公开(公告)号：WO2022051337A1

公开(公告)日：2022-03-10

申请号：PCT/US2021/048620

申请日：2021-09-01

申请人： MERCK SHARP & DOHME CORP. ,  ACTON, John, J., III ,  CHAU, Ryan ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KATTAR, Solomon ,  KEYLOR, Mitchell, H. ,  LI, Derun ,  MARGREY, Kaila, A. ,  MORRIELLO, Gregori, J. ,  YAN, Xin

发明人： ACTON, John, J., III ,  CHAU, Ryan ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KATTAR, Solomon ,  KEYLOR, Mitchell, H. ,  LI, Derun ,  MARGREY, Kaila, A. ,  MORRIELLO, Gregori, J. ,  YAN, Xin

IPC分类号： C07D239/84 ,  C07D239/95 ,  C07D401/12

摘要： The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R3, R4,X1, and X2 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：WO2020247298A2

公开(公告)日：2020-12-10

申请号：PCT/US2020/035505

申请日：2020-06-01

申请人： MERCK SHARP & DOHME CORP. ,  ZHOU, Hua ,  ACTON, John, J., III ,  ARDOLINO, Michael, J. ,  CHEN, Yi-Heng ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KAPLAN, William, P. ,  KATTAR, Solomon, D. ,  KEYLOR, Mitchell, H. ,  LI, Derun ,  LOGAN, Kaitlyn Marie ,  LU, Min ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh, F. ,  PIO, Barbara ,  SCIAMMETTA, Nunzio ,  SIMOV, Vladimir ,  SU, Jing ,  TORRES, Luis ,  YAN, Xin

发明人： ZHOU, Hua ,  ACTON, John, J., III ,  ARDOLINO, Michael, J. ,  CHEN, Yi-Heng ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KAPLAN, William, P. ,  KATTAR, Solomon, D. ,  KEYLOR, Mitchell, H. ,  LI, Derun ,  LOGAN, Kaitlyn Marie ,  LU, Min ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh, F. ,  PIO, Barbara ,  SCIAMMETTA, Nunzio ,  SIMOV, Vladimir ,  SU, Jing ,  TORRES, Luis ,  YAN, Xin

IPC分类号： C07D471/02

摘要： The present invention is directed to substituted certain 1-pyrazolyl, 5-, 6- disubstituted indazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and ring A 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 diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

公开(公告)号：WO2021080929A1

公开(公告)日：2021-04-29

申请号：PCT/US2020/056401

申请日：2020-10-20

申请人： MERCK SHARP & DOHME CORP. ,  KEYLOR, Mitchell, H. ,  ARDOLINO, Michael, J. ,  CHAU, Ryan, W. ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KATTAR, Solomon, D. ,  MARGREY, Kaila, A. ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh, F. ,  YAN, Xin ,  YU, Elsie, C. ,  ZARATE SAEZ, Cayetena Carmela

发明人： KEYLOR, Mitchell, H. ,  ARDOLINO, Michael, J. ,  CHAU, Ryan, W. ,  FULLER, Peter, H. ,  GULATI, Anmol ,  JOHNSON, Rebecca Elizabeth ,  KATTAR, Solomon, D. ,  MARGREY, Kaila, A. ,  MORRIELLO, Gregori, J. ,  NEELAMKAVIL, Santhosh, F. ,  YAN, Xin ,  YU, Elsie, C. ,  ZARATE SAEZ, Cayetena Carmela

IPC分类号： A61K31/4155 ,  A61K31/505 ,  A61K31/517 ,  A61P25/16 ,  C07D231/14 ,  C07D239/78

摘要： The present invention is directed to substituted certain N-(heteroaryl)quinazolin-2-amine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein J, R3, and R4, 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 diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.