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

Applicant: 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.

Inventor： 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: C07D471/02

CPC classification number: C07D471/04 ,  C07D217/24 ,  C07D241/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D475/02 ,  C07D475/04 ,  C07D487/04 ,  C07D519/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2006135627A3

公开(公告)日：2008-07-31

申请号：PCT/US2006022079

申请日：2006-06-07

Applicant: MERCK & CO INC ,  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

Inventor： 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: A61K31/41 ,  C07D249/00

CPC classification number: C07D471/14 ,  C07D487/14

Abstract: 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.

Abstract translation: 本发明提供了抑制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。 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。

公开(公告)号：WO2006017409A2

公开(公告)日：2006-02-16

申请号：PCT/US2005/027160

申请日：2005-07-29

Applicant: MERCK & CO., INC. ,  LAYTON, Mark, E. ,  RODZINAK, Kevin, J. ,  KELLY, Michael, J., III ,  SANDERSON, Philip, E.

Inventor： LAYTON, Mark, E. ,  RODZINAK, Kevin, J. ,  KELLY, Michael, J., III ,  SANDERSON, Philip, E.

IPC: A61K31/519 ,  C07D487/02

CPC classification number: C07D487/04

Abstract: Compounds represented by Formula I: (wherein A, B, D, P, Q, R 1 , R 2 , R 3 , W and Y are described herein) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain, Parkinson’s disease, Alzheimer’s disease, epilepsy, depression, anxiety, ischemic brain injury including stroke, and other conditions.

Abstract translation: 由式I表示的化合物：（其中A，B，D，P，Q，R

公开(公告)号：WO2004032834A3

公开(公告)日：2004-06-10

申请号：PCT/US0330867

申请日：2003-09-30

Applicant: MERCK & CO INC ,  STAAS DONNETTE D ,  LYLE TERRY A ,  WILLIAMS PETER D ,  SANDERSON PHILIP E J

Inventor： STAAS DONNETTE D ,  LYLE TERRY A ,  WILLIAMS PETER D ,  SANDERSON PHILIP E J

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D417/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12

Abstract: Compounds of the invention (Formula I) are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: I.The compounds are useful for preventing or treating unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels, in a mammal.

Abstract translation: 本发明的化合物（式I）可用于抑制具有以下结构的凝血酶和相关的血栓形成闭塞：I，该化合物可用于预防或治疗不稳定心绞痛，难治性心绞痛，心肌梗塞，短暂性脑缺血发作，心房纤颤，血栓形成中风 ，栓塞性中风，深静脉血栓形成，播散性血管内凝血，纤维蛋白的眼部积聚以及再通血管的再闭塞或再狭窄。

公开(公告)号：WO2002064559A3

公开(公告)日：2002-08-22

申请号：PCT/US2002/004658

申请日：2002-02-05

Applicant: MERCK & CO., INC. ,  SELNICK, Harold, G. ,  YOUNG, Mary Beth ,  NANTERMET, Philippe, G. ,  BARROW, James, C. ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  STAAS, Donnette, D. ,  STAUFFER, Kenneth, J. ,  SANDERSON, Philip, E.

Inventor： SELNICK, Harold, G. ,  YOUNG, Mary Beth ,  NANTERMET, Philippe, G. ,  BARROW, James, C. ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  STAAS, Donnette, D. ,  STAUFFER, Kenneth, J. ,  SANDERSON, Philip, E.

IPC: C07D403/12 ,  A61K31/41

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)-N(R 25 )CH(R 30 )- wherein the nitrogen atom is attached to R 1 , and R 25 and R 30 are independently selected from the group consisting of hydrogen, C 3-6 cycloalkyl, and C 1-6 alkyl, or 2) wherein the nitrogen atom is attached to R 1 , and m is 0, 1, or 2.

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

Applicant: 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

Inventor： 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: A61K31/44 ,  A61K31/52

CPC classification number: C07D471/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2008070041A3

公开(公告)日：2008-08-28

申请号：PCT/US2007024772

申请日：2007-12-03

Applicant: MERCK & CO INC ,  KELLY MICHAEL J III ,  LAYTON MARK E ,  SANDERSON PHILIP E

Inventor： KELLY MICHAEL J III ,  LAYTON MARK E ,  SANDERSON PHILIP E

IPC: C07D401/04 ,  A61K31/4353 ,  A61P35/00 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D407/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

CPC classification number: C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D407/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/14

Abstract: 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.

公开(公告)号：WO2006113471A3

公开(公告)日：2006-10-26

申请号：PCT/US2006/014139

申请日：2006-04-14

Applicant: MERCK & CO., INC. ,  LAYTON, Mark, E. ,  RODZINAK, Kevin, J. ,  KELLY, Michael, J. III ,  SANDERSON, Philip, E.

Inventor： LAYTON, Mark, E. ,  RODZINAK, Kevin, J. ,  KELLY, Michael, J. III ,  SANDERSON, Philip, E.

IPC: A61K31/55

Abstract: Compounds represented by Formula (I): and/or pharmaceutically acceptable salts, individual enantiomers and stereoisomers thereof, are effective as NMDA/NR2B antagonists useful for treating conditions such as pain, Parkinson’s disease, Alzheimer’s disease, epilepsy, depression, anxiety, ischemic brain injury including stroke.

公开(公告)号：WO2006091395A3

公开(公告)日：2006-08-31

申请号：PCT/US2006/004715

申请日：2006-02-10

Applicant: MERCK & CO., INC. ,  COSFORD, Nicholas, D., P. ,  LAYTON, Mark, E. ,  LIANG, Jun ,  LINDSLEY, Craig, W. ,  SANDERSON, Philip, E. ,  ZHAO, Zhijian

Inventor： COSFORD, Nicholas, D., P. ,  LAYTON, Mark, E. ,  LIANG, Jun ,  LINDSLEY, Craig, W. ,  SANDERSON, Philip, E. ,  ZHAO, Zhijian

IPC: A61K31/395

Abstract: 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.

公开(公告)号：WO1997040024A1

公开(公告)日：1997-10-30

申请号：PCT/US1997006744

申请日：1997-04-18

Applicant: MERCK & CO., INC. ,  SANDERSON, Philip, E. ,  LYLE, Terry, A. ,  DORSEY, Bruce, D. ,  VARSOLONA, Richard, J.

Inventor： MERCK & CO., INC.

IPC: C07D241/20

CPC classification number: C07D401/12 ,  C07D241/20 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having structure (a), for example (b).

Abstract translation: 本发明的化合物可用于抑制具有结构（a）的凝血酶和相关的血栓形成闭塞，例如（b）。