公开(公告)号：WO2022232320A1

公开(公告)日：2022-11-03

申请号：PCT/US2022/026601

申请日：2022-04-27

申请人： MERCK SHARP & DOHME CORP.

发明人： SHIBATA, Kazuaki ,  KONDO, Hitomi ,  YAMAMOTO, Tomohiro ,  SAKAMOTO, Toshihiro ,  ASAKURA, Hiroki ,  AKEMOTO, Kei ,  MIURA, Risako ,  SUGIMOTO, Tetsuya ,  DEL POZO, Juan ,  GIAMBUSU, George Madalin ,  GRAHAM, Thomas H. ,  HAN, Yongxin ,  HENNESSY, Elisabeth T. ,  KAWAMURA, Shuhei ,  RYAN, Michael

IPC分类号： A61K31/41 ,  A61K31/4184 ,  A61K31/4353 ,  C07D235/02 ,  C07D235/04 ,  C07D235/08

摘要： Compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds disclosed herein or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

公开(公告)号：WO2022232318A1

公开(公告)日：2022-11-03

申请号：PCT/US2022/026599

申请日：2022-04-27

申请人： MERCK SHARP & DOHME CORP.

发明人： SHIBATA, Kazuaki ,  ASAKURA, Hiroki ,  AKEMOTO, Kei ,  SAKAMOTO, Toshihiro ,  KONDO, Hitomi ,  YAMAMOTO, Tomohiro ,  MIURA, Risako ,  SCHÖPF, Patrick ,  DEL POZO, Juan ,  GIAMBUSU, George Madalin ,  GRAHAM, Thomas H. ,  HAN, Yongxin ,  HENNESSY, Elisabeth T. ,  PALANI, Anandan ,  RYAN, Michael ,  SLOMAN, David L. ,  HOWARD, Steven

IPC分类号： A61K31/409 ,  A61K31/495 ,  A61P35/00 ,  C07D471/14 ,  C07D471/22

摘要： Compounds of Formula (I) or (la) or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or (la) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.

公开(公告)号：WO2022140169A1

公开(公告)日：2022-06-30

申请号：PCT/US2021/063948

申请日：2021-12-17

申请人： MERCK SHARP & DOHME CORP. ,  BAO, Jianming ,  CHENG, Chen ,  CRUZ, Faben, A. ,  LIM, Yeon-Hee ,  HUGELSHOFER, Cedric, L. ,  JIANG, Jinlong ,  MAK, Victor, W. ,  SOUTHGATE, Emma, Helen

发明人： BAO, Jianming ,  CHENG, Chen ,  CRUZ, Faben, A. ,  LIM, Yeon-Hee ,  HUGELSHOFER, Cedric, L. ,  JIANG, Jinlong ,  MAK, Victor, W. ,  SOUTHGATE, Emma, Helen

IPC分类号： A61K31/4162 ,  A61P3/00 ,  C07D491/052

摘要： Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 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 hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.

公开(公告)号：WO2022132545A1

公开(公告)日：2022-06-23

申请号：PCT/US2021/062507

申请日：2021-12-09

申请人： MERCK SHARP & DOHME CORP. ,  COOKE, Andrew, J., Jr. ,  SCHUBERT, Jeffrey, W. ,  SKUDLAREK, Jason, W.

发明人： COOKE, Andrew, J., Jr. ,  SCHUBERT, Jeffrey, W. ,  SKUDLAREK, Jason, W.

IPC分类号： A61K31/7068 ,  A61K31/496 ,  A61K38/46

摘要： The present invention relates to novel Fused [7,5] Bicyclic Pyrazole Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, and R4 are as defined herein. The present invention also relates to compositions comprising at least one Fused [7,5] Bicyclic Pyrazole Derivative, and methods of using the Fused [7,5] Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：WO2022119888A1

公开(公告)日：2022-06-09

申请号：PCT/US2021/061344

申请日：2021-12-01

申请人： MERCK SHARP & DOHME CORP. ,  BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSSEN, Dane James ,  HUANG, Xianhai ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

发明人： BOGEN, Stephane, L. ,  CHEN, Ping ,  CLAUSSEN, Dane James ,  HUANG, Xianhai ,  RUDD, Michael, T. ,  WALSH, Shawn, P. ,  WEI, Lan ,  YANG, Dexi

IPC分类号： A61K31/454 ,  A61P25/20 ,  C07D405/14

摘要： The present invention is directed to 3-heteroaryl pyrrolidine and piperidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 diseases in which orexin receptors are involved.

公开(公告)号：WO2022093881A1

公开(公告)日：2022-05-05

申请号：PCT/US2021/056734

申请日：2021-10-27

申请人： MERCK SHARP & DOHME CORP. ,  FULLER, Peter, H. ,  GULATI, Anmol ,  KATTAR, Solomon, D. ,  KEYLOR, Mitchell, H. ,  MARGREY, Kaila, A. ,  YAN, Xin

发明人： FULLER, Peter, H. ,  GULATI, Anmol ,  KATTAR, Solomon, D. ,  KEYLOR, Mitchell, H. ,  MARGREY, Kaila, A. ,  YAN, Xin

IPC分类号： A61K31/472 ,  A61K31/47 ,  A61K31/44 ,  A61K31/496

摘要： The present invention is directed to certain 2-aminoquinzaoline derivatives of Formula (I) and pharmaceutically acceptable salts thereof, wherein 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：WO2022066823A1

公开(公告)日：2022-03-31

申请号：PCT/US2021/051626

申请日：2021-09-23

申请人： MERCK SHARP & DOHME CORP. ,  HE, Xi ,  QUAN, Shuo ,  WANG, Dexi ,  XU, Min

发明人： HE, Xi ,  QUAN, Shuo ,  WANG, Dexi ,  XU, Min

IPC分类号： C12N15/10 ,  C12P19/34 ,  C12Q1/68 ,  C12Q1/6806

摘要： This application provides materials and methods related to replication competent, noninfectious coronavirus reporter replicons, such as for SARS-CoV-2, MERS, or SARS-CoV-1 comprising at least one coronavirus gene and at least one reporter gene. The application also provides methods for assaying candidate agents for inhibition of coronavirus viral replication.

公开(公告)号：WO2022060767A1

公开(公告)日：2022-03-24

申请号：PCT/US2021/050365

申请日：2021-09-15

申请人： MERCK SHARP & DOHME CORP. ,  ABRAHAM, Anson, A. ,  ALTURA, Rachel, A. ,  WILSON, Douglas, C.

发明人： ABRAHAM, Anson, A. ,  ALTURA, Rachel, A. ,  WILSON, Douglas, C.

IPC分类号： A61K39/395 ,  A61P35/00 ,  C07K16/28

摘要： Provided herein are dosing regimens of an anti-immunoglobulin-like transcript 4 (anti-ILT4) antibody for treating cancer. Further provided are dosing regimens for treating cancer using a combination of an anti-ILT4 antibody and another agent (e.g., a PD-1 antagonist, such as an anti-PD-1 antibody or an anti-PD-L1 antibody).

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：WO2022046747A1

公开(公告)日：2022-03-03

申请号：PCT/US2021/047313

申请日：2021-08-24

申请人： MERCK SHARP & DOHME CORP. ,  FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  PISSARNITSKI, Dmitri, A. ,  YAN, Lin

发明人： FENG, Danqing ,  HUO, Pei ,  KEKEC, Ahmet ,  LIN, Songnian ,  PISSARNITSKI, Dmitri, A. ,  YAN, Lin

IPC分类号： C07K14/62 ,  A61P3/10

摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.