公开(公告)号：EP3706742A1

公开(公告)日：2020-09-16

申请号：EP18875596.1

申请日：2018-11-05

申请人： Merck Sharp & Dohme Corp. ,  Ctxt Pty Ltd

发明人： MACHACEK, Michelle, R. ,  WITTER, David, J. ,  REUTERSHAN, Michael Hale ,  ALTMAN, Michael, D. ,  STUPPLE, Paul Anthony

IPC分类号： A61K31/4375 ,  C07D217/16 ,  C07D401/02

公开(公告)号：EP2788000A1

公开(公告)日：2014-10-15

申请号：EP12855868.1

申请日：2012-11-30

申请人： Merck Sharp & Dohme Corp.

发明人： AHEARN, Sean, P. ,  CHRISTOPHER, Matthew ,  JUNG, Joon ,  PU, Qinglin ,  RIVKIN, Alexey ,  SCOTT, Mark, E. ,  WITTER, David, J. ,  WOO, Hyun Chong ,  CASH, Brandon ,  DINSMORE, Christopher ,  GUERIN, David

IPC分类号： A61K31/519 ,  C07D487/02 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I.

公开(公告)号：EP2185554A1

公开(公告)日：2010-05-19

申请号：EP08795027.5

申请日：2008-08-05

申请人： Merck Sharp & Dohme Corp.

发明人： GRIMM, Jonathan ,  HEIDEBRECHT, Richard, W., Jr. ,  MAMPREIAN, Dawn, M. ,  METHOT, Joey, L. ,  MILLER, Thomas, A. ,  OTTE, Karin, M. ,  PETERSON, Scott ,  SILIPHAIVANH, Phieng ,  WILSON, Kevin, J. ,  WITTER, David, J.

IPC分类号： C07D471/00

CPC分类号： C07F7/0812

摘要： The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.

公开(公告)号：EP2991654B1

公开(公告)日：2018-11-21

申请号：EP14791539.1

申请日：2014-04-25

申请人： Merck Sharp & Dohme Corp.

发明人： LIM, Jongwon ,  HUANG, Xianhai ,  FERGUSON, Ronald, D. ,  ZHOU, Wei ,  BOYCE, Christopher, W. ,  SILIPHAIVANH, Phieng ,  WITTER, David, J. ,  MALETIC, Milana, M. ,  KOZLOWSKI, Joseph, A. ,  WILSON, Kevin, J.

IPC分类号： A61K31/655 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

摘要： and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).

公开(公告)号：EP2900241B1

公开(公告)日：2018-08-08

申请号：EP13840779.6

申请日：2013-09-26

申请人： Merck Sharp & Dohme Corp.

发明人： WILSON, Kevin, J. ,  WITTER, David, J. ,  SILIPHAIVANH, Phieng ,  LIPFORD, Kathryn ,  SLOMAN, David ,  FALCONE, Danielle ,  O'BOYLE, Brendan ,  MANSOOR, Umar Faruk ,  LIM, Jongwon ,  METHOT, Joey, L. ,  BOYCE, Christopher ,  CHEN, Lei ,  DANIELS, Matthew, H. ,  FEVRIER, Salem ,  HUANG, Xianhai ,  KURUKULASURIYA, Ravi ,  TONG, Ling ,  ZHOU, Wei ,  KOZLOWSKI, Joseph ,  MALETIC, Milana, M. ,  SHINKRE, Bidhan, A. ,  THATAI, Jayanth Thiruvellore ,  BAKSHI, Raman Kumar ,  KARUNAKARAN, Ganesh Babu

IPC分类号： C07D471/04 ,  C07D471/16 ,  C07D498/16 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4375 ,  A61P35/00

CPC分类号： C07D498/18 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D498/14 ,  C07D498/16 ,  C07D519/00 ,  A61K2300/00

摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

公开(公告)号：EP2900241A2

公开(公告)日：2015-08-05

申请号：EP13840779.6

申请日：2013-09-26

申请人： Merck Sharp & Dohme Corp.

发明人： WILSON, Kevin, J. ,  WITTER, David, J. ,  SILIPHAIVANH, Phieng ,  LIPFORD, Kathryn ,  SLOMAN, David ,  FALCONE, Danielle ,  O'BOYLE, Brendan ,  MANSOOR, Umar Faruk ,  LIM, Jongwon ,  METHOT, Joey, L. ,  BOYCE, Christopher ,  CHEN, Lei ,  DANIELS, Matthew, H. ,  FEVRIER, Salem ,  HUANG, Xianhai ,  KURUKULASURIYA, Ravi ,  TONG, Ling ,  ZHOU, Wei ,  KOZLOWSKI, Joseph ,  MALETIC, Milana, M. ,  SHINKRE, Bidhan, A. ,  THATAI, Jayanth Thiruvellore ,  BAKSHI, Raman Kumar ,  KARUNAKARAN, Ganesh Babu

IPC分类号： A61K31/4745

CPC分类号： C07D498/18 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/16 ,  C07D498/14 ,  C07D498/16 ,  C07D519/00 ,  A61K2300/00

摘要： Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).

公开(公告)号：EP3371191A1

公开(公告)日：2018-09-12

申请号：EP16860602.8

申请日：2016-10-25

申请人： Merck Sharp & Dohme Corp.

发明人： WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

IPC分类号： C07D487/04 ,  C07D487/12

摘要： The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

公开(公告)号：EP2900223B1

公开(公告)日：2017-10-25

申请号：EP13841687.0

申请日：2013-09-26

申请人： Merck Sharp & Dohme Corp.

发明人： WILSON, Kevin, J. ,  WITTER, David, J. ,  DANIELS, Matthew, H. ,  ANGELES, Angie, R. ,  SILIPHAIVANH, Phieng ,  SLOMAN, David ,  O'BOYLE, Brendan ,  FALCONE, Danielle ,  WHITE, Catherine ,  FERGUSON, Ron ,  ZHOU, Wei ,  LIPFORD, Kathryn ,  MANSOOR, Umar Faruk ,  FEVRIER, Salem ,  HUANG, Xianhai ,  KURUKULASURIYA, Ravi ,  RICHARD, Judson, E. ,  TANG, Shuyi ,  BOYCE, Christopher ,  KOZLOWSKI, Joseph ,  BAKSHI, Raman Kumar ,  KARUNAKARAN, Ganesh Babu

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC分类号： A61K31/437 ,  A61K31/4545 ,  A61K45/06 ,  C07D471/04

公开(公告)号：EP2170339B1

公开(公告)日：2014-10-15

申请号：EP08794377.5

申请日：2008-06-24

申请人： Merck Sharp & Dohme Corp.

发明人： HEIDEBRECHT, Richard, W., Jr. ,  MILLER, Thomas, A. ,  STANTON, Matthew, G. ,  WITTER, David, J.

IPC分类号： A01N43/40

CPC分类号： C07D213/75 ,  C07D409/04 ,  C07D409/14

公开(公告)号：EP3371191B1

公开(公告)日：2020-08-26

申请号：EP16860602.8

申请日：2016-10-25

申请人： Merck Sharp & Dohme Corp.

发明人： WITTER, David, J. ,  BIFTU, Tesfaye ,  BIJU, Purakkattle ,  BOGEN, Stephane, L. ,  HONG, Qingmei ,  HUANG, Chunhui ,  HUANG, Xianhai ,  LI, Bing ,  PARK, Min, K. ,  SLOMAN, David, L.

IPC分类号： C07D491/10 ,  C07D498/08 ,  C07D471/04 ,  C07D519/00 ,  A61P35/02 ,  A61K31/5517