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1. 发明申请

WO2011133733A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活性抑制剂
公开(公告)号：WO2011133733A1
公开(公告)日：2011-10-27
申请号：PCT/US2011/033363
申请日：2011-04-21
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Yuguang , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
发明人： LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Yuguang , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
IPC分类号： A61K31/425 , A61K31/135
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14 , C07D487/08
摘要： The instant invention provides for substituted thiazoles 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活性的取代噻唑。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活性的方法。

2. 发明申请

WO2011130921A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2011130921A1
公开(公告)日：2011-10-27
申请号：PCT/CN2010/072132
申请日：2010-04-23
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
发明人： LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
IPC分类号： C07D417/04 , C07D277/20 , A61K31/426 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , C07D277/28 , C07D277/30 , C07D277/42 , C07D277/52 , C07D277/56 , C07D417/04 , C07D417/14
摘要： The instant invention provides for substituted thiazoles 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活性的取代的噻唑。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。

3. 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。

4. 发明申请

WO2009148916A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2009148916A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/045456
申请日：2009-05-28
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , 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
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：本发明提供抑制Akt活性的取代的萘啶化合物。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，优选Akt1。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，尤其是Akt1的方法。

5. 发明申请

WO2008070016A2 INHIBITORS OF AKT ACTIVITY 审中-公开
公开(公告)号：WO2008070016A2
公开(公告)日：2008-06-12
申请号：PCT/US2007/024722
申请日：2007-12-03
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
发明人： KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , 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. 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.

6. 发明申请

WO2009148887A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2009148887A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/045213
申请日：2009-05-27
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , 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
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] -1,5-二氮杂萘化合物。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，优选Akt1。本发明还提供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，特别是Akt1。

7. 发明申请

WO2010114780A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2010114780A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/028989
申请日：2010-03-29
申请人： MERCK SHARP & DOHME CORP. , CHEN, Qi , CUI, Mingziang , HU, Bin , HU, Shuangxi , PU, Zhifa , SANDERSON, Philip, E. , SOLL, Richard , TANG, Xue , WANG, Jiabing , YAN, Yongjin , YAO, Jinfeng , ZHANG, Hongjie
发明人： CHEN, Qi , CUI, Mingziang , HU, Bin , HU, Shuangxi , PU, Zhifa , SANDERSON, Philip, E. , SOLL, Richard , TANG, Xue , WANG, Jiabing , YAN, Yongjin , YAO, Jinfeng , ZHANG, Hongjie
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , C07D487/04
摘要： The instant invention provides for substituted fused pyrimidine 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活性的取代的稠合嘧啶化合物。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。

8. 发明申请

WO2011106276A1 TASK CHANNEL ANTAGONISTS 审中-公开
标题翻译：任务通道ANTAGONISTS
公开(公告)号：WO2011106276A1
公开(公告)日：2011-09-01
申请号：PCT/US2011/025596
申请日：2011-02-21
申请人： MERCK SHARP & DOHME CORP. , COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M.
发明人： COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M.
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： C07D471/04 , C07D471/18
摘要： This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders which have TASK-1 and/or TASK-3-related damage as a secondary cause.
摘要翻译：本发明涉及用于治疗和预防由活化或由活化的TASK-1引起的疾病的TASK-1和/或TASK-3拮抗剂和/或其药学上可接受的盐，组合物和方法和/或TASK-3，以及具有TASK-1和/或TASK-3相关损伤作为次要原因的疾病。

9. 发明申请

WO2011103715A1 TASK CHANNEL ANTAGONISTS 审中-公开
标题翻译：任务通道ANTAGONISTS
公开(公告)号：WO2011103715A1
公开(公告)日：2011-09-01
申请号：PCT/CN2010/070751
申请日：2010-02-25
申请人： MERCK SHARP & DOHME CORP. , COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M
发明人： COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M
IPC分类号： C07D471/04 , C07D471/18 , A61K31/519 , A61K31/529 , A61P11/00 , A61P25/08 , A61P25/20 , A61P25/24
CPC分类号： C07D471/04 , A61K31/519 , A61K31/529 , A61K45/06 , C07D471/18 , A61K2300/00
摘要： This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders which have TASK-1 and/or TASK-3-related damage as a secondary cause.
摘要翻译：本发明涉及TASK-1和/或TASK-3拮抗剂和/或其药学上可接受的盐，组合物和方法，用于治疗和预防由激活或活化的TASK-1和/或TASK-3引起的疾病，和具有TASK-1和/或TASK-3相关损伤的疾病作为次要原因。

10. 发明申请

WO2003026568A3 ANDROSTANES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003026568A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/029436
申请日：2002-09-17
申请人： MERCK & CO., INC. , WANG, Jiabing
发明人： WANG, Jiabing
IPC分类号： A61K31/56
摘要： Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating a function of the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteopenia, osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, inflammatory arthritis and joint repair, alone or in combination with other active agents.

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