公开(公告)号：US20240092794A1

公开(公告)日：2024-03-21

申请号：US18502780

申请日：2023-11-06

申请人： AMGEN INC.

发明人： Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Brian Alan LANMAN ,  Patricia LOPEZ ,  Francesco MANONI ,  Liping H. PETTUS ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Nicholas Anthony WEIRES

IPC分类号： C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

CPC分类号： C07D491/06 ,  A61P35/00 ,  C07D471/06 ,  C07D471/16 ,  C07D491/16

摘要： Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

公开(公告)号：US20190381064A1

公开(公告)日：2019-12-19

申请号：US16547747

申请日：2019-08-22

申请人： AMGEN INC.

发明人： Paul E. HARRINGTON ,  Kate ASHTON ,  Sean P. BROWN ,  Matthew R. KALLER ,  Todd J. KOHN ,  Brian Alan LANMAN ,  Kexue LI ,  Yunxiao LI ,  Jonathan D. LOW ,  Ana Elena MINATTI ,  Alexander J. PICKRELL ,  Markian M. STEC ,  Joshua TAYGERLY

IPC分类号： A61K31/553 ,  A61P35/02 ,  A61P35/00 ,  C07D498/08

摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

公开(公告)号：US20240294551A1

公开(公告)日：2024-09-05

申请号：US18614911

申请日：2024-03-25

申请人： AMGEN INC.

发明人： Ryan Paul Wurz ,  Yunxiao LI ,  Primali Vasundera NAVARATNE ,  Jose M. MEDINA ,  Ning CHEN ,  Liping PETTUS ,  Xiaofen LI ,  John STELLWAGEN ,  Kexue LI ,  Brian Alan LANMAN ,  Michael M. YAMANO ,  Wei ZHAO ,  Benjamin WIGMAN ,  Fabien EMMETIERE ,  Albert K. AMEGADZIE ,  Christopher P. MOHR ,  Aaron C. SIEGMUND ,  Rene RAHIMOFF ,  Zhichen WU ,  Adriano BAUER ,  Andrew SMALIGO ,  Quentin Tercenio ,  Qingyian Liu ,  Shon K. Booker

IPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

摘要： The present disclosure provides compounds useful for the inhibition of KRAS G12D, G12V, G12A, G12S, G13D, Q61H, Q61L or G12C. The compounds have a general Formula I′:




wherein the variables of Formula I′ are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US20240287068A1

公开(公告)日：2024-08-29

申请号：US18640641

申请日：2024-04-19

申请人： Amgen Inc.

发明人： Brian Alan LANMAN ,  Shon BOOKER ,  Clifford GOODMAN ,  Anthony B. REED ,  Jonathan D. LOW ,  Hui-Ling WANG ,  Ning CHEN ,  Ana Elena MINATTI ,  Ryan WURZ ,  Victor J. CEE

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/7068 ,  A61K38/07 ,  A61P35/00

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61P35/00 ,  A61K31/7068 ,  A61K38/07 ,  A61K2300/00

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20220175782A1

公开(公告)日：2022-06-09

申请号：US17579359

申请日：2022-01-19

申请人： AMGEN INC.

发明人： John Gordon ALLEN ,  Brian Alan LANMAN ,  Jian CHEN ,  Anthony B. REED ,  Victor J. CEE ,  Longbin LIU ,  Patricia LOPEZ ,  Ryan Paul WURZ ,  Thomas T. NGUYEN ,  Shon BOOKER ,  Jennifer Rebecca ALLEN ,  Margaret CHU-MOYER ,  Albert AMEGADZIE ,  Ning CHEN ,  Clifford GOODMAN ,  Jonathan D. LOW ,  Vu Van MA ,  Ana Elena MINATTI ,  Nobuko NISHIMURA ,  Alexander J. PICKRELL ,  Hui-Ling WANG ,  Youngsook SHIN ,  Aaron C. SIEGMUND ,  Kevin C. YANG ,  Nuria A. TAMAYO ,  Mary WALTON ,  Qiufen XUE

IPC分类号： A61K31/519 ,  A61K31/551 ,  A61K39/395 ,  A61P35/00

摘要： Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20220168280A1

公开(公告)日：2022-06-02

申请号：US17589163

申请日：2022-01-31

申请人： AMGEN INC.

发明人： Brian Alan LANMAN ,  Victor J. CEE ,  Alexander J. PICKRELL ,  Anthony B. REED ,  Kevin C. YANG ,  David John KOPECKY ,  Hui-Ling WANG ,  Patricia LOPEZ ,  Kate ASHTON ,  Shon BOOKER ,  Christopher M. TEGLEY

IPC分类号： A61K31/428 ,  A61K31/496 ,  A61K31/519 ,  A61P35/00 ,  A61K31/5025 ,  A61K31/502 ,  A61K31/517 ,  C07D275/04 ,  C07D471/08 ,  C07D403/04 ,  C07D401/04 ,  C07D513/04 ,  C07D487/04 ,  C07D417/04 ,  C07D239/80 ,  C07D487/10 ,  C07D471/04

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20200165231A1

公开(公告)日：2020-05-28

申请号：US16687546

申请日：2019-11-18

申请人： Amgen Inc.

发明人： Youngsook SHIN ,  Victor J. CEE ,  Christopher M. TEGLEY ,  Brian Alan LANMAN ,  Ryan Paul WURZ ,  Kevin C. YANG ,  Vu Van MA ,  Daniel ERLANSON ,  Joon Won JEONG ,  Raymond V. FUCINI ,  Jeffrey IWIG

IPC分类号： C07D403/14 ,  C07D487/04 ,  C07D403/12 ,  C07D498/04 ,  C07D471/04 ,  C07D417/14 ,  C07D401/14 ,  A61P35/00

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20190336514A1

公开(公告)日：2019-11-07

申请号：US16402589

申请日：2019-05-03

申请人： Amgen Inc.

发明人： Ryan Paul WURZ ,  Victor J. CEE ,  Albert AMEGADZIE ,  Ning CHEN ,  Brian Alan LANMAN ,  Michael D. BARTBERGER

IPC分类号： A61K31/675 ,  A61P35/00 ,  A61K31/553 ,  A61K31/167 ,  C07K16/30

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20220213101A1

公开(公告)日：2022-07-07

申请号：US17692026

申请日：2022-03-10

申请人： Amgen Inc.

发明人： Brian Alan LANMAN ,  Shon BOOKER ,  Clifford GOODMAN ,  Anthony B. REED ,  Jonathan D. LOW ,  Hui-Ling WANG ,  Ning CHEN ,  Ana Elena MINATTI ,  Ryan WURZ ,  Victor J. CEE

IPC分类号： C07D471/04 ,  A61P35/00 ,  A61K31/519

摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20220194955A1

公开(公告)日：2022-06-23

申请号：US17552016

申请日：2021-12-15

申请人： AMGEN INC.

发明人： Shon BOOKER ,  Matthew Paul BOURBEAU ,  John R. BUTLER ,  Sanne Ormholt Schroder GLAD ,  Brian Alan LANMAN ,  Patricia LOPEZ ,  Francesco MANONI ,  Liping H. PETTUS ,  Ian SARVARY ,  Nuria A. TAMAYO ,  Mikkel VESTERGAARD ,  Nicholas Anthony WEIRES

IPC分类号： C07D491/06 ,  C07D491/16 ,  C07D471/06 ,  C07D471/16 ,  A61P35/00

摘要： Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: