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1. 发明公开

EP2391623A1 INHIBITORS OF AKT ACTIVITY 审中-公开
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
申请人： Merck Sharp & Dohme Corp. , MSD K.K.
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.

2. 发明授权

EP2299825B1 INHIBITORS OF AKT ACTIVITY 有权
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
申请人： Merck Sharp & Dohme Corp. , MSD K.K.
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

3. 发明授权

EP2303269B1 INHIBITORS OF AKT ACTIVITY 有权
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
申请人： Merck Sharp & Dohme Corp. , MSD K.K.
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
IPC分类号： A61K31/44 , A61K31/52
CPC分类号： C07D471/14

4. 发明申请

WO2010088177A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2010088177A1
公开(公告)日：2010-08-05
申请号：PCT/US2010/021945
申请日：2010-01-25
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , 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.
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.
摘要翻译：本发明提供抑制Akt活性的化合物。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这种抑制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活性的方法。

5. 发明申请

WO2010042337A1 NOVEL 6-AZAINDOLE AMINOPYRIMIDINE DERIVATIVES HAVING NIK INHIBITORY ACTIVITY 审中-公开
标题翻译：具有NIK抑制活性的新型6-氨基亚氨基嘧啶衍生物
公开(公告)号：WO2010042337A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/058561
申请日：2009-09-28
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , GOTO, Yasuhiro , SAGARA, Takeshi , FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , MALASKA, Michael, J. , MOORE, Joseph, A., III , OUVRY, Gilles , PANDI, Bharathi , PEEL, Michael, R. , STEWARD, Kimberly, M.
发明人： GOTO, Yasuhiro , SAGARA, Takeshi , FAN, Weiming , HAXELL, Thomas, F. N. , JENKS, Matthew, G. , MALASKA, Michael, J. , MOORE, Joseph, A., III , OUVRY, Gilles , PANDI, Bharathi , PEEL, Michael, R. , STEWARD, Kimberly, M.
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D471/04
摘要： The present invention relates to a compound of formula I: wherein: R 1 is C 1-6 alkyl, C 3-8 cycloalkyl, aryl, heterocyclyl, or -COR 1x , where the C 1-6 alkyl, C 3-8 cycloalkyl, aryl, and heterocyclyl may be substituted; and R 1x is C 3-8 cycloalkyl, aryl, or heterocyclyl, any of which may be substituted; R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are each independently hydrogen, halogen, C 1-6 alkyl, or aryl, where the C 1-6 alkyl or aryl may be substituted; R 8 is hydrogen, C 1-6 alkyl, aryl, or heterocyclyl, any of which may be substituted; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式I化合物：其中：R 1是C 1-6烷基，C 3-8环烷基，芳基，杂环基或-COR 1 x，其中C 1-6烷基，C 3-8环烷基，芳基和杂环基可以被替代并且R 1 x是C 3-8环烷基，芳基或杂环基，其中任何一个可以被取代; R 2，R 3，R 4，R 5，R 6和R 7各自独立地为氢，卤素，C 1-6烷基或芳基，其中C 1-6烷基或芳基可以被取代; R 8是氢，C 1-6烷基，芳基或杂环基，其中任何一个可以被取代; 或其药学上可接受的盐或酯。

6. 发明公开

EP2299825A1 INHIBITORS OF AKT ACTIVITY 有权
标题翻译： AKT活性抑制剂
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
申请人： Merck Sharp & Dohme Corp. , Banyu Pharmaceutical Co., Ltd.
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。

7. 发明公开

EP2303269A1 INHIBITORS OF AKT ACTIVITY 有权
标题翻译： AKT活性抑制剂
公开(公告)号：EP2303269A1
公开(公告)日：2011-04-06
申请号：EP09759077.2
申请日：2009-05-28
申请人： Merck Sharp & Dohme Corp. , Banyu Pharmaceutical Co., Ltd.
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
IPC分类号： A61K31/44 , A61K31/52
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted 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，尤其是Akt1的方法。

8. 发明公开

EP2401281A1 PYRIMIDOPYRIMIDOINDAZOLE DERIVATIVE 审中-公开
标题翻译：嘧啶并嘧啶并吲唑衍生物
公开(公告)号：EP2401281A1
公开(公告)日：2012-01-04
申请号：EP10746246.7
申请日：2010-02-18
申请人： MSD K.K.
发明人： GOTO, Yasuhiro , NIIYAMA, Kenji , SUNAMI, Satoshi , TAKAHASHI, Keiji
IPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/551 , A61P35/00 , A61P43/00 , C07D519/00
CPC分类号： C07D487/14 , C07D519/00
摘要： The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R
1 means a -(C=O)
a O
b (C1-C6)alkyl group, a -(C=O)
a O
b (C2-C6)alkenyl group, a -(C=O)
a O
b (C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R
2 and R
3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a -(C=O)
a O
b (C1-C6)alkyl group or a group of -(C=O)
a N(R
1e )R
2e ; R
4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
摘要翻译：本发明提供了一种用于癌症化疗或放疗的新型抗癌剂或敏化剂。通式（I）的化合物：其中A是指芳基或杂芳基，或式（a）的基团：（C = O）aO b（C 1 -C 6）烷基， - （C = O）aO b（C 2 -C 6）链烯基， - （C = O）aO b ）环烷基，芳基或杂芳基; R 2和R 3各自表示氢原子，卤素原子，羟基，羧基， - （C = O）aO b（C 1 -C 6）烷基或 - （C = O）a N （R 1e）R 2e; R 4表示氢原子或（C 1 -C 6）烷基等具有优异的Wee1激酶抑制作用，因此可用于医学领域，特别是在各种癌症治疗领域。

9. 发明授权

EP2017278B1 DIHYDROPYRAZOLOPYRIMIDINONE DERIVATIVE 有权转让
标题翻译：二氢吡唑并嘧啶酮衍生物
公开(公告)号：EP2017278B1
公开(公告)日：2016-11-02
申请号：EP07742851.4
申请日：2007-04-25
申请人： MSD K.K.
发明人： SAKAMOTO, Toshihiro , SUNAMI, Satoshi , YAMAMOTO, Fuyuki , NIIYAMA, Kenji , BAMBA, Makoto , TAKAHASHI, Keiji , FURUYAMA, Hidetomo , GOTO, Yasuhiro , SAGARA, Takeshi , OTSUKI, Sachie , NISHIBATA, Toshihide , YOSHIZUMI, Takashi , HIRAI, Hiroshi
IPC分类号： C07D471/04 , A61K31/519 , A61K31/5377 , A61K31/54 , A61K31/551 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/519

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