一和第二氢键受体以及至少一个，优选两个第三氢键受体和第二疏水基团。 上述特征的质心的笛卡尔坐标在本说明书中定义。 当配体结合MMP-13时，第一，第二和第三（当存在）氢键受体分别与Thr245，Thr 247和Met 253键合时，第一个疏水基团位于MMP-13的S1'通道内，第二个 疏水基团（当存在时）对溶剂相对开放。 所述化合物特异性地抑制基质金属蛋白酶-13酶，因此可用于治疗由组织破坏引起的疾病，例如心脏病，多发性硬化，关节炎，动脉粥样硬化和骨质疏松症。
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公开(公告)号：US08598174B2
公开(公告)日：2013-12-03
申请号：US13128726
申请日：2009-11-12
申请人： Antonio J. M. Barbosa, Jr. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey E. Kropf , Scott A. Mitchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
发明人： Antonio J. M. Barbosa, Jr. , Peter A. Blomgren , Kevin S. Currie , Seung Lee , Jeffrey E. Kropf , Scott A. Mitchell , Daniel Ortwine , William M. Rennells , Aaron C. Schmitt , Jianjun Xu , Wendy B. Young , Zhongdong Zhao , Pavel E. Zhichkin
IPC分类号： A61K31/50 , A61K31/501 , C07D237/30
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D513/04 , C07D519/00
摘要： Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
摘要翻译： 本文描述了抑制Btk的式I化合物。 描述了包含至少一种式I化合物的药物组合物以及选自载体，佐剂和赋形剂的至少一种药学上可接受的载体。 描述了治疗患有某些对Btk活性和/或B细胞活性的抑制作出反应的某些疾病的患者的方法。 描述了确定样品中Btk的存在的方法。
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