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公开(公告)号：US07842718B2
公开(公告)日：2010-11-30
申请号：US12576513
申请日：2009-10-09
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph Raymond Stock , George Diamantidis , Dennis Michael Kubrak , Kristina Martha Kutterer , William J. Moore , David S. Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph Raymond Stock , George Diamantidis , Dennis Michael Kubrak , Kristina Martha Kutterer , William J. Moore , David S. Casebier
IPC分类号： A61K31/381 , C07D333/34
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
摘要翻译： 提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。 描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法。
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2.发明申请Piperazine Metabotropic Glutamate Receptor 5 (MGLUR5) Negative Allosteric Modulators For Anxiety/Depression 审中-公开哌嗪代谢型谷氨酸受体5（MGLUR5）阴性变构调节剂用于焦虑/抑郁公开(公告)号：US20090325964A1
公开(公告)日：2009-12-31
申请号：US12470814
申请日：2009-05-22
IPC分类号： A61K31/53 , C07D401/14 , A61K31/497 , C07D251/30
CPC分类号： C07D213/74 , C07D241/20 , C07D295/192 , C07D401/12
摘要： The present teachings relate to piperazine metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators having Formula I: wherein the constituent variables are as defined herein. The present teachings further relate to methods for the preparation of the compounds, and to methods for using the compounds for treatment of diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety.
摘要翻译： 本教导涉及具有式I的哌嗪代谢型谷氨酸受体5（mGluR5）负变构调节剂：其中组成变量如本文所定义。 本教导还涉及制备化合物的方法，以及使用该化合物治疗包括精神分裂症，偏执狂症，抑郁症，躁狂抑郁症和焦虑症在内的疾病和病症的方法。
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3.发明申请公开(公告)号：US20100120725A1
公开(公告)日：2010-05-13
申请号：US12691193
申请日：2010-01-21
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
IPC分类号： A61K31/655 , A61K31/18 , G01N33/53 , C07C303/00 , C09B29/00
CPC分类号： C07C311/40 , A61K31/18 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/4245 , A61K31/655 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/29 , C07C323/49 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07D209/16 , C07D307/52 , C07D319/06
摘要： Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's disease and Down's syndrome are also described.
摘要翻译： 提供其中R 1 -R 8在本文中定义的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。 还描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默氏病和唐氏综合征的用途。
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公开(公告)号：US07022701B2
公开(公告)日：2006-04-04
申请号：US10828014
申请日：2004-04-20
IPC分类号： C07D513/04 , A61K31/416 , A61P25/18
CPC分类号： C07D471/04 , C07D513/04
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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公开(公告)号：US07488832B2
公开(公告)日：2009-02-10
申请号：US11352820
申请日：2006-02-13
申请人： Derek Cecil Cole , Eric Steven Manas , Lee Dalton Jennings , Frank Eldridge Lovering , Joseph Raymond Stock , William Jay Moore , John Watson Ellingboe , Jeffrey Scott Condon , Mohani Nirmala Sukhdeo , Ping Zhou , Junjun Wu , Koi Michele Morris
发明人： Derek Cecil Cole , Eric Steven Manas , Lee Dalton Jennings , Frank Eldridge Lovering , Joseph Raymond Stock , William Jay Moore , John Watson Ellingboe , Jeffrey Scott Condon , Mohani Nirmala Sukhdeo , Ping Zhou , Junjun Wu , Koi Michele Morris
IPC分类号： C07D207/325 , A61K31/4025
CPC分类号： C07D207/327 , C07D207/33 , C07D207/333 , C07D207/335 , C07D207/337 , C07D207/36 , C07D401/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译： 本发明提供了式I的吡唑基酰基喹啉化合物。本发明还提供了用于抑制β-分泌酶（BACE）和治疗β-淀粉样沉积物和神经原纤维缠结的方法。
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公开(公告)号：US20080287424A1
公开(公告)日：2008-11-20
申请号：US12173303
申请日：2008-07-15
申请人： Derek Cecil Cole , Eric Steven Manas , Lee Dalton Jennings , Frank Eldridge Lovering , Joseph Raymond Stock , William Jay Moore , John Watson Ellingboe , Jeffrey Scott Condon , Mohani Nirmala Sukhdeo , Ping Zhou , Junjun Wu , Koi Michele Morris
发明人： Derek Cecil Cole , Eric Steven Manas , Lee Dalton Jennings , Frank Eldridge Lovering , Joseph Raymond Stock , William Jay Moore , John Watson Ellingboe , Jeffrey Scott Condon , Mohani Nirmala Sukhdeo , Ping Zhou , Junjun Wu , Koi Michele Morris
IPC分类号： A61K31/541 , A61K31/40 , C07D207/327 , C07D401/10 , A61P25/28 , C12N9/99 , A61K31/454 , C07D417/10
CPC分类号： C07D207/327 , C07D207/33 , C07D207/333 , C07D207/335 , C07D207/337 , C07D207/36 , C07D401/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要： The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
摘要翻译： 本发明提供了式I的吡唑基酰基喹啉化合物。本发明还提供了用于抑制β-分泌酶（BACE）和治疗β-淀粉样沉积物和神经原纤维缠结的方法。
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公开(公告)号：US20070219240A1
公开(公告)日：2007-09-20
申请号：US11724078
申请日：2007-03-14
申请人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
发明人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
IPC分类号： A61K31/4709 , A61K31/454 , A61K31/4184 , A61K31/405 , C07D403/14
CPC分类号： C07D403/10 , C07D401/10 , C07D471/04 , C07D471/14
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译： 本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。
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公开(公告)号：US07820825B2
公开(公告)日：2010-10-26
申请号：US11724078
申请日：2007-03-14
申请人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
发明人： Derek Cecil Cole , Magda Asselin , Joseph Raymond Stock , Albert Jean Robichaud , Ji-In Kim , William Ronald Solvibile , Jonathan Laird Gross
IPC分类号： A61K31/41 , A61K31/415 , C07D207/00 , C07D233/00 , C07D249/00
CPC分类号： C07D403/10 , C07D401/10 , C07D471/04 , C07D471/14
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译： 本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。
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9.发明申请N-benzoyl- and N-benzylpyrrolidin-3-ylamines as histamine-3 antagonists 失效N-苯甲酰基和N-苄基吡咯烷-3-基胺作为组胺-3拮抗剂公开(公告)号：US20070270440A1
公开(公告)日：2007-11-22
申请号：US11804686
申请日：2007-05-18
IPC分类号： A61K31/52 , A61K31/519 , A61K31/517
CPC分类号： C07D207/14 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
摘要翻译： 本发明提供式I化合物及其用于治疗与组胺-3受体相关或受组胺3受体影响的中枢神经系统病症的用途。
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公开(公告)号：US07166622B2
公开(公告)日：2007-01-23
申请号：US10457641
申请日：2003-06-09
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
IPC分类号： C07C311/17 , C07D209/14 , C07D271/12 , C07D307/52 , C07D317/08 , A61K31/18 , A61K31/34 , A61K31/357 , A61K31/4245
CPC分类号： C07C311/40 , A61K31/18 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/4245 , A61K31/655 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/29 , C07C323/49 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07D209/16 , C07D307/52 , C07D319/06
摘要： Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.
摘要翻译： 提供了其中R 1 -R 8 - 8的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。 描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默病和唐氏综合征的用途。
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