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51. 发明申请

US20110243940A1 BICYCLIC PYRANONE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：双相PYRANONE衍生物及其使用方法
公开(公告)号：US20110243940A1
公开(公告)日：2011-10-06
申请号：US13139890
申请日：2009-12-15
申请人： Dong Xiao , Anandan Palani , Xianhai Huang , Xiaohong Zhu , Robert G. Aslanian
发明人： Dong Xiao , Anandan Palani , Xianhai Huang , Xiaohong Zhu , Robert G. Aslanian
IPC分类号： A61K39/395 , C07D491/052 , A61K31/435 , A61K31/505 , A61K31/47 , A61K31/397 , A61K31/60 , A61K31/4162 , A61P3/10 , A61P35/00 , A61P11/00 , A61P1/00 , A61P25/00 , A61P3/04
CPC分类号： C07D491/052
摘要： The present invention relates to Bicyclic Pyranone Derivatives, their compositions and uses for treating or preventing a metabolic disorder, dyslipidemia, a cardiovascular disease, a neurological disorder, a hematological disease, cancer, inflammation, a respiratory disease, a gastroenterological disease, diabetes, a diabetic complication, obesity, an obesity-related disorder or non-alcoholic fatty liver disease. Formula (I). Y is —C— when an optional and additional bond is present and Y is —CH— when an optional and additional bond is not present; Z is —O—, —NH— or —N(alkyl)- when the optional and additional bond between Y and Z Is absent, and Z Is —N— when the optional and additional bond between Y and Z is present; R1 is H1 halo or —CN; R2 is alkyl, alkenyl or -(alkyleneVcydoalkyl; t is 0 or 1; R3 is O when the optional and additional bond between Y and R3 is present, and R3 is alkyl.haloalkyl.—C(0)0R5.-alkylene-O-alkyt or —O-alkyl when the optional and additional bond between Y and R3 is absent: R4 is H, alkyl or aryl, wherein an aryl group can be unsubstituted or optionally substituted.
摘要翻译：本发明涉及双环吡喃酮衍生物，其组合物和用于治疗或预防代谢紊乱，血脂异常，心血管疾病，神经障碍，血液病，癌症，炎症，呼吸系统疾病，胃肠病，糖尿病，糖尿病并发症，肥胖症，肥胖相关障碍或非酒精性脂肪性肝病。式（I）。当不存在任选和另外的键时，当存在任选的附加键且Y是-CH-时，Y是-C-; 当Y和Z之间的任选和另外的键不存在时，Z是-O - ， - NH-或-N（烷基），当存在Y和Z之间的任选的和另外的键时，Z是 - R1为H1卤素或-CN; R 2是烷基，烯基或 - （亚烷基二烷基; t是0或1;当存在Y和R 3之间的任选和另外的键时，R 3是O，R 3是烷基卤代烷基-C（O） - 烷基或-O-烷基，当Y和R3之间的任选和另外的键不存在时：R4是H，烷基或芳基，其中芳基可以是未取代的或任选被取代的。

52. 发明授权

US08026364B2 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US08026364B2
公开(公告)日：2011-09-27
申请号：US12750420
申请日：2010-03-30
申请人： Sapna S. Shah , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Laci Wrobleski , Ashwin U. Rao , Cheng Wang , Neng-Yang Shih
发明人： Sapna S. Shah , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Laci Wrobleski , Ashwin U. Rao , Cheng Wang , Neng-Yang Shih
IPC分类号： C07F7/02 , C07D215/12 , C07D215/16 , C07D213/02 , C07D211/02 , C07D405/00
CPC分类号： C07D401/04 , A61K31/4178 , A61K31/451 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/573 , A61K45/06 , C07D211/56 , C07D211/60 , C07D211/66 , C07D211/76 , C07D413/04 , C07D417/04 , C07D498/20
摘要： A compound having the general structure shown in Formula I: or pharmaceutically acceptable salt and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
摘要翻译：具有式I所示的一般结构的化合物或其药学上可接受的盐和/或溶剂合物可用于治疗由NK1受体介导的疾病或病症，例如各种生理疾病，症状或疾病，包括呕吐，抑郁，焦虑和咳嗽。

53. 发明申请

US20100297128A1 GAMMA SECRETASE MODULATORS 有权
标题翻译： GAMMA秘密调节器
公开(公告)号：US20100297128A1
公开(公告)日：2010-11-25
申请号：US12747011
申请日：2008-12-09
申请人： Xianhai Huang , Anandan Palani , Robert G. Aslanian
发明人： Xianhai Huang , Anandan Palani , Robert G. Aslanian
IPC分类号： A61K39/395 , C07D487/04 , C07D471/04 , C07D473/32 , A61K31/5025 , A61K31/437 , A61K31/52 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04 , C07D471/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula [Chemical formula should be inserted here as it appears on abstract in electronic form.] 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。化合物具有式[化学式应该插入在此，其以电子形式的摘要出现。]还公开了使用式（I）化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。

54. 发明申请

US20060258665A1 Bridged ring NK1 antagonists 失效
标题翻译：桥环NK1拮抗剂
公开(公告)号：US20060258665A1
公开(公告)日：2006-11-16
申请号：US11291363
申请日：2005-12-01
申请人： Dong Xiao , Anandan Palani , Cheng Wang , Hon-Chung Tsui , Xianhai Huang , Sapna Shah , Ashwin Rao , Xiao Chen , Sunil Paliwal , Neng-Yang Shih
发明人： Dong Xiao , Anandan Palani , Cheng Wang , Hon-Chung Tsui , Xianhai Huang , Sapna Shah , Ashwin Rao , Xiao Chen , Sunil Paliwal , Neng-Yang Shih
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D471/08
摘要： A compound having the general structure shown in Formula (I): or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
摘要翻译：具有式（I）所示的一般结构的化合物或其药学上可接受的盐和/或溶剂化物可用于治疗由NK 1受体介导的疾病或病症，例如各种生理紊乱，症状或疾病包括呕吐，抑郁，焦虑和咳嗽。

55. 发明授权

US08754216B2 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US08754216B2
公开(公告)日：2014-06-17
申请号：US13245403
申请日：2011-09-26
申请人： Sapna S. Shah , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Laci Wrobleski , Ashwin U. Rao , Cheng Wang , Neng-Yang Shih
发明人： Sapna S. Shah , Anandan Palani , Xianhai Huang , Dong Xiao , Sunil Paliwal , Hon-Chung Tsui , Michelle Laci Wrobleski , Ashwin U. Rao , Cheng Wang , Neng-Yang Shih
IPC分类号： C07F7/02 , C07D215/12 , C07D215/16 , C07D213/02 , C07D405/00
CPC分类号： C07D401/04 , A61K31/4178 , A61K31/451 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/573 , A61K45/06 , C07D211/56 , C07D211/60 , C07D211/66 , C07D211/76 , C07D413/04 , C07D417/04 , C07D498/20
摘要： A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
摘要翻译：具有式I所示的一般结构的化合物或其药学上可接受的盐和/或溶剂合物可用于治疗由NK1受体介导的疾病或病症，例如各种生理疾病，症状或疾病，包括呕吐，抑郁，焦虑和咳嗽。

56. 发明申请

US20100255005A1 GAMMA SECRETASE MODULATORS 失效
公开(公告)号：US20100255005A1
公开(公告)日：2010-10-07
申请号：US12600910
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
IPC分类号： A61K39/395 , C07D498/04 , A61K31/437 , A61P25/28 , A61P29/00 , A61K39/00 , A61P27/06 , A61P9/10 , A61P27/00 , A61K31/5383 , C07D413/10 , A61K31/423 , A61K31/5025 , A61K31/4245 , A61K31/4439 , C07D498/14 , A61K31/445 , A61K31/473 , A61K38/17
CPC分类号： C07D498/04 , C07D413/10
摘要： In its many embodiments, the present invention provides a novel class of 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.

57. 发明授权

US08759337B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08759337B2
公开(公告)日：2014-06-24
申请号：US13140987
申请日：2009-12-18
申请人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
发明人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
IPC分类号： A61K31/553 , C07D498/04
CPC分类号： C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). 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。这些化合物具有式（化学式应该插在这里，如纸上所示）。还公开了使用式（I）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。

58. 发明授权

US08580956B2 Gamma secretase modulators 失效
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08580956B2
公开(公告)日：2013-11-12
申请号：US12600910
申请日：2008-05-28
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Ruo Xu , Xianhai Huang , Xiaohong Zhu
IPC分类号： C07D498/04 , C07D498/14 , A61K31/4245 , A61K31/5365 , A61K31/5383
CPC分类号： C07D498/04 , C07D413/10
摘要： In its many embodiments, the present invention provides a novel class of 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，本发明提供了一类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这类化合物的药物制剂的方法和方法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。

59. 发明授权

US08487099B2 Gamma secretase modulators 失效
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08487099B2
公开(公告)日：2013-07-16
申请号：US12739315
申请日：2008-11-03
申请人： William J. Greenlee , Zhaoning Zhu , Theodros Asberom , Xianhai Huang , Hubert B. Josien
发明人： William J. Greenlee , Zhaoning Zhu , Theodros Asberom , Xianhai Huang , Hubert B. Josien
IPC分类号： C07D487/10 , C07D487/20 , C07D493/10 , C07D493/20 , C07D493/22 , C07F7/08 , C07F9/6571 , A61K31/397 , A61K31/4245 , A61K31/438 , A61P25/28
CPC分类号： C07D498/10 , C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/20 , C07D498/22 , C07F7/0812 , C07F9/657181
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). 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。化合物具有式（I）。还公开了使用式（I）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。

60. 发明申请

US20120107328A1 GAMMA SECRETASE MODULATORS 失效
标题翻译： GAMMA秘密调节器
公开(公告)号：US20120107328A1
公开(公告)日：2012-05-03
申请号：US12739315
申请日：2008-11-03
申请人： William J. Greenlee , Zhaoning Zhu , Theodros Asberom , Xianhai Huang , Hubert B. Josien
发明人： William J. Greenlee , Zhaoning Zhu , Theodros Asberom , Xianhai Huang , Hubert B. Josien
IPC分类号： A61K39/395 , C07D498/20 , C07F7/10 , C07F9/6574 , C07D498/22 , A61K31/438 , A61K31/5386 , A61K31/695 , A61K31/675 , A61K31/5395 , A61K31/53 , A61P29/00 , A61P25/28 , A61P27/06 , A61P25/00 , A61P9/00 , C07D498/10
CPC分类号： C07D498/10 , C07D487/10 , C07D487/20 , C07D493/20 , C07D495/20 , C07D498/20 , C07D498/22 , C07F7/0812 , C07F9/657181
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I). 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。化合物具有式（I）。还公开了使用式（I）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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