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![Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof](/abs-image/US/2013/11/05/US08575186B2/abs.jpg.150x150.jpg)
1.发明授权Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof 失效作为血清素亚型6（5-HT6）调节剂的异亚氨基环烷基[b]吲哚衍生物及其用途公开(公告)号：US08575186B2
公开(公告)日：2013-11-05
申请号：US12898271
申请日：2010-10-05
申请人： Peter R. Guzzo , Alan J. Henderson , Kassoum Nacro , Matthew L. Isherwood , Animesh Ghosh , Kai Xiang
发明人： Peter R. Guzzo , Alan J. Henderson , Kassoum Nacro , Matthew L. Isherwood , Animesh Ghosh , Kai Xiang
IPC分类号： A61K31/506 , A61K31/439 , C07D471/18 , A61P3/04 , A61P3/10 , A61P25/00 , A61P3/00 , A61P25/18 , A61P25/28
CPC分类号： C07D471/18 , C07B57/00 , C07D519/00
摘要： The present invention relates to epiminocycloalkyl[b]indole derivatives as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, and methods of preparation and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, and schizophrenia. The subject compounds have the structure of formula (I) with the substituents being described herein.
摘要翻译： 本发明涉及作为5-羟色胺亚型6（5-HT6）调节剂的异亚氨基环烷基[b]吲哚衍生物，包括这些化合物的药物组合物及其制备和使用方法。 这些化合物可用于治疗中枢神经系统疾病，包括肥胖，代谢综合征，认知和精神分裂症。 本发明化合物具有式（I）的结构，其中取代基在本文中描述。
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2.发明授权Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US07956050B2
公开(公告)日：2011-06-07
申请号：US11487884
申请日：2006-07-17
申请人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
IPC分类号： A61P25/00 , A61K31/55 , C07D223/16
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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3.发明授权Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US08791101B2
公开(公告)日：2014-07-29
申请号：US12917066
申请日：2010-11-01
申请人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
IPC分类号： A61K31/55 , C07D401/04
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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4.发明申请ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权ARYL-和HETEROARYL取代的四氢苯并噻吩并用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶公开(公告)号：US20110046114A1
公开(公告)日：2011-02-24
申请号：US12917066
申请日：2010-11-01
申请人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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5.发明申请ARYL, HETEROARYL, AND HETEROCYCLE SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF 有权ARYL，HETEROARYL和HETEROCYCLE取代的四氢喹啉和其用途公开(公告)号：US20100292242A1
公开(公告)日：2010-11-18
申请号：US12777728
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A61K31/472 , C07D401/10 , A61K31/501 , A61K31/497 , C07D217/14 , A61K31/4725 , C07D471/04 , A61P25/00 , A61P25/24 , A61P15/00
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译： 本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。 这些化合物用于治疗各种神经和生理疾病。 制备这些化合物的方法也在本发明中描述。
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6.发明授权Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof 有权芳基，杂芳基和杂环取代的四氢异喹啉及其用途公开(公告)号：US09034899B2
公开(公告)日：2015-05-19
申请号：US12777728
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A01N43/42 , A61K31/47 , C07D217/02 , C07D217/12 , C07D401/04 , C07D413/04 , C07D471/04
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译： 本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。 这些化合物用于治疗各种神经和生理疾病。 制备这些化合物的方法也在本发明中描述。
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![7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF](/abs-image/US/2010/11/18/US20100292243A1/abs.jpg.150x150.jpg)
7.发明申请7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDROISOQUINOLINE AND USE THEREOF 有权7 - （[1,2,4]三唑并[1,5-a]吡啶-6-基）-4-（3,4-二氯苯基）-1,2,3,4-四氢喹啉并及其用途公开(公告)号：US20100292243A1
公开(公告)日：2010-11-18
申请号：US12777776
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A61K31/495 , C07D471/04 , A61K31/437 , A61P25/00 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/30 , A61P19/02 , A61P1/00 , A61P15/10 , A61K31/438 , A61P25/34 , A61P25/32
CPC分类号： C07D471/04
摘要： Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.
摘要翻译： 在本发明中描述了新的[1,2,4]三唑并[1,5-a]吡啶基-6-基取代的四氢异喹啉。 这些化合物和结晶形式SA1和N-2用于治疗各种神经和生理疾病。 制备这些化合物和结晶形式SA-1和N-2的方法也在本发明中描述。
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8.发明申请Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US20080207595A9
公开(公告)日：2008-08-28
申请号：US11487884
申请日：2006-07-17
申请人： Bruce Molino , Shuang Liu , Aruna Sambandam , Peter Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David Manning , Matthew Isherwood , Kristen Fleming , Wenge Cui , Richard Olson
发明人： Bruce Molino , Shuang Liu , Aruna Sambandam , Peter Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David Manning , Matthew Isherwood , Kristen Fleming , Wenge Cui , Richard Olson
IPC分类号： A61K31/55 , C07D487/02 , C07D403/02
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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![7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoqu inoli and use thereof](/abs-image/US/2014/08/12/US08802696B2/abs.jpg.150x150.jpg)
9.发明授权7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoqu inoli and use thereof 有权7 - （[1,2,4]三唑并[1,5-a]吡啶-6-基）-4-（3,4-二氯苯基）-1,2,3,4-四氢异喹啉及其用途公开(公告)号：US08802696B2
公开(公告)日：2014-08-12
申请号：US12777776
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： C07D471/04 , A61K31/495
CPC分类号： C07D471/04
摘要： Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.
摘要翻译： 在本发明中描述了新的[1,2,4]三唑并[1,5-a]吡啶基-6-基取代的四氢异喹啉。 这些化合物和结晶形式SA1和N-2用于治疗各种神经和生理疾病。 制备这些化合物和结晶形式SA-1和N-2的方法也在本发明中描述。
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10.发明申请Aryl-and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取公开(公告)号：US20070021408A1
公开(公告)日：2007-01-25
申请号：US11487884
申请日：2006-07-17
申请人： Bruce Molino , Shuang Liu , Aruna Sambandam , Peter Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David Manning , Matthew Isherwood , Kristen Fleming , Wenge Cui , Richard Olson
发明人： Bruce Molino , Shuang Liu , Aruna Sambandam , Peter Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David Manning , Matthew Isherwood , Kristen Fleming , Wenge Cui , Richard Olson
IPC分类号： A61K31/55 , C07D487/02 , C07D403/02
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译： 本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。
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