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1.发明申请Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof 有权糖皮质激素模拟物，其制备方法，药物组合物及其用途公开(公告)号：US20060154925A1
公开(公告)日：2006-07-13
申请号：US11305362
申请日：2005-12-16
申请人： Daniel Kuzmich , Darren DiSalvo , John Regan , David Thomson
发明人： Daniel Kuzmich , Darren DiSalvo , John Regan , David Thomson
IPC分类号： A61K31/5377 , A61K31/498 , A61K31/4709
CPC分类号： C07D471/04 , C07D209/08 , C07D209/16 , C07D209/86 , C07D215/06 , C07D215/233 , C07D231/56 , C07D235/14 , C07D307/79 , C07D333/58 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译： 式（I）的化合物，其中R 1，R 2，R 3，R 4，R 4， R 5，R 6和R 7如本文所定义，或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。
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2.发明申请公开(公告)号：US20060189646A1
公开(公告)日：2006-08-24
申请号：US11305361
申请日：2005-12-16
申请人： Daniel Kuzmich , Darren DiSalvo , John Regan , David Thomson , Rajashekhar Betageri , Jennifer Kowalski
发明人： Daniel Kuzmich , Darren DiSalvo , John Regan , David Thomson , Rajashekhar Betageri , Jennifer Kowalski
IPC分类号： C07D471/02 , A61K31/4745 , A61K31/404 , C07D209/14
CPC分类号： C07D471/04 , C07D209/08 , C07D209/16 , C07D209/86 , C07D215/06 , C07D215/233 , C07D231/56 , C07D235/14 , C07D307/79 , C07D333/58 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
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3.发明申请Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof 有权糖皮质激素模拟物，其制备方法，药物组合物及其用途公开(公告)号：US20100197678A1
公开(公告)日：2010-08-05
申请号：US12517874
申请日：2007-11-29
IPC分类号： A61K31/5383 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , C07D498/04 , A61P29/00
CPC分类号： C07D417/06 , C07D231/56 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D407/14 , C07D409/06 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
摘要： Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译： 其中R1，R2，R3，A，B，C，D，E，G，X，Y和Z如本文所定义的式（IA）化合物或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。
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4.发明授权Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof 有权糖皮质激素模拟物，其制备方法，药物组合物及其用途公开(公告)号：US07741361B2
公开(公告)日：2010-06-22
申请号：US11305362
申请日：2005-12-16
IPC分类号： A61K31/404 , A61K31/18 , C07D209/04 , C07C307/02
CPC分类号： C07D471/04 , C07D209/08 , C07D209/16 , C07D209/86 , C07D215/06 , C07D215/233 , C07D231/56 , C07D235/14 , C07D307/79 , C07D333/58 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译： 其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义的式（I）化合物或其互变异构体，前药，溶剂化物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。
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公开(公告)号：US08008327B2
公开(公告)日：2011-08-30
申请号：US12937378
申请日：2009-04-23
申请人： Darren DiSalvo , Daniel Kuzmich , Can Mao , Hossein Razavi , Christopher Ronald Sarko , Alan David Swinamer , David Smith Thomson , Qiang Zhang
发明人： Darren DiSalvo , Daniel Kuzmich , Can Mao , Hossein Razavi , Christopher Ronald Sarko , Alan David Swinamer , David Smith Thomson , Qiang Zhang
IPC分类号： A61K31/416 , A61K31/4439 , C07D231/56 , C07D401/02
CPC分类号： C07D231/56 , C07D401/12
摘要： Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译： 公开的吲唑化合物可用作CCR1活性的拮抗剂，因此可用于治疗通过CCR1的活性介导或维持的多种疾病和病症，包括自身免疫性疾病，例如类风湿性关节炎和多发性硬化症。 还公开了包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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6.发明授权Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 有权糖皮质激素模拟物，其制备方法，药物组合物及其用途公开(公告)号：US08658637B2
公开(公告)日：2014-02-25
申请号：US12517874
申请日：2007-11-29
IPC分类号： A61K31/5383 , A61K31/437 , A61K31/519 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D417/06 , C07D231/56 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D407/14 , C07D409/06 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
摘要： Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译： 其中R1，R2，R3，A，B，C，D，E，G，X，Y和Z如本文所定义的式（IA）化合物或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。
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公开(公告)号：US08546442B2
公开(公告)日：2013-10-01
申请号：US13328199
申请日：2011-12-16
申请人： Rajashekhar Betageri , Brian Nicholas Cook , Darren DiSalvo , Christian Harcken , Daniel Kuzmich , Pingrong Liu , John Lord , Can Mao , Hossein Razavi
发明人： Rajashekhar Betageri , Brian Nicholas Cook , Darren DiSalvo , Christian Harcken , Daniel Kuzmich , Pingrong Liu , John Lord , Can Mao , Hossein Razavi
IPC分类号： A01N43/56 , A01N43/42 , A61K31/415 , A61K31/44 , C07D231/54 , C07D487/02
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
摘要翻译： 公开了式（I）化合物，其可用于治疗通过包括自身免疫疾病如类风湿性关节炎和多发性硬化的CCR1的活性介导或持续的多种疾病和病症。 还公开了制备方法和使用方法。
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公开(公告)号：US07879873B2
公开(公告)日：2011-02-01
申请号：US12564129
申请日：2009-09-22
申请人： Brian Nicholas Cook , Darren DiSalvo , Daniel Robert Fandrick , Christian Harcken , Daniel Kuzmich , Thomas Wai-Ho Lee , Pingrong Liu , John Lord , Can Mao , Jochen Neu , Brian Christopher Raudenbush , Hossein Razavi , Jonathan Timothy Reeves , Jinhua J. Song , Alan David Swinamer , Zhulin Tan
发明人： Brian Nicholas Cook , Darren DiSalvo , Daniel Robert Fandrick , Christian Harcken , Daniel Kuzmich , Thomas Wai-Ho Lee , Pingrong Liu , John Lord , Can Mao , Jochen Neu , Brian Christopher Raudenbush , Hossein Razavi , Jonathan Timothy Reeves , Jinhua J. Song , Alan David Swinamer , Zhulin Tan
IPC分类号： A61K31/437 , C07D515/04
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
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9.发明授权Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof 有权糖皮质激素模拟物，其制备方法，药物组合物及其用途公开(公告)号：US07635711B2
公开(公告)日：2009-12-22
申请号：US11305361
申请日：2005-12-16
申请人： Daniel Kuzmich , Darren DiSalvo , John Robinson Regan , David S. Thomson , Rajashekhar Betageri , Jennifer A. Kowalski
发明人： Daniel Kuzmich , Darren DiSalvo , John Robinson Regan , David S. Thomson , Rajashekhar Betageri , Jennifer A. Kowalski
IPC分类号： A61K31/404 , A61K31/18 , C07D209/04 , C07C307/02
CPC分类号： C07D471/04 , C07D209/08 , C07D209/16 , C07D209/86 , C07D215/06 , C07D215/233 , C07D231/56 , C07D235/14 , C07D307/79 , C07D333/58 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译： 其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义的式（I）化合物或其互变异构体，前药，溶剂化物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。
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公开(公告)号：US07550473B2
公开(公告)日：2009-06-23
申请号：US10933635
申请日：2004-09-03
申请人： Mario G. Cardozo , Derek Cogan , Charles Lawrence Cywin , George Dahmann , Darren DiSalvo , John David Ginn , Anthony S. Prokopowicz, III , Denice M. Spero , Erick Richard Roush Young
发明人： Mario G. Cardozo , Derek Cogan , Charles Lawrence Cywin , George Dahmann , Darren DiSalvo , John David Ginn , Anthony S. Prokopowicz, III , Denice M. Spero , Erick Richard Roush Young
IPC分类号： C07D239/42 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , H01L51/0089
摘要： Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译： 公开了式（I）的新化合物：其中R 1，R 2和R 3如本文所定义，其可用作PKC-θ的抑制剂，因此可用于治疗通过该活性介导或维持的多种疾病和病症 的PKC-θ，包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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