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公开(公告)号：US08809318B2
公开(公告)日：2014-08-19
申请号：US13128316
申请日：2009-11-11
申请人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
发明人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
IPC分类号： A61K31/553 , C07D498/04 , C07D498/14 , C07D498/20
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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![NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES](/abs-image/US/2015/10/08/US20150284411A1/abs.jpg.150x150.jpg)
公开(公告)号：US20150284411A1
公开(公告)日：2015-10-08
申请号：US14419774
申请日：2013-08-19
申请人： James M. APGAR , Ashok ARASAPPAN , Tesfaye BIFTU , Ping CHEN , Danqing FENG , Erin GUIDRY , Jacqueline HICKS , Ahmet KEKEC , Kenneth LEAVITT , Bing LI , Troy MCCRACKEN , Iyassu SEBHAT , Xiaoxia QIAN , Lan WEI , Robert WILKENING , Zhicai WU , Merck Sharp & Dohme Corp.
发明人： James M. Apgar , Ashok Arasappan , Tesfaye Biftu , Ping Chen , Danqing Feng , Erin Guidry , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Troy McCracken , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： C07D519/00 , A61K31/438 , A61K45/06 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/437 , A61K31/506
CPC分类号： C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US08450343B2
公开(公告)日：2013-05-28
申请号：US12746041
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert G. Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhu , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
发明人： Xianhai Huang , Anandan Palani , Jun Qin , Robert G. Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhu , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04 , C07D403/10 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号：US20110257156A1
公开(公告)日：2011-10-20
申请号：US13126056
申请日：2009-11-05
申请人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
发明人： Zhaoning Zhu , William J. Greenlee , David James Cole , Dmitri A. Pissarnitski , Gioconda V. Gallo , Hongmei Li , Hubert B. Josien , Jun Qin , Chad E. Knutson , Mihirbaran Mandal , Monica L. Vicarel , Murali Rajagopalan , Pawan Kumar Dhondi , Ruo Xu , Zhong-Yue Sun , Thomas A. Bara , Xianhai Huang , Xiaohong Zhu , Zhiqiang Zhao , John W. Clader , Anandan Palani , Theodros Asberom , Troy McCracken , Chad E. Bennett
IPC分类号： A61K31/55 , A61K31/5383 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/506 , A61K31/438 , A61K31/437 , C07D413/10 , C07D498/20 , C07D498/04 , A61P25/00 , A61P25/28 , A61K31/4245 , A61K31/5386
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了新颖的杂环化合物作为γ-分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这样的化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及治疗方法， 使用这种化合物或药物组合物预防，抑制或改善与中枢神经系统相关的一种或多种疾病。
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公开(公告)号：US20110015190A1
公开(公告)日：2011-01-20
申请号：US12746041
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhou , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
发明人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee , Hubert Josien , Wei Zhou , Xiaohong Zhou , Chad E. Bennett , Dmitri Pissarnitski , Mihirbaran Mandal , Pawan Dhondi , Troy McCracken , Thomas Bara , Zhiqiang Zhao , Duane Burnett , John Clader
IPC分类号： A61K31/5383 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61K31/5377 , C07D498/04 , C07D403/02 , A61K31/4178 , A61P25/28
CPC分类号： C07D471/04 , C07D403/10 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译： 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。
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公开(公告)号：US10358435B2
公开(公告)日：2019-07-23
申请号：US15554614
申请日：2016-03-11
申请人： Merck Sharp & Dohme Corp. , Dong-Ming Shen , Christopher J. Sinz , Alejandro Crespo , Johnathan E. Wilson , Troy McCracken , Shimin Xu , Haitang Li
发明人： Dong-Ming Shen , Christopher J. Sinz , Alejandro Crespo , Johnathan E. Wilson , Troy McCracken , Shimin Xu , Haitang Li
IPC分类号： C07D471/04 , C07D403/04 , C07D487/04 , A61K31/4192 , A61K31/4196 , A61K31/506 , C07D498/04 , A61P25/00
摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
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7.发明授权公开(公告)号：US08907086B2
公开(公告)日：2014-12-09
申请号：US14000641
申请日：2012-03-01
申请人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
发明人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
IPC分类号： C07D239/70 , C07D401/04 , C07D487/04 , A61K31/4523 , A61K31/517 , A61K31/52 , A61P3/10 , A61K45/06 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/64 , A61K31/522 , C07D473/28
CPC分类号： C07D487/04 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/522 , A61K31/64 , A61K45/06 , C07D473/18 , C07D473/28 , A61K2300/00
摘要： The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式（I）的新型双环杂环，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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8.发明申请FUSED BICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS 有权作为DIPEPTIDYL PEPTIDASE-IV抑制剂的FUSED BICYCLIC HETEROCYCLES有用公开(公告)号：US20130324562A1
公开(公告)日：2013-12-05
申请号：US14000641
申请日：2012-03-01
申请人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
发明人： Chad E. Bennett , Duane A. Burnett , Hongmei Li , Yonggang Chen , Troy McCracken , Monica Vicarel
IPC分类号： C07D487/04 , A61K45/06 , A61K31/522 , A61K31/519 , C07D473/28
CPC分类号： C07D487/04 , A61K31/155 , A61K31/427 , A61K31/519 , A61K31/522 , A61K31/64 , A61K45/06 , C07D473/18 , C07D473/28 , A61K2300/00
摘要： The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式（I）的新型双环杂环，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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公开(公告)号：US20120129846A1
公开(公告)日：2012-05-24
申请号：US13126680
申请日：2009-11-05
申请人： Zhaoning Zhu , William J. Greenlee , Mihir Baran Mandal , Duane A. Burnett , Chad E. Bennett , Troy McCracken
发明人： Zhaoning Zhu , William J. Greenlee , Mihir Baran Mandal , Duane A. Burnett , Chad E. Bennett , Troy McCracken
IPC分类号： A61K31/5386 , A61K31/53 , A61K31/55 , C07D498/04 , A61K31/5383 , A61P25/28 , A61K31/438 , C07D471/10 , C07D498/10 , C07D513/04 , C07D403/10 , C07D471/04 , A61K31/437
CPC分类号： C07D471/04 , C07D413/10 , C07D498/04 , C07D498/20 , C07F7/0812
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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公开(公告)号：US20110306593A1
公开(公告)日：2011-12-15
申请号：US13128316
申请日：2009-11-11
申请人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
发明人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
IPC分类号： A61K31/553 , C07D498/10 , C07D498/04 , A61P25/28 , C07D413/14 , C07D498/14 , A61K31/5395 , C07D498/20 , C07D413/10
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法 化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。
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