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公开(公告)号：US20100190861A1
公开(公告)日：2010-07-29
申请号：US12688474
申请日：2010-01-15
申请人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campbell
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campbell
IPC分类号： A61K31/135 , C07C211/15 , C07C215/48 , A61P25/00 , A61P25/24
CPC分类号： C07D333/20 , C07C211/17 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/06 , C07D207/08 , C07D211/14 , C07D211/16 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056
摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
摘要翻译： 本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。
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公开(公告)号：US20070203111A1
公开(公告)日：2007-08-30
申请号：US11649927
申请日：2007-01-05
申请人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Jianguo Ma , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , John Campbell
发明人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Jianguo Ma , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , John Campbell
IPC分类号： A61K31/55 , A61K31/445 , A61K31/40 , A61K31/397 , A61K31/396 , C07D211/06 , C07D203/04 , C07D207/04
CPC分类号： C07D333/20 , C07C211/17 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/06 , C07D207/08 , C07D211/14 , C07D211/16 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056
摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
摘要翻译： 本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。
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公开(公告)号：US08877975B2
公开(公告)日：2014-11-04
申请号：US12688474
申请日：2010-01-15
申请人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campbell
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Larry R. Bush , Jianguo Ma , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , John E. Campbell
IPC分类号： C07C211/17 , A61K31/137 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07D207/06 , C07D207/08 , C07D211/14 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D333/20 , C07D491/056
CPC分类号： C07D333/20 , C07C211/17 , C07C211/29 , C07C211/40 , C07C215/42 , C07C215/44 , C07C217/52 , C07C217/74 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/06 , C07D207/08 , C07D211/14 , C07D211/16 , C07D265/14 , C07D277/28 , C07D295/06 , C07D307/52 , C07D317/58 , C07D317/72 , C07D319/06 , C07D491/056
摘要： The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
摘要翻译： 本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。
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公开(公告)号：US20090005456A1
公开(公告)日：2009-01-01
申请号：US12131845
申请日：2008-06-02
申请人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Jianguo Ma , Seth Ribe , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , Rudy Schreiber , Kerry L. Spear
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Jianguo Ma , Seth Ribe , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , Rudy Schreiber , Kerry L. Spear
IPC分类号： A61K31/135 , C07C211/29 , A61P25/24 , A61P3/04 , A61P25/34
CPC分类号： C07C215/42 , A61K31/135 , A61P25/24 , A61P25/28 , C07B2200/07 , C07C217/52 , C07C217/76 , C07C2601/14
摘要： Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
摘要翻译： 公开了苯基取代的环己胺衍生物及其合成和表征的方法。 本文阐述了这些化合物治疗/预防神经系统疾病及其合成方法的用途。 本发明的示例性化合物抑制内源性单胺如多巴胺，5-羟色胺和去甲肾上腺素的再摄取（例如，从突触腭裂）并调节一种或多种单胺转运蛋白。 还提供了掺入本发明化合物的药物制剂。
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公开(公告)号：US6166018A
公开(公告)日：2000-12-26
申请号：US332824
申请日：1999-06-14
IPC分类号： A61K31/4196 , A61P31/10 , C07D249/12 , C07D405/06 , C07D405/14 , C07D521/00 , A61K31/495 , C07D413/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/12
摘要： A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.
摘要翻译： 公开了制备羟基特他康唑的旋光纯异构体的方法，特别是仲丁基（R，S） - 异构体及其磷酸盐和硫酸盐衍生物的两种顺式二氧戊环非对映异构体。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。
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公开(公告)号：US20050222211A1
公开(公告)日：2005-10-06
申请号：US11140675
申请日：2005-05-27
申请人： Patrick Koch , Paul Rubin , William Yelle
发明人： Patrick Koch , Paul Rubin , William Yelle
CPC分类号： A61K31/4439 , A61K31/00
摘要： Methods and compositions are disclosed utilizing optically pure S(−)rabeprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of rabeprazole. The optically pure S(−) isomer is also useful for the treatment of gastroesophageal reflux. S(−)rabeprazole is an inhibitor of H+ release and is therefore useful in the treatment of other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.
摘要翻译： 公开了使用光学纯的S（ - ）雷贝拉唑治疗人体溃疡的方法和组合物，同时显着减少与雷贝拉唑的外消旋混合物相关的副作用的伴随的责任。 光学纯的S（ - ）异构体也可用于治疗胃食管反流。 S（ - ）雷贝拉唑是一种H +抑制剂，因此可用于治疗与胃分泌异常有关的其他病症，如Zollinger-Ellison综合征。
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公开(公告)号：US06455530B1
公开(公告)日：2002-09-24
申请号：US09663992
申请日：2000-09-18
IPC分类号： A61K31496
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/12
摘要： A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.
摘要翻译： 公开了制备羟基特他康唑的光学纯异构体的方法，特别是仲丁基（S，S） - 异构体的两种顺式二氧戊环非对映体及其磷酸盐和硫酸盐衍生物。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。
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公开(公告)号：US5952502A
公开(公告)日：1999-09-14
申请号：US968780
申请日：1997-11-12
IPC分类号： A61K31/4196 , A61P31/10 , C07D249/12 , C07D405/06 , C07D405/14 , C07D521/00 , C07D413/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/12
摘要： A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and to their use for the treatment of fungal infection are also disclosed.
摘要翻译： 公开了制备羟基特他康唑的旋光纯异构体的方法，特别是仲丁基（R，S） - 异构体及其磷酸盐和硫酸盐衍生物的两种顺式二氧戊环非对映异构体。 还公开了含有这些化合物的药物组合物及其用于治疗真菌感染的用途。
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公开(公告)号：US08669291B2
公开(公告)日：2014-03-11
申请号：US12131845
申请日：2008-06-02
申请人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Jianguo Ma , Seth Ribe , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , Rudy Schreiber , Kerry L. Spear
发明人： Liming Shao , Fengjiang Wang , Scott Christopher Malcolm , Michael Charles Hewitt , Jianguo Ma , Seth Ribe , Mark A. Varney , Una Campbell , Sharon Rae Engel , Larry Wendell Hardy , Patrick Koch , Rudy Schreiber , Kerry L. Spear
IPC分类号： A61K31/133 , A61K31/135 , C07C211/17
CPC分类号： C07C215/42 , A61K31/135 , A61P25/24 , A61P25/28 , C07B2200/07 , C07C217/52 , C07C217/76 , C07C2601/14
摘要： Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
摘要翻译： 公开了苯基取代的环己胺衍生物及其合成和表征的方法。 本文阐述了这些化合物治疗/预防神经系统疾病及其合成方法的用途。 本发明的示例性化合物抑制内源性单胺如多巴胺，5-羟色胺和去甲肾上腺素的再摄取（例如，从突触腭裂）并调节一种或多种单胺转运蛋白。 还提供了掺入本发明化合物的药物制剂。
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公开(公告)号：US20070197588A1
公开(公告)日：2007-08-23
申请号：US11643190
申请日：2006-12-21
申请人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , Jianguo Ma
发明人： Liming Shao , Fengjiang Wang , Scott Malcolm , Michael Hewitt , Larry Bush , Mark Varney , Una Campbell , Sharon Engel , Larry Hardy , Patrick Koch , Jianguo Ma
IPC分类号： A61K31/4706 , A61K31/137 , A61K31/135
CPC分类号： C07C211/40 , C07C17/16 , C07C17/35 , C07C45/38 , C07C45/52 , C07C45/63 , C07C45/67 , C07C45/68 , C07C45/74 , C07C211/29 , C07C211/30 , C07C211/42 , C07C215/44 , C07C217/74 , C07C2601/14 , C07C2602/10 , C07D215/12 , C07C25/22 , C07C22/04 , C07C47/453 , C07C49/67 , C07C49/697 , C07C49/255 , C07C49/755 , C07C49/683
摘要： The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
摘要翻译： 本发明涉及新的四氢萘酮类胺及其用于治疗中枢神经系统（CNS）障碍，例如抑郁症，注意缺陷多动障碍（ADHD）和帕金森病。 本发明还涉及含有本发明化合物和组合物的药物组合物以及抑制一种或多种单胺（例如多巴胺和去甲肾上腺素）从突触裂缝再摄取的方法，以及调节一种或多种单胺转运蛋白的方法 。
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