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1.发明公开(1,4-DIAZA-BICYCLO[3.2.2]NON-6-EN-4-YL)-HETEROCYCLYL-METHANONE LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, USEFUL FOR THE TREATMENT OF DISEASE 审中-公开（1,4-二氮杂双环[3.2.2]壬-6-烯-4-基）HETEROCYCLYLMETHANONLIGANDEN参与疾病治疗的烟碱乙酰胆碱受体是合适的
公开(公告)号：EP2212321A2
公开(公告)日：2010-08-04
申请号：EP08840882.8
申请日：2008-10-22
发明人： HERBERT, Brian , SCHUMACHER, Richard , DAI, Guangxiu , XIE, Wenge
IPC分类号： C07D453/00 , C07D307/78 , A61K31/4045 , A61K31/439
CPC分类号： C07D471/08 , C07D519/00
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds, which act as ligands for the a7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. The novel compounds include compounds of formula I: (I) wherein X, R1, and R2 are as herein defined.
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2.发明公开QUINOLINE AND ISOQUINOLINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS 审中-公开喹啉和异喹啉衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：EP1996574A1
公开(公告)日：2008-12-03
申请号：EP07752718.2
申请日：2007-03-08
发明人： LIU, Ruiping , ARRINGTON, Mark, P. , HOPPER, Allen, T. , CONTICELLO, Richard, D. , HITCHCOCK, Stephen, A.
IPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , A61K31/47 , A61P25/00 , A61P25/18
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention is directed to certain quinoline and isoquinoline compounds that are PDElO inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDElO enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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3.发明公开INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, PYRAZOLOPYRIDINES, ISOTHIAZOLOPYRIDINES, AND PREPARATION AND USES THEREOF 审中-公开吲唑，苯并噻唑，苯并异噻唑，异恶唑，吡唑并，ISOTHIAZOLOPYRIDINE和其生产和使用
公开(公告)号：EP1940833A1
公开(公告)日：2008-07-09
申请号：EP06815264.4
申请日：2006-09-22
发明人： SCHUMACHER, Richard , DANCA, Mihaela Diana , MA, Jianguo , HERBERT, Brian , NGUYEN, Truc Minh , XIE, Wenge , TEHIM, Ashok
IPC分类号： C07D453/02 , A61K31/435 , A61P25/00
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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公开(公告)号：EP1940819A1
公开(公告)日：2008-07-09
申请号：EP06801638.5
申请日：2006-08-16
发明人： ARRINGTON, Mark, Philip , CONTICELLO, Richard, D. , GAUSS, Carla, Maria , HITCHCOOK, Stephen , HOPPER, Allen , LIU, Ruiping , NGUYEN, Truc, Minh , TEHIM, Ashok
IPC分类号： C07D401/04 , C07D403/04 , C07D403/06 , C07D495/04 , C07D471/04 , A61K31/517 , A61P25/00 , A61P3/04
CPC分类号： C07D401/04 , C07D403/04 , C07D403/06 , C07D471/04 , C07D495/04
摘要： Provided are certain quinazolines of formular (I) or (II) that are PDElO inhibitors, pharmaceutical compositions, containing the same and processes for preparing the same. Also provided are methods of treating diseases treatable by PDElO enzyme such as obesity, non-insulin dependent diabetes, schizophrenia or bipolar disorder, obsessive-compulsive disorder, and the like, by administering those certain quinasolines .
摘要翻译： 提供的是作为PDE10抑制剂的式（I）或（II）的某些喹唑啉，含有其的药物组合物及其制备方法。 还提供了通过给予那些特定的喹喔啉治疗通过PDE10酶如肥胖症，非胰岛素依赖性糖尿病，精神分裂症或双相型障碍，强迫性障碍等可治疗的疾病的方法。
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5.发明授权INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, AND 1,2-BENZISOTHIAZOLES, AND PREPARATION AND USES THEREOF 有权吲哚，1H-吲唑，1,2-苯并异恶唑和-1,2-苯并异噻唑及其制备和应用
公开(公告)号：EP1697378B1
公开(公告)日：2007-11-21
申请号：EP04814981.9
申请日：2004-12-22
发明人： XIE, Wenge , HERBERT, Brian , MA. Jianguo , NGUYEN, Truc Minh , SCHUMACHER, Richard, A. , GAUSS, Carla-Maria , TEHIM, Ashok
IPC分类号： C07D487/18 , A61K31/4995 , A61P25/00
CPC分类号： C07D487/08
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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6.发明公开1 H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZIOSOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF 有权1H吲唑，苯并噻唑，1,2-苯并异恶唑，1,2-苯并异噻唑及其制备和用途和色酮
公开(公告)号：EP1745046A2
公开(公告)日：2007-01-24
申请号：EP05747486.8
申请日：2005-05-06
发明人： XIE, Wenge , HERBERT, Brian , SCHUMACHER, Richard A. , MA, Jianguo , NGUYEN, Truc, Minh , GAUSS, Carla, Maria , TEHIM, Ashok
IPC分类号： C07D471/08 , C07D487/08 , A61K31/4985 , A61K31/551 , A61P25/28
CPC分类号： C07D471/08 , C07D487/08
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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7.发明公开INDAZOLES, BENZOTHIAZOLES, BENZOISOTHIAZOLES, BENZISOXAZOLES, AND PREPARATION AND USES THEREOF 审中-公开吲唑，苯并噻唑，苯并异噻唑，异恶唑及其制备方法和用途
公开(公告)号：EP1735306A2
公开(公告)日：2006-12-27
申请号：EP05745169.2
申请日：2005-03-25
发明人： XIE, Wenge , HERBERT, Brian , SCHUMACHER, Richard , NGUYEN, Truc, Minh , MA, Jianguo , GAUSS, Carla, Maria , TEHIM, Ashok
IPC分类号： C07D453/02 , A61K31/439 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/32
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the a7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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公开(公告)号：EP1631568A1
公开(公告)日：2006-03-08
申请号：EP04759965.9
申请日：2004-04-16
IPC分类号： C07D407/12 , C07D407/04 , C07D403/04 , C07D231/12 , A61K31/4155 , A61P25/00
CPC分类号： C07D403/04 , C07D231/12 , C07D231/56 , C07D307/20 , C07D405/04 , C07D405/12 , C07D409/12
摘要： Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
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9.发明公开Benzoisothiazoles and preparation and uses thereof 审中-公开Benzisthiazole und deren Herstellung und Verwendungen
公开(公告)号：EP2336128A1
公开(公告)日：2011-06-22
申请号：EP10013706.6
申请日：2005-03-25
发明人： Xie, Wenge , Herbert, Brian , Schumacher, Richard , Nguyen, Truc, Minh , Ma, Jianguo , Gauss, Carla, Maria , Tehim, Ashok
IPC分类号： C07D453/02 , A61K31/439 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/32
CPC分类号： C07D453/02
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods and use thereof.
wherein
A is摘要翻译： 本发明一般涉及烟碱型乙酰胆碱受体（nACh受体）配体，nACh受体的活化以及与缺陷或功能异常的烟碱型乙酰胆碱受体，特别是脑相关的疾病状态的治疗领域。 此外，本发明涉及作为±7nACh受体亚型的配体的新化合物（例如吲唑和苯并噻唑），制备这种化合物的方法，含有这些化合物的组合物及其方法和用途。 其中A是
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10.发明授权1 H-INDAZOLES, BENZOTHIAZOLES, 1,2-BENZIOSOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND CHROMONES AND PREPARATION AND USES THEREOF 有权1H吲唑，苯并噻唑，1,2-苯并异恶唑，1,2-苯并异噻唑及其制备和用途和色酮
公开(公告)号：EP1745046B1
公开(公告)日：2011-04-13
申请号：EP05747486.8
申请日：2005-05-06
发明人： XIE, Wenge , HERBERT, Brian , SCHUMACHER, Richard A. , MA, Jianguo , NGUYEN, Truc, Minh , GAUSS, Carla, Maria , TEHIM, Ashok
IPC分类号： C07D471/08 , C07D487/08 , A61K31/4985 , A61K31/551 , A61P25/28
CPC分类号： C07D471/08 , C07D487/08
摘要： The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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