公开(公告)号：EP3781687A1

公开(公告)日：2021-02-24

申请号：EP19789285.4

申请日：2019-04-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： CHANG, Wonsuk ,  PARISH, Craig, A. ,  SIU, Tony ,  TRUONG, Quang, T. ,  WANG, Hongwu ,  WASSERMANN, Anne Mai

IPC: C12N15/113 ,  C12N15/117

公开(公告)号：EP2513098B1

公开(公告)日：2016-11-09

申请号：EP10801736.9

申请日：2010-12-15

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： ALTMANN, Michael D. ,  ANDRESEN, Brian M. ,  ARRINGTON, Kenneth L. ,  CHILDERS, Kaleen Konrad ,  DI FRANCESCO, Maria Emilia ,  DONOFRIO, Anthony ,  ELLIS, John Michael ,  FISCHER, Christian ,  GUERIN, David Joseph ,  HAIDLE, Andrew M. ,  KATTAR, Solomon ,  KNOWLES, Sandra Lee ,  LI, Chaomin ,  LIM, Jongwon ,  MACHACEK, Michelle ,  NORTHRUP, Alan B. ,  O'BOYLE, Brendan M. ,  OTTE, Ryan D. ,  PETROCCHI, Alessia ,  REUTERSHAN, Michael H. ,  ROMEO, Eric ,  SIU, Tony ,  TAOKA, Brandon M. ,  TROTTER, B. Wesley ,  ZHOU, Hua ,  BURCH, Jason ,  COTE, Bernard ,  DUPONT-GAUDET, Kristina ,  FOURNIER, Jean-Francois ,  GAUTHIER, Jacques Yves ,  GUAY, Daniel ,  ROBICHAUD, Joel S. ,  GRIMM, Jonathan ,  MADDESS, Matthew L. ,  SCHELL, Adam J. ,  SPENCER, Kerrie B. ,  WOO, Hyun Chong ,  BHAT, Sathesh

IPC: C07D417/12 ,  C07D417/14 ,  A61K31/497 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D417/12 ,  C07D417/14 ,  C07D451/06 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/08 ,  C07D495/04 ,  C07F9/65583

公开(公告)号：EP2490693A1

公开(公告)日：2012-08-29

申请号：EP10825388.1

申请日：2010-09-29

Applicant: Merck Sharp & Dohme Corp.

Inventor： SIU, Tony ,  DINSMORE, Christopher ,  KUMARASINGHE, Sathyajith, E.

IPC: A61K31/542 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.

公开(公告)号：EP2299816A1

公开(公告)日：2011-03-30

申请号：EP09767466.7

申请日：2009-06-08

Applicant: Merck Sharp & Dohme Corp.

Inventor： MACHACEK, Michelle ,  DE ALMEIDA, Gabriela ,  GRIMM, Jonathan, B. ,  MACCOSS, Rachel, N. ,  ROMEO, Eric ,  SIU, Tony ,  WHITE, Catherine ,  WILSON, Kevin

IPC: A01N43/06 ,  A61K31/38

CPC classification number: C07D513/04 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

Abstract translation: 本发明提供了抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 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骨髓增生性疾病或癌症的患者来抑制JAK1，JAK2，JAK3，TYK2和PDK1活性的方法。

公开(公告)号：EP3523287A1

公开(公告)日：2019-08-14

申请号：EP17784507.0

申请日：2017-10-02

Applicant: Merck Sharp & Dohme Corp.

Inventor： ALTMAN, Michael, D. ,  CASH, Brandon, D. ,  CHANG, Wonsuk ,  CUMMING, Jared, N. ,  HAIDLE, Andrew, M. ,  HENDERSON, Timothy, J. ,  JEWELL, James, P. ,  LARSEN, Matthew, A. ,  LIANG, Rui ,  LIM, Jongwon ,  LU, Min ,  OTTE, Ryan, D. ,  SIU, Tony ,  TROTTER, Benjamin Wesley ,  TYAGARAJAN, Sriram

IPC: C07D333/60 ,  C07D409/12 ,  C07D498/04 ,  A61K31/381 ,  A61K31/385 ,  A61K31/424 ,  A61P35/00

公开(公告)号：EP2758377B1

公开(公告)日：2017-08-02

申请号：EP12833410.9

申请日：2012-09-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： BRUBAKER, Jason ,  DINSMORE, Christopher J. ,  HOFFMAN, Dawn Marie ,  JUNG, Joon ,  LIU, Duan ,  PETERSON, Scott ,  SIU, Tony ,  TORRES, Luis E. ,  ZHANG, Hongjun ,  WEI, Zhongyong ,  SHI, Feng

IPC: C07D231/10 ,  A61K31/415 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D405/08 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

公开(公告)号：EP2863914A1

公开(公告)日：2015-04-29

申请号：EP13807800.1

申请日：2013-06-18

Applicant: Merck Sharp & Dohme Corp. ,  Merck Canada Inc.

Inventor： MACHACEK, Michele, R. ,  ALTMAN, Michael, D. ,  ROMEO, Eric, T. ,  WITHARANA, Dilrukshi ,  CASH, Brandon ,  SIU, Tony ,  ZHOU, Hua ,  CHRISTOPHER, Matthew ,  KATTAR, Solomon, D. ,  HAIDLE, Andrew, M. ,  CHILDERS, Kaleen Konrad ,  MADDESS, Matthew, H. ,  REUTERSHAN, Michael, H. ,  DUCHARME, Yves ,  GUERIN, David, J. ,  SPENCER, Kerrie ,  BEAULIEU, Christian ,  TRUONG, Vouy Linh ,  GUAY, Daniel ,  NORTHRUP, Alan, B. ,  TAOKA, Brandon, M. ,  LIM, Jongwon ,  FISCHER, Christian ,  BUTCHER, John, W. ,  OTTE, Ryan, D. ,  SUN, Binyuan ,  ELLIS, John, Michael

IPC: A61K31/50 ,  A61K31/501

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.

Abstract translation: 本发明提供了式I的新型吡唑衍生物，它们是脾酪氨酸激酶的有效抑制剂，并且可用于治疗和预防由所述酶介导的疾病，例如哮喘，COPD，类风湿性关节炎和癌症。

公开(公告)号：EP2758051A1

公开(公告)日：2014-07-30

申请号：EP12834379.5

申请日：2012-09-21

Applicant: Merck Sharp & Dohme Corp.

Inventor： BRUBAKER, Jason ,  CHILDERS, Matthew Lloyd ,  CHRISTOPHER, Matthew ,  CLOSE, Joshua, T. ,  KATZ, Jason David ,  JUNG, Joon ,  PETERSON, Scott ,  SILIPHAIVANH, Phieng ,  SIU, Tony ,  SMITH, Graham Frank ,  TORRES, Luis, E. ,  WOO, Hyun Chong ,  YOUNG, Jonathan, R. ,  ZHANG, Hongjun

IPC: A61K31/415 ,  C07D231/02

CPC classification number: C07D405/08 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Abstract translation: 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。

公开(公告)号：EP2166846A1

公开(公告)日：2010-03-31

申请号：EP08768504.6

申请日：2008-06-16

Applicant: Merck Sharp & Dohme Corp.

Inventor： ALTMAN, Michael ,  CHRISTOPHER, Matthew ,  GRIMM, Jonathan, B. ,  HAIDLE, Andrew ,  KONRAD, Kaleen ,  LIM, Jongwon ,  MACCOSS, Rachel, N. ,  MACHACEK, Michelle ,  OSIMBONI, Ekundayo ,  OTTE, Ryan, D. ,  SIU, Tony ,  SPENCER, Kerrie ,  TAOKA, Brandon ,  TEMPEST, Paul ,  WILSON, Kevin ,  WOO, Hyun Chong ,  YOUNG, Jonathan ,  ZABIEREK, Anna

IPC: A01N43/06 ,  A61K31/38 ,  A61K31/535

CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10 ,  C07F9/65586 ,  C07F9/65685

Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

公开(公告)号：EP3344644A1

公开(公告)日：2018-07-11

申请号：EP16835872.9

申请日：2016-08-11

Applicant: Merck Sharp & Dohme Corp.

Inventor： ALTMAN, Michael, D. ,  ANDRESEN, Brian ,  CHANG, Wonsuk ,  CHILDERS, Matthew Lloyd ,  CUMMING, Jared, N. ,  HAIDLE, Andrew Marc ,  HENDERSON, Timothy, J. ,  JEWELL, James, P. ,  LU, Min ,  NORTHRUP, Alan, B. ,  OTTE, Ryan, D. ,  SIU, Tony ,  TROTTER, Benjamin Wesley ,  TRUONG, Quang, T.

IPC: C07H21/02

CPC classification number: C07H21/04 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7084 ,  A61K39/39 ,  A61P35/00 ,  C07H19/20 ,  C07H19/23 ,  C07H21/00 ,  C07H21/02

Abstract: A class of polycyclic compounds of general formula (I), of general formula (I'), or of general formula (I"), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.