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公开(公告)号：EP2299825A1
公开(公告)日：2011-03-30
申请号：EP09759048.3
申请日：2009-05-27
发明人： FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , OGINO, Yoshio , ONOZAKI, Yu , ROSSI, Michael, A. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A01N43/90
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了抑制Akt活性的取代的[1,2,4]三唑并[4,3-a] -1,5-萘啶化合物。 具体而言，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。 本发明还提供了包含这种抑制性化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，特别是Akt1的方法。
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公开(公告)号：EP2770995B1
公开(公告)日：2019-01-02
申请号：EP12843015.4
申请日：2012-10-26
发明人： LAYTON, Mark, E. , PERO, Joseph, E. , FIJI, Hannah , KELLY, Michael, J., III , DE LEON, Pablo , ROSSI, Michael, A. , GILBERT, Kevin, F. , ROECKER, Anthony, J. , ZHAO, Zhijian , MERCER, Swati Pal , WOLKENBERG, Scott , MULHEARN, James , ZHAO, Lianyun , LI, Dansu
IPC分类号： C07D417/14 , C07D417/12 , C07D451/02 , C07D471/04 , C07D493/10 , C07D491/107 , A61K31/423 , A61P29/00 , A61K31/433 , A61K31/427 , A61K31/55 , A61K31/437 , A61K31/4725 , A61K31/4709
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公开(公告)号：EP2391623A1
公开(公告)日：2011-12-07
申请号：EP10736277.4
申请日：2010-01-25
发明人： ARMSTRONG, Donna, J. , GOTO, Yasuhiro , HASHIHAYATA, Takashi , KATO, Tetsuya , KELLY, Michael, J., III , LAYTON, Mark, E. , LINDSLEY, Craig, W. , OGINO, Yoshio , ONOZAKI, Yu , RODZINAK, Kevin, J. , ROSSI, Michael, A. , SANDERSON, Philip, E. , WANG, Jiabing , YAROSCHAK, Melissa, M.
IPC分类号： C07D471/02
CPC分类号： C07D471/04 , C07D217/24 , C07D241/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D519/00
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
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4.发明公开N-SUBSTITUTED INDAZOLE SULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 审中-公开N-取代INDAZOLSULFONAMIDVERBINDUNGEN选择性活动压控钠通道
公开(公告)号：EP2911663A1
公开(公告)日：2015-09-02
申请号：EP13849733.4
申请日：2013-10-23
发明人： PERO, Joseph, E. , LEHMAN, Hannah, D. G. F. , LAYTON, Mark, E. , ROSSI, Michael, A. , KELLY, Michael, J., III
IPC分类号： A61K31/416
CPC分类号： C07D471/08 , C07D231/56 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14
摘要： Disclosed are compounds of Formula A
A and Formula A
B : wherein "Heteroaryl-1", R
A1 , R
A2 , R
B1 , and R
C are defined herein, which novel compounds have properties for blocking Na
v 1.7 ion channels found in peripherial and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae A
A and A
B or their salts, and methods of treating neuropathic pain disorders using the same.-
公开(公告)号：EP2721029A1
公开(公告)日：2014-04-23
申请号：EP12801127.7
申请日：2012-06-14
发明人： FIJI, Hannah, D. , KELLY, Michael, J., III , KERN, Jeffrey, C. , LAYTON, Mark, E. , PERO, Joseph, E. , REIF, Alexander, J. , ROSSI, Michael, A.
IPC分类号： C07D471/04
CPC分类号： C07D513/04 , C07D471/04 , C07D519/00
摘要： The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
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公开(公告)号：EP1898903B1
公开(公告)日：2013-03-27
申请号：EP06772406.2
申请日：2006-06-07
发明人： ARMSTRONG, Donna, J. , HU, Essa, H. , KELLY, Michael, J. III , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , ROSSI, Michael, A. , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D471/14 , C07D487/14
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7.发明公开BENZOXAZOLINONE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 审中-公开选择性活动压控钠通道BENZOXAZOLINONVERBINDUNGEN
公开(公告)号：EP2911668A1
公开(公告)日：2015-09-02
申请号：EP13849421.6
申请日：2013-10-23
发明人： PERO, Joseph, E. , LEHMAN, Hannah, D. G. F. , KELLY, Michael, J., III , ZHAO, Lianyun , ROSSI, Michael, A. , LI, Dansu , GILBERT, Kevin, F. , WOLKENBERG, Scott , MULHEARN, James , LAYTON, Mark, E. , DE LEON, Pablo
IPC分类号： A61K31/423 , C07D263/54
CPC分类号： C07D413/14 , A61K31/44 , C07D263/58 , C07D413/12
摘要： Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.
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公开(公告)号：EP1898903B8
公开(公告)日：2013-05-15
申请号：EP06772406.2
申请日：2006-06-07
发明人： ARMSTRONG, Donna, J. , HU, Essa, H. , KELLY, Michael, J. III , LAYTON, Mark, E. , LI, Yiwei , LIANG, Jun , RODZINAK, Kevin, J. , ROSSI, Michael, A. , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A61K31/41 , C07D249/00
CPC分类号： C07D471/14 , C07D487/14
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公开(公告)号：EP2911663B1
公开(公告)日：2020-03-18
申请号：EP13849733.4
申请日：2013-10-23
发明人： PERO, Joseph, E. , LEHMAN, Hannah, D. G. F. , LAYTON, Mark, E. , ROSSI, Michael, A. , KELLY, Michael, J., III
IPC分类号： A61K31/416
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公开(公告)号：EP2721029B1
公开(公告)日：2018-07-18
申请号：EP12801127.7
申请日：2012-06-14
发明人： FIJI, Hannah, D. , KELLY, Michael, J., III , KERN, Jeffrey, C. , LAYTON, Mark, E. , PERO, Joseph, E. , REIF, Alexander, J. , ROSSI, Michael, A.
IPC分类号： C07D471/04 , C07D513/04 , C07D519/00
CPC分类号： C07D513/04 , C07D471/04 , C07D519/00
摘要： The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
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