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1. 发明授权

US09708313B2 Substituted pyrido[3,4-b]pyrazines as GPR6 modulators 有权
公开(公告)号：US09708313B2
公开(公告)日：2017-07-18
申请号：US14883174
申请日：2015-10-14
申请人： Jason W. Brown , Stephen Hitchcock , Maria Hopkins , Shota Kikuchi , Holger Monenschein , Holly Reichard , Kristin Schleicher , Huikai Sun , Todd Macklin
发明人： Jason W. Brown , Stephen Hitchcock , Maria Hopkins , Shota Kikuchi , Holger Monenschein , Holly Reichard , Kristin Schleicher , Huikai Sun , Todd Macklin
IPC分类号： C07D241/38 , C07D471/04
CPC分类号： C07D471/04
摘要： This present invention provides compounds of formula II: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

2. 发明授权

US08633315B2 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US08633315B2
公开(公告)日：2014-01-21
申请号：US13427802
申请日：2012-03-22
申请人： Wenge Zhong , Stephen Hitchcock , Patel F. Vinod , Michael Croghan , Bryant Yang
发明人： Wenge Zhong , Stephen Hitchcock , Patel F. Vinod , Michael Croghan , Bryant Yang
IPC分类号： C07D491/107 , C07D311/96 , C07D471/10
CPC分类号： C07D491/107 , C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中R 1a，R 1b，R 1c，B，W，R 3，R 4和R 5在本文中定义。在另一个实施方案中，本发明提供通式II的化合物，其中A1，A2，A3，A4，R1a，R1b，R1c，R2，R4，R5，W，X和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。

3. 发明授权

US08552181B2 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US08552181B2
公开(公告)日：2013-10-08
申请号：US13410201
申请日：2012-03-01
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Walker , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang , Russell Graceffa
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Scott Harried , Daniel Horne , Ted Judd , Matthew Walker , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Matthew Weiss , Qiufen Xue , Bryant Yang , Russell Graceffa
IPC分类号： C07D471/10 , C07D491/107 , C07D495/10
CPC分类号： C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase activity and for the treatment of diseases, including Alzheimer's disease (AD) and related CNS conditions, mediated thereby. In one embodiment, the compounds have a general Formula I or Formula II wherein R1a-1c, B, R3-5 and W of Formula I, and R1a-1c, R2-5, A1-4, W, X, Z, m and n of Formula II are defined herein. The invention further provides compounds of Formula III and IV and sub-Formulas II-A-II-D and III-A-III-D. The compounds may be used in pharmaceutical compositions for treating, prophylactically or therapeutically, disorders related to the activity of beta-secretase protein, including without limitation, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.
摘要翻译：本发明包括可用于调节β-分泌酶活性和用于治疗包括阿尔茨海默病（AD）和相关CNS病症在内的疾病的新一类化合物。在一个实施方案中，化合物具有通式I或式II，其中式I的R 1a-1c，B，R 5-5和W，以及R 1a-1c，R 2-5，A1-4，W，X，Z，m 并且式II的n定义在本文中。本发明进一步提供式III和IV的化合物和式II-A-II-D和III-A-III-D的化合物。该化合物可用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病的药物组合物，包括但不限于AD，认知缺陷和损伤，精神分裂症和其它类似的中枢神经系统疾病。

4. 发明申请

US20110118250A1 BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
标题翻译： BETA-SECRETASE调制器和使用方法
公开(公告)号：US20110118250A1
公开(公告)日：2011-05-19
申请号：US12909566
申请日：2010-10-21
申请人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
发明人： Brian K. Albrecht , Denise Lyn Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart C. Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod F. Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang , Wenge Zhong
IPC分类号： A61K31/538 , C07D405/12 , A61K31/4433 , A61K31/444 , C07D405/14 , A61K31/4439 , A61K31/506 , A61K31/497 , C07D413/12 , A61K31/5377 , A61K31/4178 , A61K31/4545 , A61K31/453 , C07D311/96 , A61K31/352 , C07D407/12 , A61K31/4709 , C07D401/12 , C07D409/12 , A61K31/422 , A61K31/4025 , C07D471/04 , A61K31/501 , A61P25/28 , A61P25/00 , A61P25/16
CPC分类号： C07D405/12 , C07D413/12
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默氏病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中A，B，R 3，R 4，R 5，i和j在本文中定义。本发明还包括药物组合物，其包括一种或多种式I化合物，这些化合物的使用方法，包括治疗AD和相关疾病，通过给受试者施用式I化合物或包含它们的组合物。本发明还包括式II和III的其它实施方案，可用于制备本发明化合物的中间体和方法。

5. 发明申请

US20090036478A1 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20090036478A1
公开(公告)日：2009-02-05
申请号：US12154497
申请日：2008-05-23
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
IPC分类号： A61K31/438 , C07D221/20 , C07D233/54 , A61K31/4178 , A61P25/28 , A61P25/00
CPC分类号： C07D491/107 , C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein.The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中R 1a，R 1b，R 1c，B，W，R 3，R 4和R 5在本文中定义。在另一个实施方案中，本发明提供通式II的化合物，其中A1，A2，A3，A4，R1a，R1b，R1c，R2，R4，R5，W，X和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。

6. 发明申请

US20060154922A1 Muscarinic agonists 审中-公开
标题翻译：毒蕈碱激动剂
公开(公告)号：US20060154922A1
公开(公告)日：2006-07-13
申请号：US10546910
申请日：2004-03-12
申请人： Jennifer Allen , Stephen Hitchcock , William Turner , Bin Liu
发明人： Jennifer Allen , Stephen Hitchcock , William Turner , Bin Liu
IPC分类号： A61K31/54 , A61K31/537 , C07D279/12 , C07D211/06 , C07D265/30 , A61K31/445
CPC分类号： C07D409/12 , C07D207/22 , C07D211/72 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06
摘要： The present invention relates to compounds of Formula (I): which are agonists of the M-1 muscarinic receptor.
摘要翻译：本发明涉及式（I）化合物：它是M-1毒蕈碱受体的激动剂。

7. 发明申请

US20120220583A1 SUBSTITUTED HYDROXYETHYL AMINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权
标题翻译：取代的羟基乙胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US20120220583A1
公开(公告)日：2012-08-30
申请号：US13410201
申请日：2012-03-01
申请人： Wenge ZHONG , Stephen HITCHCOCK , Vinod F. PATEL , Michael CROGHAN , Thomas DINEEN , Scott HARRIED , Daniel HORNE , Ted JUDD , Matthew KALLER , Charles KREIMAN , Patricia LOPEZ , Holger MONENSCHEIN , Thomas NGUYEN , Matthew WEISS , Qiufen XUE , Bryant YANG , Russell GRACEFFA
发明人： Wenge ZHONG , Stephen HITCHCOCK , Vinod F. PATEL , Michael CROGHAN , Thomas DINEEN , Scott HARRIED , Daniel HORNE , Ted JUDD , Matthew KALLER , Charles KREIMAN , Patricia LOPEZ , Holger MONENSCHEIN , Thomas NGUYEN , Matthew WEISS , Qiufen XUE , Bryant YANG , Russell GRACEFFA
IPC分类号： A61K31/438 , C07D495/10 , A61P25/00 , A61K31/5377 , A61P25/28 , C07D471/10 , C07D491/107
CPC分类号： C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase activity and for the treatment of diseases, including Alzheimer's disease (AD) and related CNS conditions, mediated thereby. In one embodiment, the compounds have a general Formula I or Formula II wherein R1a-1c, B, R3-5 and W of Formula I, and R1a-1c, R2-5, A1-4, W, X, Z, m and n of Formula II are defined herein. The invention further provides compounds of Formula III and IV and sub-Formulas II-A-II-D and III-A-III-D. The compounds may be used in pharmaceutical compositions for treating, prophylactically or therapeutically, disorders related to the activity of beta-secretase protein, including without limitation, AD, cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.
摘要翻译：本发明包括可用于调节β-分泌酶活性和用于治疗包括阿尔茨海默病（AD）和相关CNS病症在内的疾病的新一类化合物。在一个实施方案中，化合物具有通式I或式II，其中式I的R 1a-1c，B，R 5-5和W，以及R 1a-1c，R 2-5，A1-4，W，X，Z，m 并且式II的n定义在本文中。本发明进一步提供式III和IV的化合物和式II-A-II-D和III-A-III-D的化合物。该化合物可用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病的药物组合物，包括但不限于AD，认知缺陷和损伤，精神分裂症和其它类似的中枢神经系统疾病。

8. 发明授权

US08173810B2 Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use 有权
标题翻译：取代的羟乙基胺化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：US08173810B2
公开(公告)日：2012-05-08
申请号：US12154497
申请日：2008-05-23
申请人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
发明人： Wenge Zhong , Stephen Hitchcock , Vinod F. Patel , Michael Croghan , Thomas Dineen , Daniel Horne , Matthew Kaller , Charles Kreiman , Patricia Lopez , Holger Monenschein , Thomas Nguyen , Lewis Pennington , Qiufen Xue , Bryant Yang , Yuan Cheng
IPC分类号： A61K31/438 , A61P25/28 , C07D491/107
CPC分类号： C07D491/107 , C07D221/06 , C07D311/96 , C07D471/10 , C07D491/10 , C07D493/10 , C07D495/10
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中R 1a，R 1b，R 1c，B，W，R 3，R 4和R 5在本文中定义。在另一个实施方案中，本发明提供通式II的化合物，其中A1，A2，A3，A4，R1a，R1b，R1c，R2，R4，R5，W，X和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。这些疾病包括例如阿尔茨海默病（AD），认知缺陷和损伤，精神分裂症和其他类似的中枢神经系统疾病。本发明还包括式II的其它实施方案，可用于制备式I和II化合物的中间体和方法。

9. 发明申请

US20110251199A1 NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS AND METHODS OF USE 失效
标题翻译：含氮的双环杂环化合物及其使用方法
公开(公告)号：US20110251199A1
公开(公告)日：2011-10-13
申请号：US13163666
申请日：2011-06-17
申请人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel M. Retz , Adrian L. Smith , Jiawang Zhu
发明人： Frenel F. De Morin , Jian J. Chen , Elizabeth M. Doherty , Stephen Hitchcock , Qi Huang , Joseph L. Kim , Gang Liu , Thomas Nixey , Nick A. Paras , Jeffrey Petkus , Daniel M. Retz , Adrian L. Smith , Jiawang Zhu
IPC分类号： A61K31/502 , A61K31/517 , A61P35/00 , A61K31/506 , C07D403/10 , C07D413/14 , C07D417/10 , C07D401/14
CPC分类号： C07D401/14 , C07D239/84 , C07D239/95 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译：本发明包括能够调节Raf激酶的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。该化合物具有通式Ⅰ和A1，A2，A3，A4，X，Z，Z'，R1，R2，R3，R4，R5和R6的定义。本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

10. 发明申请

US20070299067A1 Quinoline and isoquinoline derivatives as phosphodiesterase 10 inhibitors 审中-公开
标题翻译：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：US20070299067A1
公开(公告)日：2007-12-27
申请号：US11716307
申请日：2007-03-08
申请人： Ruiping Liu , Mark Arrington , Allen Hopper , Richard Conticello , Stephen Hitchcock
发明人： Ruiping Liu , Mark Arrington , Allen Hopper , Richard Conticello , Stephen Hitchcock
IPC分类号： A61K31/535 , A61K31/47 , A61P25/00 , C07D217/00 , C07D217/22 , C07D413/00
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 PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：本发明涉及某些属于PDE10抑制剂的喹啉和异喹啉化合物，含有这些化合物的药物组合物及其制备方法。本发明还涉及治疗由PDE10酶介导的疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相障碍，强迫症等。

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