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1.发明授权Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof 有权氮杂酮取代的azapolycycle MCH-1拮抗剂，其制备方法和用途公开(公告)号：US08618299B2
公开(公告)日：2013-12-31
申请号：US12828890
申请日：2010-07-01
IPC分类号： A61K31/44 , C07D471/00
CPC分类号： C07D471/14 , C07D471/22
摘要： MCH-1 receptor antagonists are disclosed having the general formula 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： 公开了具有通式的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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2.发明授权Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof 失效氮杂双环烷基 - 吲哚和氮杂双环链烷基 - 吡咯并 - 吡啶MCH-1拮抗剂，其制备方法和用途公开(公告)号：US08629158B2
公开(公告)日：2014-01-14
申请号：US12828855
申请日：2010-07-01
申请人： Peter R. Guzzo , Matthew David Surman , Alan John Henderson , Mark Hadden , Emily Elizabeth Freeman
发明人： Peter R. Guzzo , Matthew David Surman , Alan John Henderson , Mark Hadden , Emily Elizabeth Freeman
IPC分类号： A61K31/437 , A61K31/4412 , C07D471/18
CPC分类号： 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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![Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof](/abs-image/US/2014/01/28/US08637501B2/abs.jpg.150x150.jpg)
3.发明授权Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof 失效氮杂酮取代的氮杂环庚烯并[b]吲哚和吡啶并吡咯并吖庚因MCH-1拮抗剂，其制备方法和用途公开(公告)号：US08637501B2
公开(公告)日：2014-01-28
申请号：US12828807
申请日：2010-07-01
IPC分类号： A61P3/04 , A61P25/00 , A61K31/55 , C07D487/02
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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4.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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![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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![Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia](/abs-image/US/2015/06/30/US09067949B2/abs.jpg.150x150.jpg)
6.发明授权Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia 有权苯并呋喃并[3,2-c]吡啶和相关类似物作为血清素亚型6型（5-HT6）调节剂，用于治疗肥胖，代谢综合征，认知和精神分裂症公开(公告)号：US09067949B2
公开(公告)日：2015-06-30
申请号：US13352864
申请日：2012-01-18
申请人： Peter R. Guzzo , Alan J. Henderson , Matthew Isherwood , Chong Yew Lee , Animesh Ghosh , He Zhao
发明人： Peter R. Guzzo , Alan J. Henderson , Matthew Isherwood , Chong Yew Lee , Animesh Ghosh , He Zhao
IPC分类号： C07D491/048 , C07D307/91 , C07D491/18 , C07D491/08
CPC分类号： C07D491/048 , C07D307/91 , C07D491/08 , C07D491/18
摘要： The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.
摘要翻译： 本发明涉及作为血清素亚型6（5-HT6）调节剂的苯并呋喃并[3,2-c]吡啶和吖庚因类似物，包括这些化合物的药物组合物，其制备方法和用途。 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，精神分裂症，注意缺陷多动障碍，双相情感障碍，罕见和孤儿疾病以及睡眠障碍。 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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7.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：US08227486B2
公开(公告)日：2012-07-24
申请号：US12252823
申请日：2008-10-16
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： A01N43/42 , A61K31/47 , C07D217/00
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 below 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以下 本文定义的R1，R2，R3，R4，R5，R6，R7，R8和R14。
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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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