公开(公告)号：WO2022177869A1

公开(公告)日：2022-08-25

申请号：PCT/US2022/016378

申请日：2022-02-15

Applicant: MERCK SHARP & DOHME LLC ,  LIM, Jongwon ,  SIMOV, Vladimir ,  VARA, Brandon, A. ,  YEUNG, Charles, S. ,  SCHNEIDER, Sebastian, E. ,  DIMAURO, Erin, F.

Inventor： LIM, Jongwon ,  SIMOV, Vladimir ,  VARA, Brandon, A. ,  YEUNG, Charles, S. ,  SCHNEIDER, Sebastian, E. ,  DIMAURO, Erin, F.

IPC: A61K31/18 ,  A61K31/407 ,  C07D487/04 ,  A61P35/00

Abstract: The present invention is directed to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or pharmaceutical salts thereof.

公开(公告)号：WO2021126729A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/064759

申请日：2020-12-14

Applicant: MERCK SHARP & DOHME CORP. ,  MACHACEK, Michelle ,  ALTMAN, Michael, D. ,  KAWAMURA, Shuhei ,  REUTERSHAN, Michael, H. ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  SCHNEIDER, Sebastian, E. ,  YEUNG, Charles, S. ,  WITTER, David, J. ,  GIBEAU, Craig, R.

Inventor： MACHACEK, Michelle ,  ALTMAN, Michael, D. ,  KAWAMURA, Shuhei ,  REUTERSHAN, Michael, H. ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  SCHNEIDER, Sebastian, E. ,  YEUNG, Charles, S. ,  WITTER, David, J. ,  GIBEAU, Craig, R.

IPC: A61K31/4747 ,  A61P25/04 ,  C07D471/10

Abstract: The present invention provides a compound of Formula (I) (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

公开(公告)号：WO2021126728A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/064755

申请日：2020-12-14

Applicant: MERCK SHARP & DOHME CORP. ,  MACHACEK, Michelle ,  ALTMAN, Michael, D. ,  HUANG, Chunhui ,  REUTERSHAN, Michael, H. ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  SCHNEIDER, Sebastian, E. ,  YEUNG, Charles, S. ,  WITTER, David, J. ,  GIBEAU, Craig, R. ,  YE, Yingchun

Inventor： MACHACEK, Michelle ,  ALTMAN, Michael, D. ,  HUANG, Chunhui ,  REUTERSHAN, Michael, H. ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  SCHNEIDER, Sebastian, E. ,  YEUNG, Charles, S. ,  WITTER, David, J. ,  GIBEAU, Craig, R. ,  YE, Yingchun

IPC: A61K31/4725 ,  C07D217/00 ,  C07D401/14 ,  A61P35/00

Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

公开(公告)号：WO2020033288A1

公开(公告)日：2020-02-13

申请号：PCT/US2019/045050

申请日：2019-08-05

Applicant: MERCK SHARP & DOHME CORP. ,  IDENIX PHARMACEUTICALS LLC ,  MACHACEK, Michelle ,  WITTER, David ,  GIBEAU, Craig ,  HUANG, Chunhui ,  KAWAMURA, Shuhei ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  QUIROZ, Ryan ,  WAN, Murray ,  SCHNEIDER, Sebastian ,  YEUNG, Charles, S. ,  REUTERSHAN, Michael, H. ,  HENDERSON, Timothy, J. ,  PAPARIN, Jean-Laurent ,  RAHALI, Houcine ,  HUGHES, Jonathan, M., E. ,  SANYAL, Sulagna ,  YE, Yingchun ,  CANDITO, David, A. ,  FIER, Patrick, S. ,  SILVERMAN, Steven, M.

Inventor： MACHACEK, Michelle ,  WITTER, David ,  GIBEAU, Craig ,  HUANG, Chunhui ,  KAWAMURA, Shuhei ,  SLOMAN, David, L. ,  SILIPHAIVANH, Phieng ,  QUIROZ, Ryan ,  WAN, Murray ,  SCHNEIDER, Sebastian ,  YEUNG, Charles, S. ,  REUTERSHAN, Michael, H. ,  HENDERSON, Timothy, J. ,  PAPARIN, Jean-Laurent ,  RAHALI, Houcine ,  HUGHES, Jonathan, M., E. ,  SANYAL, Sulagna ,  YE, Yingchun ,  CANDITO, David, A. ,  FIER, Patrick, S. ,  SILVERMAN, Steven, M.

IPC: A61K31/519 ,  C07D471/04

Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

公开(公告)号：WO2020033282A1

公开(公告)日：2020-02-13

申请号：PCT/US2019/045040

申请日：2019-08-05

Applicant: MERCK SHARP & DOHME CORP. ,  WITTER, David ,  KAWAMURA, Shuhei ,  MACHACEK, Michelle ,  QUIROZ, Ryan ,  REUTERSHAN, Michael, H. ,  SCHNEIDER, Sebastian ,  SILIPHAIVANH, Phieng ,  YE, Yingchun ,  YEUNG, Charles, S.

Inventor： WITTER, David ,  KAWAMURA, Shuhei ,  MACHACEK, Michelle ,  QUIROZ, Ryan ,  REUTERSHAN, Michael, H. ,  SCHNEIDER, Sebastian ,  SILIPHAIVANH, Phieng ,  YE, Yingchun ,  YEUNG, Charles, S.

IPC: C07D487/04 ,  C07D519/00

Abstract: The present invention provides a compound of Formula (I) Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

公开(公告)号：WO2022197577A1

公开(公告)日：2022-09-22

申请号：PCT/US2022/020110

申请日：2022-03-14

Applicant: MERCK SHARP & DOHME LLC ,  CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, J. ,  GUNAYDIN, Hakan ,  SCOTT, Jack, D. ,  TANG, Haiqun ,  YEUNG, Charles, S.

Inventor： CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, J. ,  GUNAYDIN, Hakan ,  SCOTT, Jack, D. ,  TANG, Haiqun ,  YEUNG, Charles, S.

IPC: A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  C07D231/10 ,  C07D231/12 ,  C07D231/14

Abstract: The present invention is directed to certain (hetero)aroyl 4-aminopyrazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

公开(公告)号：WO2022197575A1

公开(公告)日：2022-09-22

申请号：PCT/US2022/020108

申请日：2022-03-14

Applicant: MERCK SHARP & DOHME LLC ,  CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, H. ,  GULATI, Anmol ,  GUNAYDIN, Hakan ,  KATTAR, Solomon, D. ,  KURUKULASURIYA, Ravi ,  METHOT, Joey, L. ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh ,  LAPOINTE, Blair, T. ,  SIMOV, Vladimir ,  YEUNG, Charles, S.

Inventor： CHILDERS, Kaleen Konrad ,  ELLIS, J. Michael ,  FULLER, Peter, H. ,  GULATI, Anmol ,  GUNAYDIN, Hakan ,  KATTAR, Solomon, D. ,  KURUKULASURIYA, Ravi ,  METHOT, Joey, L. ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh ,  LAPOINTE, Blair, T. ,  SIMOV, Vladimir ,  YEUNG, Charles, S.

IPC: A61K31/166 ,  A61K31/167 ,  A61K31/4155 ,  C07D231/12 ,  C07D401/00 ,  C07D401/14

Abstract: The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, R1, R2, and R3 are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.