公开(公告)号：US20240239788A1

公开(公告)日：2024-07-18

申请号：US18555640

申请日：2022-04-15

申请人： Merck Sharp & Dohme LLC

发明人： David L. Sloman ,  Gianni Chessari ,  Patrick Schöpf ,  Steven Howard ,  Yuichi Kawai ,  Kazuaki Shibata ,  Hiroki Asakura ,  Takao Uno ,  Takeshi Sagara ,  Masayuki Nakamura ,  Yu Kobayakawa ,  David Jonathan Bennett ,  Indu Bharathan ,  Thomas H. Graham ,  Yongxin Han ,  Zahid Hussain ,  Xiaoshen Ma ,  Mihir Mandal ,  Ryan D. Otte ,  Anandan Palani ,  Uma Swaminathan ,  Mycah Uehling ,  Yingchun Ye ,  Ryan Chau ,  Alec H. Christian ,  Symon Gathiaka ,  Timothy J. Henderson ,  Elisabeth T. Hennessy ,  Andrew J. Hoover ,  Shuhei Kawamura ,  Igri Kolaj ,  Thomas W. Lyons ,  Matthew J. Mitcheltree ,  Aaron Sather

IPC分类号： C07D451/06 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/08 ,  C07D519/00

CPC分类号： C07D451/06 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/08 ,  C07D519/00

摘要： Compounds or their pharmaceutically acceptable salts can inhibit the G12D 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：US20240083913A1

公开(公告)日：2024-03-14

申请号：US18311639

申请日：2023-05-03

申请人： Merck Sharp & Dohme LLC

发明人： Indu Bharathan ,  Symon Gathiaka ,  Yongxin Han ,  Xiaoshen Ma ,  Ryan D. Otte ,  David L. Sloman ,  Thomas H. Graham ,  Timothy Henderson ,  Elisabeth Hennessy ,  Anandan Palani

IPC分类号： C07D498/22 ,  A61K31/519 ,  A61P35/00 ,  C07D471/22 ,  C07D519/00

CPC分类号： C07D498/22 ,  A61K31/519 ,  A61P35/00 ,  C07D471/22 ,  C07D519/00 ,  C07B2200/05

摘要： The disclosure provides compounds of Formula (I)




or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, CY, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The 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 of Formula (I) 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：US20240043448A1

公开(公告)日：2024-02-08

申请号：US18311646

申请日：2023-05-03

申请人： Merck Sharp & Dohme LLC

发明人： Indu Bharathan ,  Symon Gathiaka ,  Yongxin Han ,  Xiaoshen Ma ,  Ryan D. Otte ,  David L. Sloman ,  Thomas H. Graham ,  Timothy Henderson ,  Elisabeth Hennessy ,  Anandan Palani

IPC分类号： C07D498/22 ,  A61P35/00 ,  A61K31/519 ,  C07D471/22 ,  C07D519/00

CPC分类号： C07D498/22 ,  A61P35/00 ,  A61K31/519 ,  C07D471/22 ,  C07D519/00 ,  C07B2200/05

摘要： The disclosure provides compounds of Formula (I)




or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz, and the subscripts m, n, q, and r are as described herein. The 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 of Formula (I) 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：US20230322785A1

公开(公告)日：2023-10-12

申请号：US18015387

申请日：2022-07-21

申请人： Christopher W. BOYCE ,  Thomas H. GRAHAM ,  Andrew J. HOOVER ,  Xianhai HUANG ,  Rognze KUANG ,  Jae-Hun KIM ,  Joseph M. KELLY ,  Michael Man-Chu LO ,  Jing SU ,  Dong XIAO ,  Xiaohong ZHU ,  Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Christopher W. Boyce ,  Jared N. Cumming ,  Duane DeMong ,  Thomas H. Graham ,  Subrahmanyam Gudipati ,  Andrew J. Hoover ,  Xianhai Huang ,  Rongze Kuang ,  Jae-Hun Kim ,  Joseph M. Kelly ,  Yeon-Hee Lim ,  Michael Man-Chu Lo ,  Jesus Moreno ,  Jing Su ,  Heping Wu ,  Dong Xiao ,  Younong Yu ,  Xiaohong Zhu

IPC分类号： C07D487/04 ,  C07K16/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07K16/2896

摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US12060357B2

公开(公告)日：2024-08-13

申请号：US17657515

申请日：2022-03-31

申请人： Merck Sharp & Dohme LLC

发明人： Matthew A. Larsen ,  Amjad Ali ,  Jared Cumming ,  Duane DeMong ,  Qiaolin Deng ,  Thomas H. Graham ,  Elisabeth Hennessy ,  Andrew J. Hoover ,  Ping Liu ,  Kun Liu ,  Umar Faruk Mansoor ,  Jianping Pan ,  Christopher W. Plummer ,  Aaron Sather ,  Uma Swaminathan ,  Huijun Wang ,  Yonglian Zhang

IPC分类号： C07D487/04 ,  C07K16/28

CPC分类号： C07D487/04 ,  C07K16/2818

摘要： In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I):




and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US20240076297A1

公开(公告)日：2024-03-07

申请号：US18015364

申请日：2021-07-22

申请人： Merck Sharp & Dohme LLC

发明人： Amjad Ali ,  Jared N. Cumming ,  Manuel De Lera Ruiz ,  Duane DeMong ,  Thomas H. Graham ,  Elisabeth T. Hennessy ,  Joseph M. Kelly ,  Rongze Kuang ,  Michael Man-Chu Lo ,  Umar Faruk Mansoor ,  Jesus Moreno ,  Uma Swaminathan ,  Heping Wu ,  Yingchun Ye ,  Younong Yu

IPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/28

CPC分类号： C07D487/04 ,  A61K45/06 ,  C07D519/00 ,  C07K16/2818

摘要： The present invention provides compounds of the structural Formula (I), and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

公开(公告)号：US11697657B2

公开(公告)日：2023-07-11

申请号：US17081477

申请日：2020-10-27

申请人： Merck Sharp & Dohme LLC

发明人： Indu Bharathan ,  Symon Gathiaka ,  Yongxin Han ,  Xiaoshen Ma ,  Ryan D. Otte ,  David L. Sloman ,  Thomas H. Graham ,  Timothy Henderson ,  Elisabeth Hennessy ,  Anandan Palani

IPC分类号： A61K31/519 ,  A61P35/00 ,  C07D498/22 ,  C07D471/22 ,  C07D519/00

CPC分类号： C07D498/22 ,  A61K31/519 ,  A61P35/00 ,  C07D471/22 ,  C07D519/00 ,  C07B2200/05

摘要： The disclosure provides compounds of Formula (I)




or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz and the subscripts m, n, q, and r are as described herein. The 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 of Formula (I) 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.