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1. 发明申请

US20110081297A1 Novel Substituted Pyrazoles, 1,2,4-Oxadiazoles, and 1,3,4-Oxadiazoles 审中-公开
标题翻译：新型取代的吡唑，1,2,4-恶二唑和1,3,4-恶二唑
公开(公告)号：US20110081297A1
公开(公告)日：2011-04-07
申请号：US12995412
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
IPC分类号： A61K49/10 , C07D413/04 , A61K31/4439 , A61P25/28 , A61K49/00 , A61K49/04 , C07D413/10 , A61K31/4245 , C07D231/12 , A61K31/415 , C07D471/02 , A61K31/437
CPC分类号： C07D231/12 , C07D271/06 , C07D271/10 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , F22B35/001 , F22B35/002 , F22B37/00 , F23C9/00 , F23J15/006 , F23J15/06 , F23L7/007 , Y02E20/344 , Y02E20/363
摘要： The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted pyrazole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者淀粉样斑块水平的变化来测量化合物的效果的新型淀粉样蛋白结合化合物和方法。更具体地说，本发明涉及在正电子发射断层摄影（PET）成像中使用本发明化合物作为示踪剂的方法，以在体内研究脑中的淀粉样蛋白沉积物以允许诊断阿尔茨海默氏病。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的吡唑衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

2. 发明授权

US08530483B2 Substituted azabenzoxazoles 有权
标题翻译：取代的氮杂苯并唑
公开(公告)号：US08530483B2
公开(公告)日：2013-09-10
申请号：US12995314
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg , Eric Hostetler
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg , Eric Hostetler
IPC分类号： A01N43/90 , A01N43/42 , A61K31/519 , A61K31/44 , C07D239/00 , C07D471/00 , C07D491/00 , C07D513/02 , C07D515/02 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
摘要翻译：本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH。

3. 发明申请

US20110212031A1 NOVEL SUBSTITUTED AZABENZOXAZOLES 审中-公开
标题翻译：新型取代的AZABENZOXAZOLES
公开(公告)号：US20110212031A1
公开(公告)日：2011-09-01
申请号：US13125939
申请日：2009-10-21
申请人： Cyrille Sur , David L. Williams
发明人： Cyrille Sur , David L. Williams
IPC分类号： A61K49/10 , A61P25/16 , A61K31/5377 , A61K49/00 , A61P25/28 , A61P25/18 , A61K31/437
CPC分类号： A61K31/519 , A61K51/0455 , A61K51/0463
摘要： The present invention relates to novel MAO-B binding compounds and methods for measuring effects of the compounds, by measuring changes of MAO-B levels in living patients. More specifically, the present invention relates to use of the compounds of this invention as therapeutic agents for inhibition of MAO-B activity as well as a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study MAO-B levels in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel MAO-B binding compounds as diagnostic, as we a therapeutic, agents. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者中MAO-B水平的变化来测量化合物的效果的新型MAO-B结合化合物和方法。更具体地，本发明涉及本发明化合物作为抑制MAO-B活性的治疗剂的用途以及使用本发明化合物作为正电子发射断层摄影（PET）成像中的示踪物来研究MAO的方法 -B水平在体内，以允许诊断阿尔茨海默病。因此，本发明涉及新型MAO-B结合化合物作为诊断的用途，作为治疗剂。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

4. 发明申请

US20110085985A1 NOVEL SUBSTITUTED AZABENZOXAZOLES 有权
标题翻译：新型取代的AZABENZOXAZOLES
公开(公告)号：US20110085985A1
公开(公告)日：2011-04-14
申请号：US12995314
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
IPC分类号： A61K31/437 , C07D498/04 , C07D519/00 , A61K31/5377 , A61K49/00 , A61K49/04 , A61K49/06 , A61P25/28 , A61P25/18
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH;
摘要翻译：本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH;

5. 发明申请

US20060233843A1 Treatment of psychosis with a muscarinic m1 receptor ectopic activator 审中-公开
标题翻译：用毒蕈碱m1受体异位活化剂治疗精神病
公开(公告)号：US20060233843A1
公开(公告)日：2006-10-19
申请号：US10545767
申请日：2004-02-17
申请人： P. Conn , Marlene Jacobson , Pierre Mallorga , Edward Scolnick , Cyrille Sur
发明人： P. Conn , Marlene Jacobson , Pierre Mallorga , Edward Scolnick , Cyrille Sur
IPC分类号： A61K31/5415 , A61K31/4439 , A61K31/4745 , A61K9/00
CPC分类号： A61K31/4439 , A61K31/00 , A61K31/335 , A61K31/4745 , A61K31/475 , A61K31/5415 , A61K31/55
摘要： A muscarinic M1 receptor ectopic activator, such as a muscarinic M1 receptor allosteric potentiator or a muscarinic M1 receptor ectopic agonist is useful, alone or in combination with other antipsychotic agents, for treating or preventing psychosis, such as a schizophrenic disorder or psychosis in Alzheimer's disease or bipolar disorder, for enhancing cognition and for neuropathic pain.
摘要翻译：毒蕈碱M1受体异位活化剂，例如毒蕈碱M1受体变构增强剂或毒蕈碱M1受体异位激动剂，单独使用或与其它抗精神病药联合用于治疗或预防精神病，如阿尔茨海默病中的精神分裂症或精神病或双相情感障碍，用于增强认知和神经性疼痛。

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