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1.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：US08268859B2
公开(公告)日：2012-09-18
申请号：US12477586
申请日：2009-06-03
申请人： Christian Harcken , Rajashekhar Betageri , Todd Bosanac , Michael Jason Burke , Soojin Kim , Daniel Kuzmich , Thomas Wai-ho Lee , Zhibin Li , Pingrong Liu , John Lord , Hossein Razavi , Jonathan Timothy Reeves , David Thomson
发明人： Christian Harcken , Rajashekhar Betageri , Todd Bosanac , Michael Jason Burke , Soojin Kim , Daniel Kuzmich , Thomas Wai-ho Lee , Zhibin Li , Pingrong Liu , John Lord , Hossein Razavi , Jonathan Timothy Reeves , David Thomson
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, 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，X和Y如本文所定义的式（I）化合物或其互变异构体，旋光异构体，前药，共结晶或其盐; 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：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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公开(公告)号：US20100093724A1
公开(公告)日：2010-04-15
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： A61K31/5377 , A61K31/497 , A61K31/4353 , C07D413/12 , C07D471/02
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.
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：US20120035370A1
公开(公告)日：2012-02-09
申请号：US13273509
申请日：2011-10-14
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： C07D471/04 , C07D213/71
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 intermediates thereof, and 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。 还公开了其中间体及其制备方法及其使用方法。
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5.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：US20090325988A1
公开(公告)日：2009-12-31
申请号：US12477586
申请日：2009-06-03
申请人： Christian Harcken , Rajashekhar Betageri , Todd Bosanac , Michael Jason Burke , Soojin Kim , Daniel Kuzmich , Thomas Wai-Ho Lee , Zhibin Li , Pingrong Liu , John Lord , Hossein Razavi , Jonathan Timothy Reeves , Daivd Thomson
发明人： Christian Harcken , Rajashekhar Betageri , Todd Bosanac , Michael Jason Burke , Soojin Kim , Daniel Kuzmich , Thomas Wai-Ho Lee , Zhibin Li , Pingrong Liu , John Lord , Hossein Razavi , Jonathan Timothy Reeves , Daivd Thomson
IPC分类号： A61K31/437 , C07D471/04 , C07D211/72 , C07D239/46 , A61K31/44 , A61K31/505 , A61P9/00 , A61P37/08 , A61P17/00 , A61P1/00 , A61P25/00 , A61P35/00 , A61P7/00
CPC分类号： C07D471/04
摘要： Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, 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，X和Y如本文所定义的式（I）化合物或其互变异构体，旋光异构体，前药，共结晶或其盐; 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：US09079832B2
公开(公告)日：2015-07-14
申请号：US14072352
申请日：2013-11-05
IPC分类号： C07C313/06 , C07D319/18 , C07D295/185 , C07C327/46
CPC分类号： C07C313/06 , C07C327/46 , C07C2601/02 , C07C2601/04 , C07C2603/74 , C07C2603/94 , C07D295/185 , C07D319/18
摘要： Disclosed is a process for making diastereomeric N-sulfinyl α-amino amides by reaction of chiral sulfinimines with formamides and lithium diisopropylamide. The process of the invention provides the N-sulfinyl α-amino amides in high yields and with high diastereoselectivity.
摘要翻译： 公开了通过手性亚磺酰亚胺与甲酰胺和二异丙基氨基锂的反应来制备非对映异构N-亚磺酰基α-氨基酰胺的方法。 本发明的方法以高产率和高非对映选择性提供了N-亚磺酰基α-氨基酰胺。
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公开(公告)号：US20140135493A1
公开(公告)日：2014-05-15
申请号：US13921145
申请日：2011-12-15
申请人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
发明人： Daniel Robert Fandrick , Zhi-Hui Lu , Diana Crimhilda Reeves , Jonathan Timothy Reeves , Chris Hugh Senanayake , Jinhua J. Song , Yongda Zhang
IPC分类号： C07D413/10 , C07D213/64 , C07C271/48 , C07D265/10
CPC分类号： C07D413/10 , C07C271/48 , C07D213/64 , C07D265/10
摘要： Disclosed is a process for making diastereomeric compound of the formula (I): wherein m, n and R1 to R4 are as defined herein. The process of the invention provides the compound of formula (I) in high yield and substantially free of the corresponding diastereomers. The compounds of formula (I) prepared by the process of the invention are useful for making pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.
摘要翻译： 公开了制备式（I）的非对映体化合物的方法：其中m，n和R 1至R 4如本文所定义。 本发明的方法以高产率提供式（I）化合物，基本上不含相应的非对映异构体。 通过本发明的方法制备的式（I）化合物可用于制备药学活性化合物，例如11-羟基类固醇类氢化酶1型（11-＆amp; -HSD1）抑制剂。
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8.发明申请公开(公告)号：US20110275808A1
公开(公告)日：2011-11-10
申请号：US12990056
申请日：2009-04-28
IPC分类号： C07D487/04
CPC分类号： C07B57/00 , C07D487/04
摘要： A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein.
摘要翻译： 其中R 1，R 2，R 3，R 4和R 5如本文所述的式（I）化合物的立体选择性合成方法。
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公开(公告)号：US20140171641A1
公开(公告)日：2014-06-19
申请号：US14072352
申请日：2013-11-05
IPC分类号： C07C313/06 , C07C327/46 , C07D319/18
CPC分类号： C07C313/06 , C07C327/46 , C07C2601/02 , C07C2601/04 , C07C2603/74 , C07C2603/94 , C07D295/185 , C07D319/18
摘要： Disclosed is a process for making diastereomeric N-sulfinyl α-amino amides by reaction of chiral sulfinimines with formamides and lithium diisopropylamide. The process of the invention provides the N-sulfinyl α-amino amides in high yields and with high diastereoselectivity.
摘要翻译： 公开了通过手性亚磺酰亚胺与甲酰胺和二异丙基氨基锂的反应来制备非对映异构N-亚磺酰基α-氨基酰胺的方法。 本发明的方法以高产率和高非对映选择性提供了N-亚磺酰基α-氨基酰胺。
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公开(公告)号：US20120136158A1
公开(公告)日：2012-05-31
申请号：US13368397
申请日：2012-02-08
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： C07D213/73
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 intermediates thereof, and 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。 还公开了其中间体及其制备方法及其使用方法。
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