公开(公告)号：US09018391B2

公开(公告)日：2015-04-28

申请号：US14011183

申请日：2013-08-27

申请人： Yuri Bukhtiyarov ,  Salvacion Cacatian ,  Lawrence Wayne Dillard ,  Klaus Fuchs ,  Lanqi Jia ,  Deepak S. Lala ,  Angel Morales-Ramos ,  Suresh B. Singh ,  Shankar Venkatraman ,  Zhenrong Xu ,  Jing Yuan ,  Yi Zhao ,  Yajun Zheng ,  Cornelia Dorner-Ciossek ,  Ulrike Gross ,  Niklas Heine ,  Achim Sauer

发明人： Yuri Bukhtiyarov ,  Salvacion Cacatian ,  Lawrence Wayne Dillard ,  Klaus Fuchs ,  Lanqi Jia ,  Deepak S. Lala ,  Angel Morales-Ramos ,  Suresh B. Singh ,  Shankar Venkatraman ,  Zhenrong Xu ,  Jing Yuan ,  Yi Zhao ,  Yajun Zheng ,  Cornelia Dorner-Ciossek ,  Ulrike Gross ,  Niklas Heine ,  Achim Sauer

IPC分类号： C07D235/02 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D401/14 ,  A61K31/4184

CPC分类号： C07D235/02 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/506 ,  C07C49/747 ,  C07C49/755 ,  C07C229/50 ,  C07C255/59 ,  C07C313/06 ,  C07C331/26 ,  C07C2603/94 ,  C07C2603/97 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06

摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

摘要翻译： 本发明涉及螺环酰基胍及其作为分泌酶（BACE1）活性的抑制剂，含有它们的药物组合物的用途，以及将其用作治疗神经变性疾病的治疗剂的方法，其特征在于认知 衰退，认知障碍，痴呆和以淀粉样蛋白聚集体生产为特征的疾病。

公开(公告)号：US20140057927A1

公开(公告)日：2014-02-27

申请号：US14011183

申请日：2013-08-27

申请人： Yuri Bukhtiyarov ,  Salvacion Cacatian ,  Lawrence Wayne Dillard ,  Klaus Fuchs ,  Lanqi Jia ,  Deepak S. Lala ,  Angel Morales-Ramos ,  Suresh B. Singh ,  Shankar Venkatraman ,  Zhenrong Xu ,  Jing Yuan ,  Yi Zhao ,  Yajun Zheng ,  Cornelia Dorner-Ciossek ,  Ulrike Gross ,  Niklas Heine ,  Achim Sauer

发明人： Yuri Bukhtiyarov ,  Salvacion Cacatian ,  Lawrence Wayne Dillard ,  Klaus Fuchs ,  Lanqi Jia ,  Deepak S. Lala ,  Angel Morales-Ramos ,  Suresh B. Singh ,  Shankar Venkatraman ,  Zhenrong Xu ,  Jing Yuan ,  Yi Zhao ,  Yajun Zheng ,  Cornelia Dorner-Ciossek ,  Ulrike Gross ,  Niklas Heine ,  Achim Sauer

IPC分类号： C07D405/06 ,  C07D401/06 ,  C07D401/14 ,  C07D235/02 ,  C07D403/04

CPC分类号： C07D235/02 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/506 ,  C07C49/747 ,  C07C49/755 ,  C07C229/50 ,  C07C255/59 ,  C07C313/06 ,  C07C331/26 ,  C07C2603/94 ,  C07C2603/97 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06

摘要： The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

摘要翻译： 本发明涉及螺环酰基胍及其作为β-分泌酶（BACE1）活性抑制剂的用途，含有它们的药物组合物及其用作治疗神经变性疾病的治疗剂的方法，其特征在于认知衰退 ，认知障碍，痴呆和以β-淀粉样蛋白聚集体生产为特征的疾病。

公开(公告)号：US07695975B2

公开(公告)日：2010-04-13

申请号：US11159944

申请日：2005-06-23

申请人： Yuri Bukhtiyarov ,  Cathey M. Briggs ,  Laura J. Duggan

发明人： Yuri Bukhtiyarov ,  Cathey M. Briggs ,  Laura J. Duggan

IPC分类号： G01N33/00

CPC分类号： G01N33/84 ,  G01N31/22 ,  G01N33/4833 ,  G01N33/487 ,  G01N33/493 ,  G01N33/52 ,  Y10T436/206664

摘要： In some embodiments, the present invention pertains to a method for detecting an adulterant in a biological sample. A combination of a biological sample, an agent for detecting the adulterant and an ionic moiety capable of undergoing reduction by gaining electrons is provided in an assay medium. The combination is incubated under conditions sufficient for the ionic moiety to undergo reduction and for the agent for detecting the adulterant to interact with the adulterant. The reduction of the ionic moiety enhances the detection of the adulterant as a result of increasing the sensitivity of the agent for detecting the adulterant. The extent of interaction between the agent for detecting the adulterant and the adulterant is measured and is related to the presence or absence of the adulterant in the biological sample.

摘要翻译： 在一些实施方案中，本发明涉及用于检测生物样品中掺假剂的方法。 在测定介质中提供生物样品，用于检测掺杂剂的试剂和能够通过获得电子进行还原的离子部分的组合。 将该组合在足以使离子部分进行还原的条件下孵育，并且用于检测掺假剂与掺假剂相互作用的试剂。 由于增加了用于检测掺假剂的药剂的灵敏度，离子部分的减少增强了掺假剂的检测。 测量用于检测掺假剂和掺假剂的相互作用的程度，并与生物样品中掺假剂的存在或不存在相关。

公开(公告)号：US20060292699A1

公开(公告)日：2006-12-28

申请号：US11159944

申请日：2005-06-23

申请人： Yuri Bukhtiyarov ,  Cathey Briggs ,  Laura Duggan

发明人： Yuri Bukhtiyarov ,  Cathey Briggs ,  Laura Duggan

IPC分类号： G01N33/00

CPC分类号： G01N33/84 ,  G01N31/22 ,  G01N33/4833 ,  G01N33/487 ,  G01N33/493 ,  G01N33/52 ,  Y10T436/206664

摘要： In some embodiments, the present invention pertains to a method for detecting an adulterant in a biological sample. A combination of a biological sample, an agent for detecting the adulterant and an ionic moiety capable of undergoing reduction by gaining electrons is provided in an assay medium. The combination is incubated under conditions sufficient for the ionic moiety to undergo reduction and for the agent for detecting the adulterant to interact with the adulterant. The reduction of the ionic moiety enhances the detection of the adulterant as a result of increasing the sensitivity of the agent for detecting the adulterant. The extent of interaction between the agent for detecting the adulterant and the adulterant is measured and is related to the presence or absence of the adulterant in the biological sample.

摘要翻译： 在一些实施方案中，本发明涉及用于检测生物样品中掺假剂的方法。 在测定介质中提供生物样品，用于检测掺杂剂的试剂和能够通过获得电子进行还原的离子部分的组合。 将该组合在足以使离子部分进行还原的条件下孵育，并且用于检测掺假剂与掺假剂相互作用的试剂。 由于增加了用于检测掺假剂的药剂的灵敏度，离子部分的减少增强了掺假剂的检测。 测量用于检测掺假剂和掺假剂的相互作用的程度，并与生物样品中掺假剂的存在或不存在相关。

公开(公告)号：US08293188B2

公开(公告)日：2012-10-23

申请号：US12711970

申请日：2010-02-24

申请人： Yuri Bukhtiyarov ,  Cathey M Briggs ,  Laura J Duggan

发明人： Yuri Bukhtiyarov ,  Cathey M Briggs ,  Laura J Duggan

IPC分类号： G01N33/00

CPC分类号： G01N33/84 ,  G01N31/22 ,  G01N33/4833 ,  G01N33/487 ,  G01N33/493 ,  G01N33/52 ,  Y10T436/206664

摘要： In some embodiments, the present invention pertains to a method for detecting an adulterant in a biological sample. A combination of a biological sample, an agent for detecting the adulterant and an ionic moiety capable of undergoing reduction by gaining electrons is provided in an assay medium. The combination is incubated under conditions sufficient for the ionic moiety to undergo reduction and for the agent for detecting the adulterant to interact with the adulterant. The reduction of the ionic moiety enhances the detection of the adulterant as a result of increasing the sensitivity of the agent for detecting the adulterant. The extent of interaction between the agent for detecting the adulterant and the adulterant is measured and is related to the presence or absence of the adulterant in the biological sample.

摘要翻译： 在一些实施方案中，本发明涉及用于检测生物样品中掺假剂的方法。 在测定介质中提供生物样品，用于检测掺杂剂的试剂和能够通过获得电子进行还原的离子部分的组合。 将该组合在足以使离子部分进行还原的条件下孵育，并且用于检测掺假剂与掺假剂相互作用的试剂。 由于增加了用于检测掺假剂的药剂的灵敏度，离子部分的减少增强了掺假剂的检测。 测量用于检测掺假剂和掺假剂的相互作用的程度，并与生物样品中掺假剂的存在或不存在相关。

公开(公告)号：US20100150778A1

公开(公告)日：2010-06-17

申请号：US12711970

申请日：2010-02-24

申请人： Yuri Bukhtiyarov ,  Cathey M. Briggs ,  Laura J. Duggan

发明人： Yuri Bukhtiyarov ,  Cathey M. Briggs ,  Laura J. Duggan

IPC分类号： G01N33/48

CPC分类号： G01N33/84 ,  G01N31/22 ,  G01N33/4833 ,  G01N33/487 ,  G01N33/493 ,  G01N33/52 ,  Y10T436/206664

摘要： In some embodiments, the present invention pertains to a method for detecting an adulterant in a biological sample. A combination of a biological sample, an agent for detecting the adulterant and an ionic moiety capable of undergoing reduction by gaining electrons is provided in an assay medium. The combination is incubated under conditions sufficient for the ionic moiety to undergo reduction and for the agent for detecting the adulterant to interact with the adulterant. The reduction of the ionic moiety enhances the detection of the adulterant as a result of increasing the sensitivity of the agent for detecting the adulterant. The extent of interaction between the agent for detecting the adulterant and the adulterant is measured and is related to the presence or absence of the adulterant in the biological sample.

摘要翻译： 在一些实施方案中，本发明涉及用于检测生物样品中掺假剂的方法。 在测定培养基中提供生物样品，用于检测掺假剂的试剂和能够通过获得电子进行还原的离子部分的组合。 将该组合在足以使离子部分进行还原的条件下孵育，并且用于检测掺假剂与掺假剂相互作用的试剂。 由于增加了用于检测掺假剂的药剂的灵敏度，离子部分的减少增强了掺假剂的检测。 测量用于检测掺假剂和掺假剂的相互作用的程度，并与生物样品中掺假剂的存在或不存在相关。