公开(公告)号：WO2011090911A1

公开(公告)日：2011-07-28

申请号：PCT/US2011/021423

申请日：2011-01-14

Applicant: AMGEN INC. ,  PARAS, Nick A, ,  BROWN, James ,  CHENG, Yuan ,  HITCHCOCK, Stephen ,  JUDD, Ted ,  LOPEZ, Patricia ,  MINATTI, Ana Elena ,  NIXEY, Thomas ,  POWERS, Timothy ,  TEGLEY, Christopher M. ,  XUE, Qiufen ,  YANG, Bryant ,  ZHONG, Wenge

Inventor： PARAS, Nick A, ,  BROWN, James ,  CHENG, Yuan ,  HITCHCOCK, Stephen ,  JUDD, Ted ,  LOPEZ, Patricia ,  MINATTI, Ana Elena ,  NIXEY, Thomas ,  POWERS, Timothy ,  TEGLEY, Christopher M. ,  XUE, Qiufen ,  YANG, Bryant ,  ZHONG, Wenge

IPC: C07D215/38 ,  C07D401/10 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D413/10 ,  C07D471/04 ,  C07D471/08 ,  C07D498/08 ,  A61K31/47 ,  A61K31/4709 ,  A61P25/28

CPC classification number: C07D401/10 ,  C07D215/38 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D413/10 ,  C07D471/04 ,  C07D471/08 ,  C07D498/08

Abstract: 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 ring A, B 1 , B 2 , B 3 , L, R 1 , R 2 , ring Z, m and n of Formula I 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, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).

Abstract translation: 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）; 其中式I中的环A，B1，B2，B3，L，R1，R2，环Z，m和n定义在本文中。 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疾病和病症的用途。 这些疾病包括例如阿尔茨海默氏病（AD），认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式（I）的其它实施方案，可用于制备式（I）化合物的中间体和方法。

公开(公告)号：WO2008083323A9

公开(公告)日：2008-09-12

申请号：PCT/US2007089113

申请日：2007-12-28

Applicant: INVITROGEN CORP ,  DEES ROBERT ,  DEMBROW DALE ,  HENRY BRENT ,  KAHATT ESPIR ,  POWERS TIMOTHY ,  ROMAN STEVEN ,  ROSSIO JEFFREY ,  MEEGAN JAMES

Inventor： DEES ROBERT ,  DEMBROW DALE ,  HENRY BRENT ,  KAHATT ESPIR ,  POWERS TIMOTHY ,  ROMAN STEVEN ,  ROSSIO JEFFREY ,  MEEGAN JAMES

IPC: G01N33/50 ,  G01N33/53

CPC classification number: G01N33/54373

Abstract: The present invention relates to, in part, methods, reagents and apparatuses for the detection of agents. The present invention also relates, in part, to compositions including, but not limited to, flow cells, assay chambers, reagent reservoir delivery units and devices for holding an assay chamber. The present invention also provides various components and combinations of components for various detection apparatuses. The present invention also relates to a portable agent detection apparatus that can be used in the field or at a point of care and is not limited to specialized laboratories or limited to use by highly skilled users.

Abstract translation: 本发明部分涉及用于检测试剂的方法，试剂和装置。 本发明还部分涉及包括但不限于流动池，测定室，试剂储存器输送单元和用于保持测定室的装置的组合物。 本发明还提供了用于各种检测装置的各种部件和组件的组合。 本发明还涉及一种便携式检测装置，其可以在现场使用或在一个关注点处使用，并且不限于专门的实验室或被高技能用户使用。

公开(公告)号：WO2007079199A2

公开(公告)日：2007-07-12

申请号：PCT/US2006/049521

申请日：2006-12-28

Applicant: ALANTOS PHARMACEUTICALS, INC. ,  SUCHOLEIKI, Irving ,  POWERS, Timothy ,  GEGE, Christian ,  BLUHM, Harald ,  DODD, Rory ,  DENG, Hongbo ,  WU, Xinyuan ,  STEENECK, Christoph

Inventor： SUCHOLEIKI, Irving ,  POWERS, Timothy ,  GEGE, Christian ,  BLUHM, Harald ,  DODD, Rory ,  DENG, Hongbo ,  WU, Xinyuan ,  STEENECK, Christoph

IPC: C07D239/28 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D403/12 ,  C07D239/28 ,  C07D409/12 ,  C07D417/12

Abstract: This invention relates to substituted bis-amide pyrimidine compounds of Formula (I), which are useful for the treatment of metalloprotease mediated diseases, in particular MMP-13 related diseases.

Abstract translation: 本发明涉及式（I）的取代双酰胺嘧啶化合物，其可用于治疗金属蛋白酶介导的疾病，特别是MMP-13相关疾病。

公开(公告)号：WO2006128184A3

公开(公告)日：2007-03-08

申请号：PCT/US2006020970

申请日：2006-05-22

Applicant: ALANTOS PHARMACEUTICALS INC ,  STEENECK CHRISTOPH ,  GEGE CHRISTIAN ,  RICHTER FRANK ,  HOCHGUERTEL MATTHIAS ,  FEURSTEIN TIM ,  BLUHM HARALD ,  SUCHOLEIKI IRVING ,  BOER JURGEN ,  WU XINYUAN ,  SCHNEIDER MATTHIAS ,  NOLTE BERT ,  GALLAGHER BRIAN ,  VAN VELDHUIZEN JOSHUA ,  DENG HONGBO ,  ESSERS MICHAEL ,  KROTH HEIKO ,  KIELY ANDREW ,  POWERS TIMOTHY ,  TAVERAS ARTHUR G

Inventor： STEENECK CHRISTOPH ,  GEGE CHRISTIAN ,  RICHTER FRANK ,  HOCHGUERTEL MATTHIAS ,  FEURSTEIN TIM ,  BLUHM HARALD ,  SUCHOLEIKI IRVING ,  BOER JURGEN ,  WU XINYUAN ,  SCHNEIDER MATTHIAS ,  NOLTE BERT ,  GALLAGHER BRIAN ,  VAN VELDHUIZEN JOSHUA ,  DENG HONGBO ,  ESSERS MICHAEL ,  KROTH HEIKO ,  KIELY ANDREW ,  POWERS TIMOTHY ,  TAVERAS ARTHUR G

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/00

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制化合物，其表现出与目前已知的MMP-13抑制剂相关的效力增加。

公开(公告)号：WO2010075116A2

公开(公告)日：2010-07-01

申请号：PCT/US2009068130

申请日：2009-12-15

Applicant: LIFE TECHNOLOGIES CORP ,  MARTIN PHILLIP ,  OLIVARES ERIC ,  LEE BYUNG-IN ,  POWERS TIMOTHY ,  MEYER JOE

Inventor： MARTIN PHILLIP ,  OLIVARES ERIC ,  LEE BYUNG-IN ,  POWERS TIMOTHY ,  MEYER JOE

IPC: C12N15/10

CPC classification number: G01N30/6091 ,  B01D15/22 ,  B01L3/5021 ,  B01L3/50255 ,  B01L2300/0609 ,  B01L2300/0681 ,  B01L2300/0829 ,  B01L2400/0409 ,  B01L2400/049 ,  G01N21/75

Abstract: Provided herein is a clarification/binding device for the isolation of at least one target molecule from a sample. The clarification/binding device can comprise an clarification column and a binding column. The clarification column can be configured to receive the sample. Further, the clarification column can comprise a filter configured to filter at least one non-target molecule from the sample. The binding column can be configured to receive the filtered sample from the clarification column. The binding column can comprise a binding material for binding at least one target molecule. The clarification/binding device can be configured to filter the sample and bind at least one target molecule under negative pressure. Further provided herein is an apparatus for the isolation of a target molecule from a sample. The apparatus can comprise a top plate and a vacuum manifold comprising a first chamber and a second chamber. The top plate can be configured to be used with one or both of the first vacuum chamber and the second chamber of the vacuum manifold. Further provided herein are methods of use of the clarification/binding device and the vacuum apparatus and kits comprising the clarification/binding device and vacuum apparatus.

Abstract translation: 本文提供了用于从样品中分离至少一种靶分子的澄清/结合装置。 澄清/结合装置可以包括澄清柱和结合柱。 澄清栏可以配置为接收样品。 此外，澄清柱可以包括被配置成从样品中过滤至少一种非目标分子的过滤器。 绑定列可以配置为从澄清列接收过滤的样品。 结合柱可以包含用于结合至少一种靶分子的结合材料。 澄清/结合装置可以被配置为过滤样品并在负压下结合至少一个靶分子。 本文还提供了用于从样品中分离靶分子的装置。 该装置可以包括顶板和包括第一室和第二室的真空歧管。 顶板可被配置为与真空歧管的第一真空室和第二室中的一个或两个一起使用。 本文还提供了使用澄清/装订装置和真空装置的方法以及包括澄清/装订装置和真空装置的试剂盒。

公开(公告)号：WO2008083323A1

公开(公告)日：2008-07-10

申请号：PCT/US2007/089113

申请日：2007-12-28

Applicant: ROSSIO, Jeffrey ,  DEES, Robert ,  DEMBROW, Dale ,  HENRY, Brent ,  KAHATT, Espir ,  POWERS, Timothy ,  ROMAN, Steven

Inventor： ROSSIO, Jeffrey ,  DEES, Robert ,  DEMBROW, Dale ,  HENRY, Brent ,  KAHATT, Espir ,  POWERS, Timothy ,  ROMAN, Steven

IPC: G01N33/50 ,  G01N33/53

CPC classification number: G01N33/54373

Abstract: The present invention relates to, in part, methods, reagents and apparatuses for the detection of agents. The present invention also relates, in part, to compositions including, but not limited to, flow cells, assay chambers, reagent reservoir delivery units and devices for holding an assay chamber. The present invention also provides various components and combinations of components for various detection apparatuses. The present invention also relates to a portable agent detection apparatus that can be used in the field or at a point of care and is not limited to specialized laboratories or limited to use by highly skilled users.

Abstract translation: 本发明部分涉及用于检测试剂的方法，试剂和设备。 本发明还部分涉及包括但不限于流动池，测定室，试剂池输送单元和用于保持测定室的装置的组合物。 本发明还提供用于各种检测设备的各种组件和组件的组合。 本发明还涉及可用于现场或护理点的便携式药剂检测设备，并且不限于专业实验室或限于由高度熟练的用户使用。

公开(公告)号：WO2008002671A3

公开(公告)日：2008-03-27

申请号：PCT/US2007015255

申请日：2007-06-29

Applicant: ALANTOS PHARM HOLDING ,  SUCHOLEIKI IRVING ,  GEGE CHRISTIAN ,  GALLAGHER BRIAN M ,  POWERS TIMOTHY ,  DENG HONGBO ,  WU XINYUAN ,  STEENECK CHRISTOPH ,  KIELY ANDREW ,  TAVERAS ARTHUR

Inventor： SUCHOLEIKI IRVING ,  GEGE CHRISTIAN ,  GALLAGHER BRIAN M ,  POWERS TIMOTHY ,  DENG HONGBO ,  WU XINYUAN ,  STEENECK CHRISTOPH ,  KIELY ANDREW ,  TAVERAS ARTHUR

IPC: C07D239/38 ,  A61K31/505 ,  A61K31/506 ,  A61K31/538 ,  A61P19/00 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D403/12 ,  C07D239/38 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14

Abstract: The present invention relates to amide containing aromatic MMP inhibiting compounds with a mono-amide heteroaromatic group, of formulas I and II: (I) (II).

Abstract translation: 本发明涉及具有式I和II的单酰胺杂芳族基团的含芳族MMP抑制化合物的酰胺：（I）（II）。

公开(公告)号：WO2006128184A2

公开(公告)日：2006-11-30

申请号：PCT/US2006/020970

申请日：2006-05-22

Applicant: ALANTOS-PHARMACEUTICALS, INC. ,  STEENECK, Christoph ,  GEGE, Christian ,  RICHTER, Frank ,  HOCHGUERTEL, Matthias ,  FEURSTEIN, Tim ,  BLUHM, Harald ,  SUCHOLEIKI, Irving ,  BOER, Jurgen ,  WU, Xinyuan ,  SCHNEIDER, Matthias ,  NOLTE, Bert ,  GALLAGHER, Brian ,  VAN VELDHUIZEN, Joshua ,  DENG, Hongbo ,  ESSERS, Michael ,  KROTH, Heiko ,  KIELY, Andrew ,  POWERS, Timothy ,  TAVERAS, Arthur, G.

Inventor： STEENECK, Christoph ,  GEGE, Christian ,  RICHTER, Frank ,  HOCHGUERTEL, Matthias ,  FEURSTEIN, Tim ,  BLUHM, Harald ,  SUCHOLEIKI, Irving ,  BOER, Jurgen ,  WU, Xinyuan ,  SCHNEIDER, Matthias ,  NOLTE, Bert ,  GALLAGHER, Brian ,  VAN VELDHUIZEN, Joshua ,  DENG, Hongbo ,  ESSERS, Michael ,  KROTH, Heiko ,  KIELY, Andrew ,  POWERS, Timothy ,  TAVERAS, Arthur, G.

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/00

CPC classification number: C07D487/04

Abstract: The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.

Abstract translation: 本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。 更具体地，本发明提供了一类新型的杂双环MMP-13抑制化合物，其表现出与目前已知的MMP-13抑制剂相关的效力增加。

公开(公告)号：WO2011063233A1

公开(公告)日：2011-05-26

申请号：PCT/US2010/057428

申请日：2010-11-19

Applicant: AMGEN INC. ,  CHENG, Yuan ,  POWERS, Timothy ,  ASHTON, Kate ,  BROWN, James ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  JUDD, Ted ,  LOPEZ, Patricia ,  NIXEY, Thomas ,  PARAS, Nick A, ,  POON, Steve F. ,  ST. JEAN JR., David J. ,  XUE, Qiufen ,  ZHONG, Wenge

Inventor： CHENG, Yuan ,  POWERS, Timothy ,  ASHTON, Kate ,  BROWN, James ,  HARRIED, Scott ,  HITCHCOCK, Stephen ,  JUDD, Ted ,  LOPEZ, Patricia ,  NIXEY, Thomas ,  PARAS, Nick A, ,  POON, Steve F. ,  ST. JEAN JR., David J. ,  XUE, Qiufen ,  ZHONG, Wenge

IPC: C07D215/38 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D417/04 ,  A61K31/4709 ,  A61P25/28

CPC classification number: C07D215/38 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/12 ,  C07D417/04

Abstract: 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 ring A, B 1 , B 2 , B 3 , L, R 1 , R 4 , R 5 and m of Formula I 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, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 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，其中式I的环A，B 1，B 2，B 3，L，R 1，R 4，R 5和m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疾病和病症的用途。 这些疾病包括例如阿尔茨海默氏病（AD），认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

公开(公告)号：WO2017040341A1

公开(公告)日：2017-03-09

申请号：PCT/US2016/049124

申请日：2016-08-26

Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING ,  DELOS PHARMACEUTICALS INC. ,  GREGORY, Matthew Alan ,  MOSS, Steven ,  VELARDE, Michael ,  POWERS, Timothy ,  TZANNIS, Stelios

Inventor： GREGORY, Matthew Alan ,  MOSS, Steven ,  VELARDE, Michael ,  POWERS, Timothy ,  TZANNIS, Stelios

IPC: C07D498/18 ,  A61K31/436 ,  A61K45/06

CPC classification number: A61K31/436 ,  A61K38/13 ,  A61K45/06 ,  C07D498/18 ,  A61K2300/00

Abstract: In various embodiments novel rapamycin analogs are provides that show improved mTORC1 specificity.

Abstract translation: 在各种实施方案中，提供了表现出改善的mTORC1特异性的新型雷帕霉素类似物。