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1.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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公开(公告)号：US08710046B2
公开(公告)日：2014-04-29
申请号：US13384050
申请日：2010-06-30
申请人： Peter R. Guzzo , David D. Manning , William Earley
发明人： Peter R. Guzzo , David D. Manning , William Earley
IPC分类号： C07D487/04 , C07D403/04 , A61K31/5517 , A61P25/00
CPC分类号： C07D513/06 , A61K31/439 , A61K31/55 , A61K31/5517 , A61K45/06 , C07D453/02 , C07D487/04 , C07D513/04
摘要： Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
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3.发明授权Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof 失效哌嗪酮取代的四氢 - 咔啉MCH-1拮抗剂，其制备方法和用途公开(公告)号：US08697700B2
公开(公告)日：2014-04-15
申请号：US13330989
申请日：2011-12-20
申请人： Matthew D. Surman , Peter R. Guzzo
发明人： Matthew D. Surman , Peter R. Guzzo
IPC分类号： A61K31/496 , A61K31/501 , A61K31/506 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to piperazinone-substituted tetrahydrocarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
摘要翻译： 本发明涉及式（I）的哌嗪酮取代的四氢咔啉衍生物：具有本文所述的取代基，其是黑色素浓缩激素（MCH-1）受体拮抗剂。 本发明还涉及包含这些化合物的药物组合物及其制备和使用方法。
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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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![AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF](/abs-image/US/2011/01/06/US20110003793A1/abs.jpg.150x150.jpg)
5.发明申请AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF 失效AZINONE-取代的AZEPINO [b]吲哚和吡啶并吡咯并-Met-1拮抗剂，其制备方法及其用途公开(公告)号：US20110003793A1
公开(公告)日：2011-01-06
申请号：US12828807
申请日：2010-07-01
IPC分类号： A61K31/55 , C07D487/04 , C07D471/14 , A61P3/04 , A61P1/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/18 , A61P25/00
CPC分类号： C07D471/04 , C07D471/14 , C07D487/04
摘要： Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
摘要翻译： 公开了新的MCH-1受体拮抗剂。 这些化合物用于治疗各种疾病，包括肥胖症，焦虑症，抑郁症，非酒精性脂肪性肝病和精神疾病。 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- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢异喹啉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：US07541357B2
公开(公告)日：2009-06-02
申请号：US11183066
申请日：2005-07-15
申请人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D403/04 , C07D217/02 , A61K31/47
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a 吡啶并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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7.发明授权Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof 有权氮杂酮取代的氮杂双环链烷基 - 吲哚和氮杂二环烷基 - 吡咯并 - 吡啶MCH-1拮抗剂，其制备方法和用途公开(公告)号：US09073925B2
公开(公告)日：2015-07-07
申请号：US12828955
申请日：2010-07-01
申请人： Peter R. Guzzo , Matthew David Surman , Lei Zhu
发明人： Peter R. Guzzo , Matthew David Surman , Lei Zhu
IPC分类号： A61K31/55 , C07D487/18 , C07D487/12 , C07D487/22 , C07D471/18 , C07D471/22
CPC分类号： C07D471/18 , C07D471/22
摘要： Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
摘要翻译： 公开了新的MCH-1受体拮抗剂。 这些化合物用于治疗各种疾病，包括肥胖症，焦虑症，抑郁症，非酒精性脂肪性肝病和精神疾病。 制备这些化合物的方法也在本发明中描述。
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8.发明授权Glycine transporter-1 inhibitors, methods of making them, and uses thereof 有权甘氨酸转运蛋白-1抑制剂，其制备方法及其应用公开(公告)号：US09045445B2
公开(公告)日：2015-06-02
申请号：US13151992
申请日：2011-06-02
IPC分类号： A61K31/496 , C07D403/12 , C07D295/26 , C07D205/04 , C07D207/48 , C07D211/58 , C07D213/71 , C07D233/84 , C07D241/04 , C07D249/04 , C07D309/14 , C07D313/04 , C07D405/12 , C07D487/08
CPC分类号： C07D295/26 , C07D205/04 , C07D207/48 , C07D211/58 , C07D213/71 , C07D233/84 , C07D241/04 , C07D249/04 , C07D309/14 , C07D313/04 , C07D405/12 , C07D487/08
摘要： The compounds of the present invention are represented by the following formula (I): wherein the substituents R1, R2, R3, R4, (R5)m, R6, A, X, and Y are as defined herein. The compounds are useful in methods of treating a disorder which is created by or is dependent upon inhibiting GlyT-1.
摘要翻译： 本发明的化合物由下式（I）表示：其中取代基R 1，R 2，R 3，R 4，（R 5）m，R 6，A，X和Y如本文所定义。 该化合物可用于治疗由抑制GlyT-1产生或依赖于其的依赖性疾病的方法。
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公开(公告)号：US20120270857A1
公开(公告)日：2012-10-25
申请号：US13384050
申请日：2010-06-30
申请人： Peter R. Guzzo , David D. Manning , William Earley
发明人： Peter R. Guzzo , David D. Manning , William Earley
IPC分类号： C07D487/06 , A61P1/00 , A61K31/439 , A61P25/32 , A61P29/00 , A61K31/55 , A61P25/22 , A61P25/28 , A61P25/16 , A61P35/00 , A61P25/08 , A61K31/5517 , A61P25/18
CPC分类号： C07D513/06 , A61K31/439 , A61K31/55 , A61K31/5517 , A61K45/06 , C07D453/02 , C07D487/04 , C07D513/04
摘要： Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
摘要翻译： 公开了新的5-HT 3受体调节剂。 这些化合物用于治疗各种疾病，包括化疗诱发的恶心和呕吐，术后恶心呕吐和肠易激综合征。 制备这些化合物的方法也在本发明中描述。
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10.发明授权Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权芳基和杂芳基取代的四氢异喹啉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：US08236796B2
公开(公告)日：2012-08-07
申请号：US12417598
申请日：2009-04-02
申请人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
发明人： Bruce F. Molino , Shuang Liu , Peter R. Guzzo , James P. Beck
IPC分类号： C07D403/04 , C07D217/02 , A61K31/47
CPC分类号： C07D417/04 , A61K31/4709 , A61K31/4741 , A61K31/4743 , A61K31/502 , A61K31/517 , A61K31/53 , C07D217/00 , C07D217/04 , C07D217/08 , C07D217/12 , C07D217/14 , C07D217/16 , C07D217/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.
摘要翻译： 本发明的化合物由式（I）中所示的化学结构表示：其中：指定为*的碳原子为R或S构型; 并且X是选自苯并呋喃基，苯并[b]噻吩基，苯并异噻唑基，苯并异恶唑基，吲唑基，吲哚基，异吲哚基，吲嗪基，苯并咪唑基，苯并恶唑基，苯并噻唑基，苯并三唑基，咪唑并[1,2-a ]吡啶基，吡唑并[1,5-a]吡啶基，[1,2,4]三唑并[4,3-a]吡啶基，噻吩并[2,3-b]吡啶基，噻吩并[3,2-b] 二氢苯并噻吩基，二氢苯并呋喃基，二氢苯并噻吩基，四氢萘基，喹啉基，异喹啉基，4H-喹啉基，9H-喹啉基，喹唑啉基，噌啉基，酞嗪基，喹喔啉基， 苯并[1,2,3]三嗪基，苯并[1,2,4]三嗪基，2H-色烯基，4H-色烯基和稠合的双环碳环或稠合双环杂环，其任选被如所定义的取代基（数目为1至4） 在R14; 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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