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1. 发明申请

WO2007081542A9 TETRALONE-BASED MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译：基于四氢呋喃的单胺类复制抑制剂
公开(公告)号：WO2007081542A9
公开(公告)日：2008-10-09
申请号：PCT/US2006049069
申请日：2006-12-21
申请人： SEPRACOR INC , SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , VARNEY MARK , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , MA JIANGUO
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , VARNEY MARK , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , MA JIANGUO
IPC分类号： A61K31/4706
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。

2. 发明申请

WO2007081857A3 CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译：环烷基胺作为单胺再生抑制剂
公开(公告)号：WO2007081857A3
公开(公告)日：2007-11-08
申请号：PCT/US2007000376
申请日：2007-01-05
申请人： SEPRACOR INC , SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , MA JIANGUO , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , CAMPBELL JOHN E
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , MA JIANGUO , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , CAMPBELL JOHN E
IPC分类号： A61K31/381 , A61K31/335
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）疾病如抑郁症，焦虑症，精神分裂症和睡眠障碍中的用途以及它们的合成方法。本发明还涉及含有本发明化合物的药物组合物，以及从突触间隙抑制内源性单胺（例如多巴胺，5-羟色胺和去甲肾上腺素）的再摄取的方法以及调节一种或多种单胺转运体的方法。

3. 发明申请

WO2007081542A3 TETRALONE-BASED MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译：基于四氢呋喃的单胺再用抑制剂
公开(公告)号：WO2007081542A3
公开(公告)日：2008-12-11
申请号：PCT/US2006049069
申请日：2006-12-21
申请人： SEPRACOR INC , SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , VARNEY MARK , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , MA JIANGUO
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , VARNEY MARK , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , MA JIANGUO
IPC分类号： A01N43/42 , A61K31/47
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：本发明涉及新型基于四氢萘酮的胺及其在治疗中枢神经系统（CNS）疾病如抑郁症，注意力缺陷多动障碍（ADHD）和帕金森病中的用途。本发明还涉及含有本发明的化合物和组合物的药物组合物以及抑制一种或多种单胺的再摄取的方法，例如，如多巴胺和去甲肾上腺素，从突触间隙，和调节一种或多种单胺转运蛋白的方法。

4. 发明公开

EP1976513A4 CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 失效转让
标题翻译：环烷基胺类称为单胺再摄取抑制剂
公开(公告)号：EP1976513A4
公开(公告)日：2012-04-18
申请号：EP07716419
申请日：2007-01-05
申请人： SEPRACOR INC
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , MA JIANGUO , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , CAMPBELL JOHN E
IPC分类号： A61K31/381 , A61K31/335
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.

5. 发明公开

EP2154962A4 PHENYL SUBSTITUTED CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译：苯基取代的环烷基称为单胺再摄取抑制剂
公开(公告)号：EP2154962A4
公开(公告)日：2012-08-15
申请号：EP08756635
申请日：2008-06-02
申请人： SEPRACOR INC
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , MA JIANGUO , RIBE SETH , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , SCHREIBER RUDY , SPEAR KERRY L
IPC分类号： C07C215/42 , A61P25/24 , A61P25/28 , C07C217/52
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.

6. 发明公开

EP1978961A4 TETRALONE-BASED MONOAMINE REUPTAKE INHIBITORS 失效转让
标题翻译：单胺再摄取抑制剂对TETRALONBASIS
公开(公告)号：EP1978961A4
公开(公告)日：2010-10-27
申请号：EP06848050
申请日：2006-12-21
申请人： SEPRACOR INC
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , BUSH LARRY R , VARNEY MARK , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , MA JIANGUO
IPC分类号： C07D215/12 , A01N43/42 , A61K31/47 , C07C211/30 , C07C211/40 , C07C215/44 , C07C217/74
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

7. 发明专利

RU2470011C2 ЦИКЛОАЛКИЛАМИНЫ, СОДЕРЖАЩИЕ В КАЧЕСТВЕ ЗАМЕСТИТЕЛЯ ФЕНИЛ, КАК ИНГИБИТОРЫ ОБРАТНОГО ЗАХВАТА МОНОАМИНОВ 未知
公开(公告)号：RU2470011C2
公开(公告)日：2012-12-20
申请号：RU2009149292
申请日：2008-06-02
申请人： SEPRACOR INC
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , MA JIANGUO , RIBE SETH , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , SCHREIBER RUDY , SPEAR KERRY L
IPC分类号： C07C215/42 , A61K31/133 , A61P3/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/30 , C07C217/52
摘要： Изобретениеотноситсяк новымпроизводнымциклоалкиламинов, обладающимингибирующейактивностьюв отношении, поменьшеймере, одноготранспортерамоноаминов, выбранногоизгруппы, состоящейизтранспортерасеротонина, транспортерадофаминаи транспортеранорэпинефрина. Вформуле (IV):,n равно 1; s равно 1; Y и Z каждыйнезависимопредставляетсобойгалоген; Хпредставляетсобой OR; где RозначаетН илинезамещенный C-Салкил; АпредставляетсобойН, незамещенныйС-Салкилилигалоген; Rи RкаждыйнезависимопредставляетсобойН; Rи RкаждыйнезависимопредставляетсобойН илинезамещенный C-Салкил. Изобретениетакжеотноситсяк фармацевтическойкомпозиции, содержащейуказанныесоединения, ик способулеченияилипредотвращенияневрологическогорасстройстваилирасстройствапищевогоповедения, опосредованныхактивностьютранспортерамоноамина, выбранногоизгруппы, состоящейизтранспортерасеротонина, транспортерадофаминаи транспортеранорэпинефрина, такогокакдепрессия, нейродегенеративноезаболевание, злоупотреблениепсихоактивнымивеществами, фибромиалгия, боль, расстройствосна, синдромнарушениявнимания, синдромнарушениявниманияс гиперактивностью, синдромусталыхног, шизофрения, тревожность, обсессивно-компульсивноерасстройство, паническоерасстройство, посттравматическийстресс, предменструальнаядисфория. 7 н. и 28 з.п. ф-лы, 6 ил., 8 пр.

8. 发明专利

RU2430913C2 ЦИКЛОАЛКИЛАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ПОВТОРНОГО ПОГЛОЩЕНИЯ МОНОАМИНА 未知
公开(公告)号：RU2430913C2
公开(公告)日：2011-10-10
申请号：RU2008132320
申请日：2007-01-05
申请人： SEPRACOR INC
发明人： CAMPBELL UNA , MA JIANGUO , BUSH LARRY R , ENGEL SHARON RAE , HARDY LARRY WENDELL , WANG FENGJIANG , VARNEY MARK A , HEWITT MICHAEL CHARLES , KOCH PATRICK , SHAO LIMING , MALCOLM SCOTT CHRISTOPHER , CAMPBELL JOHN E
IPC分类号： A61K31/335 , A61K31/381 , A61P15/12 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , C07C215/42 , C07C215/64 , C07D265/14 , C07D317/48 , C07D317/72 , C07D491/056
摘要： Изобретениеотноситсяк новымциклогексиламиновымпроизводным, имеющимструктуру, соответствующуюформуле (I),обладающимсвойствамиингибитораактивностипоменьшеймереодноготранспортерамоноамина, такогокактранспортерсеротонина, транспортердопаминаилитранспортернорэпинефрина, иликомбинациидвухилиболеетранспортеров. Соединениямогутбытьиспользованыдлялеченияи/илипрофилактикирасстройствцентральнойнервнойсистемы (ЦНС), такихкакболь, депрессия, беспокойство, шизофренияи расстройстваснаи др. Вформуле (I) ! ! n равно 0 или 1; s равно 1, 2 или 3; m равноцеломучислуот 0 до 12; Аr представляетсобой ! ! где Y и Z представляютсобой (i) обагалоген; или (ii) одиниз Y и Z представляетсобойСF3 илиОСF3, адругойпредставляетсобойводород; Y1, Z1, Y2 и Z2 каждыйнезависимопредставляетсобойН илигалоген;каждыйХ независимопредставляетсобойН, галоген, СF3, OR5, (С1-С4)алкил, необязательнозамещенныйгалогеномилиОН, или NR6R7; ! каждый R1 и R2 независимопредставляетсобойН или (С1-С6)алкил; икаждый R3 и R4 независимопредставляетсобойН или (С1-С9)алкил, необязательнозамещенныйОН; где ! каждый R5 независимопредставляетсобойН, (С1-С4)алкилилифенил; икаждый R6 и R7 независимопредставляетсобойН или (С1-С4)алкил; гдепоменьшеймередваиз R1, R2, R3, R4 иХ вместес атомами, ккоторымониприсоединены, необязательносвязаныс образованием 5-6-членногокольца, где 5-6-членноекольцовыбираютиз: а) R3 и R4 вместес атомомазота, ккоторомуониприсоединены, необязательнообразуютпирролидиновое, пиперидиновое, пиперазиновоеилиморфолиновоекольцо, котороенеобязательнозамещено (С1-С4)алкилом; b) когда R3 представляетсобойН илинизший

9. 发明专利

CA2636324A1 CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 未知
公开(公告)号：CA2636324A1
公开(公告)日：2007-07-19
申请号：CA2636324
申请日：2007-01-05
申请人： SEPRACOR INC
发明人： CAMPBELL UNA , MA JIANGUO , BUSH LARRY R , ENGEL SHARON RAE , HARDY LARRY WENDELL , WANG FENGJIANG , VARNEY MARK A , HEWITT MICHAEL CHARLES , KOCH PATRICK , SHAO LIMING , MALCOLM SCOTT CHRISTOPHER , CAMPBELL JOHN E
IPC分类号： A61K31/381 , A61K31/335
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.

10. 发明专利

CA2688493A1 PHENYL SUBSTITUTED CYCLOALKYLAMINES AS MONOAMINE REUPTAKE INHIBITORS 未知
公开(公告)号：CA2688493A1
公开(公告)日：2008-12-11
申请号：CA2688493
申请日：2008-06-02
申请人： SEPRACOR INC
发明人： SHAO LIMING , WANG FENGJIANG , MALCOLM SCOTT CHRISTOPHER , HEWITT MICHAEL CHARLES , MA JIANGUO , RIBE SETH , VARNEY MARK A , CAMPBELL UNA , ENGEL SHARON RAE , HARDY LARRY WENDELL , KOCH PATRICK , SCHREIBER RUDY , SPEAR KERRY L
IPC分类号： C07C215/42 , A61K31/135 , A61P3/04 , A61P25/00
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.

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