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公开(公告)号：EP2299825B1
公开(公告)日：2013-07-31
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
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2.发明授权AMINOPYRIMIDINE DERIVATIVES HAVING AURORA-A-SELECTIVE INHIBITORY ACTIVITY 有权WITH AURORA选择性抑制效果氨基嘧啶衍生物
公开(公告)号：EP2017279B1
公开(公告)日：2013-09-04
申请号：EP07742848.0
申请日：2007-04-25
申请人： MSD K.K.
发明人： KATO, Tetsuya , KAWANISHI, Nobuhiko , MITA, Takashi , NAGAI, Keita , NONOSHITA, Katsumasa , OHKUBO, Mitsuru
IPC分类号： C07D487/08 , A61K31/497 , A61K31/4995 , A61K31/506 , A61K45/08 , A61P35/00 , A61P43/00
CPC分类号： C07D487/08
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公开(公告)号：EP2406250A1
公开(公告)日：2012-01-18
申请号：EP10751342.6
申请日：2010-03-10
发明人： FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , KAWANISHI, Nobuhiko , LEE, Shuliang , LIU, Hao , MALASKA, Michael, J. , MOORE, Joseph, A., III , OGINO, Yoshio , ONOZAKI, Yu , PANDI, Bharathi , PEEL, Michael, R. , SAKAMOTO, Toshihiro , SIU, Tony
IPC分类号： C07D403/00 , C07D413/00
CPC分类号： C07D471/14 , C07D487/14 , C07D519/00
摘要： The instant invention provides for substituted fused naphthyridine derivatives 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.
摘要翻译： 本发明提供了抑制Akt活性的取代的稠合萘啶衍生物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含此类抑制性化合物的组合物以及通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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4.发明授权NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权选择性AURORA-A-NEW抑制氨基吡啶衍生物
公开(公告)号：EP2411010B1
公开(公告)日：2013-11-06
申请号：EP10756579.8
申请日：2010-03-12
发明人： BINCH, Hayley , HASHIMOTO, Masaya , IWAMA, Toshiharu , KAWANISHI, Nobuhiko , MORTIMORE, Michael , OHKUBO, Mitsuru , SUNAMI, Tomoko
IPC分类号： A61K31/535 , C07D401/04 , C07D403/14 , A61P35/00
CPC分类号： C07D403/14
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5.发明公开NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 审中-公开具有选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：EP2411012A1
公开(公告)日：2012-02-01
申请号：EP10756585.5
申请日：2010-03-15
IPC分类号： A61K31/535 , C07D401/04
CPC分类号： C07D471/04 , C07D498/04
摘要： The present invention relates to a compound of Formula (I): wherein: n is 0 or 1; X is O or CH
2 ; R
1 is H or C
1-2 alkyl; R
2 is H or C
1-3 alkyl; R
3 and R
4 are each independently H or C
1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R
10 R
5 is H or OCH
3 ; R
10 is F or Cl; or a pharmaceutically acceptable salt or ester thereof.摘要翻译： 本发明涉及式（I）的化合物：其中：n是0或1; X是O或CH 2; R 1是H或C 1-2烷基; R 2是H或C 1-3烷基; R 3和R 4各自独立地为H或C 1-2烷基，其中所述烷基可被1-3个选自R 10 R 5为H或OCH 3的相同或不同取代基取代; R 10是F或Cl; 或其药学上可接受的盐或酯。
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6.发明公开NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权选择性AURORA-A-NEW抑制氨基吡啶衍生物
公开(公告)号：EP2411010A1
公开(公告)日：2012-02-01
申请号：EP10756579.8
申请日：2010-03-12
发明人： BINCH, Hayley , HASHIMOTO, Masaya , IWAMA, Toshiharu , KAWANISHI, Nobuhiko , MORTIMORE, Michael , OHKUBO, Mitsuru , SUNAMI, Tomoko
IPC分类号： A61K31/535 , C07D401/04
CPC分类号： C07D403/14
摘要： The present invention relates to a compound of Formula (I): wherein: R
1 is H or C
1-2 alkyl; R
2 is H or C
1-3 alkyl; R
3 and R
4 are each independently H or C
1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R
10 ; R
5 is H, hydroxy, C
1-2 alkyl, or OCH
3 ; and R
10 is F or Cl, or a pharmaceutically acceptable salt or ester thereof.-
公开(公告)号：EP2406250B1
公开(公告)日：2015-08-12
申请号：EP10751342.6
申请日：2010-03-10
发明人： FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , KAWANISHI, Nobuhiko , LEE, Shuliang , LIU, Hao , MALASKA, Michael, J. , MOORE, Joseph, A., III , OGINO, Yoshio , ONOZAKI, Yu , PANDI, Bharathi , PEEL, Michael, R. , SAKAMOTO, Toshihiro , SIU, Tony
IPC分类号： C07D403/00 , C07D413/00 , C07D471/14 , C07D487/14 , A61K31/4375 , A61K35/00
CPC分类号： C07D471/14 , C07D487/14 , C07D519/00
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8.发明授权NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 有权与选择性AURORA-A-抗炎作用NEW氨基吡啶衍生物
公开(公告)号：EP2254888B1
公开(公告)日：2014-12-24
申请号：EP09711943.2
申请日：2009-02-18
申请人： MSD K.K.
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4545 , A61K31/506 , A61P35/00 , A61P41/00
CPC分类号： C07D417/14 , C07D401/14 , C07D413/14
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公开(公告)号：EP2303269B1
公开(公告)日：2014-07-30
申请号：EP09759077.2
申请日：2009-05-28
发明人： FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , NAYA, Akira , OGINO, Yoshio , ONOZAKI, Yu , RODZINAK, Kevin, J. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
CPC分类号： C07D471/14
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10.发明授权
公开(公告)号：EP2062887B1
公开(公告)日：2012-07-04
申请号：EP07806706.3
申请日：2007-08-29
申请人： MSD K.K.
发明人： IWASAWA, Yoshikazu , KATO, Tetsuya , KAWANISHI, Nobuhiko , MASUTANI, Kouta , MITA, Takashi , NONOSHITA, Katsumasa , OHKUBO, Mitsuru
IPC分类号： C07D401/12 , C07D403/12 , C07D417/12 , A61K31/4439 , A61K31/497 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00
CPC分类号： C07D413/14 , A61K45/06 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Disclosed is a compound represented by the general formula [I] below or a pharmaceutically acceptable salt or ester thereof. (I) (In the formula, R1 represents a hydrogen atom, F, CN or the like; R1' represents a hydrogen atom or an optionally substituted lower alkyl group; R2 represents O, S, SO, SO2 or the like;R3 represents an optionally substituted phenyl group; X1, X2 and X3 independently represent CH, N or the like, provided that none or one of X1, X2 and X3 is N; and W represents a group represented by the following formula: , wherein W1, W2 and W3 independently represent CH, N or the like.)
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