公开(公告)号：US20250057817A1

公开(公告)日：2025-02-20

申请号：US18443925

申请日：2024-02-16

Applicant: AMGEN INC.

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

Abstract: 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：US20220395504A1

公开(公告)日：2022-12-15

申请号：US17363878

申请日：2021-06-30

Applicant: Amgen Inc.

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

IPC: A61K31/517 ,  A61P35/00 ,  A61K31/4985 ,  A61K39/395 ,  C07D403/04 ,  C07D471/04

Abstract: 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：US20200069657A1

公开(公告)日：2020-03-05

申请号：US16675121

申请日：2019-11-05

Applicant: AMGEN INC.

Inventor： 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: 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

Abstract: Provided herein are methods of treating cancer with KRAS G12C inhibitors and compositions of the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：US20180177767A1

公开(公告)日：2018-06-28

申请号：US15849905

申请日：2017-12-21

Applicant: AMGEN INC.

Inventor： 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: A61K31/428 ,  A61K31/496 ,  A61K31/519 ,  A61K31/517 ,  A61K31/5025 ,  A61K31/502 ,  A61P35/00

Abstract: 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：US20170035744A1

公开(公告)日：2017-02-09

申请号：US15298748

申请日：2016-10-20

Applicant: AMGEN INC.

Inventor： Ning CHEN ,  Xiaoqi CHEN ,  Yinhong CHEN ,  Alan C. CHENG ,  Richard V. CONNORS ,  Jeffrey DEIGNAN ,  Paul John DRANSFIELD ,  Xiaohui DU ,  Zice FU ,  Julie Anne HEATH ,  Daniel HORNE ,  Jonathan HOUZE ,  Matthew R. KALLER ,  Aarif Yusuf KHAKOO ,  David John KOPECKY ,  Su-Jen LAI ,  Zhihua MA ,  Lawrence R. MCGEE ,  Julio C. MEDINA ,  Jeffrey T. MIHALIC ,  Nobuko NISHIMURA ,  Steven H. OLSON ,  Vatee PATTAROPONG ,  Gayathri SWAMINATH ,  Xiaodong WANG ,  Kevin YANG ,  Wen-Chen YEH ,  Mikkel V. DEBENEDETTO ,  Robert P. FARRELL ,  Simon J. HEDLEY ,  Ted C. JUDD ,  Frank KAYSER

IPC: A61K31/4439 ,  C07D239/30 ,  C07D241/18 ,  C07D213/61 ,  A61K31/695 ,  A61K31/444 ,  A61K31/497 ,  A61K31/437 ,  A61K31/501 ,  A61K45/06 ,  C07C311/13 ,  C07D241/12 ,  C07D239/34 ,  C07D295/16 ,  A61K31/506 ,  C07D239/26

CPC classification number: A61K31/506 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07C311/13 ,  C07D211/54 ,  C07D213/61 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D241/24 ,  C07D249/08 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.

公开(公告)号：US20220168280A1

公开(公告)日：2022-06-02

申请号：US17589163

申请日：2022-01-31

Applicant: AMGEN INC.

Inventor： 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: 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

Abstract: 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：US20170144971A1

公开(公告)日：2017-05-25

申请号：US15412804

申请日：2017-01-23

Applicant: AMGEN INC.

Inventor： Michael D. BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason A. DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian M. FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael W. GRIBBLE, Jr. ,  Darin J. GUSTIN ,  Julie A. HEATH ,  Xin HUANG ,  XianYun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  SuJen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan D. LOW ,  Brian S. LUCAS ,  Zhihua MA ,  Lawrence R. MCGEE ,  Joel MCINTOSH ,  Dustin L. MCMINN ,  Julio C. MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven H. OLSON ,  Yosup REW ,  Phillip M. ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

IPC: C07D211/76 ,  C07D417/12 ,  C07D413/06 ,  C07D471/10 ,  C07D409/04 ,  C07D417/06 ,  C07D405/04 ,  C07D401/04 ,  C07D279/02 ,  C07D401/12 ,  C07D491/08 ,  C07D498/08 ,  C07D409/12 ,  C07D405/12 ,  C07D417/14 ,  C07D498/20 ,  C07D401/06

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

公开(公告)号：US20160137667A1

公开(公告)日：2016-05-19

申请号：US15008342

申请日：2016-01-27

Applicant: AMGEN INC.

Inventor： Michael D. BARTBERGER ,  Ana GONZALEZ BUENROSTRO ,  Hilary Plake BECK ,  Xiaoqi CHEN ,  Richard Victor CONNORS ,  Jeffrey DEIGNAN ,  Jason A. DUQUETTE ,  John EKSTEROWICZ ,  Benjamin FISHER ,  Brian M. FOX ,  Jiasheng FU ,  Zice FU ,  Felix GONZALEZ LOPEZ DE TURISO ,  Michael W. GRIBBLE, JR. ,  Darin J. GUSTIN ,  Julie A. HEATH ,  Xin HUANG ,  XianYun JIAO ,  Michael G. JOHNSON ,  Frank KAYSER ,  David John KOPECKY ,  SuJen LAI ,  Yihong LI ,  Zhihong LI ,  Jiwen LIU ,  Jonathan D. LOW ,  Brian S. LUCAS ,  Zhihua MA ,  Lawrence R. MCGEE ,  Joel MCINTOSH ,  Dustin L. MCMINN ,  Julio C. MEDINA ,  Jeffrey Thomas MIHALIC ,  Steven H. OLSON ,  Yosup REW ,  Phillip M. ROVETO ,  Daqing SUN ,  Xiaodong WANG ,  Yingcai WANG ,  Xuelei YAN ,  Ming YU ,  Jiang ZHU

IPC: C07D498/14 ,  C07D221/20 ,  C07D471/10

CPC classification number: C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

Abstract translation: 本发明提供了式I的MDM2抑制剂化合物，其中变量如上所定义，哪些化合物可用作治疗剂，特别是用于治疗癌症。 本发明还涉及含有MDM2抑制剂的药物组合物。

公开(公告)号：US20200055845A1

公开(公告)日：2020-02-20

申请号：US16661907

申请日：2019-10-23

Applicant: Amgen Inc.

Inventor： Brian Alan LANMAN ,  Jian CHEN ,  Anthony B. REED ,  Victor J. CEE ,  Longbin LIU ,  David John KOPECKY ,  Patricia LOPEZ ,  Ryan Paul WURZ ,  Thomas T. NGUYEN ,  Shon BOOKER ,  Nobuko NISHIMURA ,  Youngsook SHIN ,  Nuria A. TAMAYO ,  John Gordon ALLEN ,  Jennifer Rebecca ALLEN

IPC: C07D417/04 ,  C07D475/00 ,  C07D275/04 ,  A61K31/7068 ,  A61P35/00 ,  A61K31/5025 ,  A61K31/502 ,  A61K31/519 ,  A61K31/517 ,  A61K31/454 ,  A61K31/55 ,  A61K31/416 ,  A61K31/496 ,  C07D403/04 ,  C07D237/34 ,  C07D401/14 ,  C07D239/80 ,  C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04 ,  C07D417/12 ,  C07D487/08 ,  A61K38/07

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

公开(公告)号：US20170320860A1

公开(公告)日：2017-11-09

申请号：US15584109

申请日：2017-05-02

Applicant: AMGEN INC.

Inventor： Xiaoqi CHEN ,  Yinhong CHEN ,  Alan C. CHENG ,  Richard V. CONNORS ,  Mikkel V. DEBENEDETTO ,  Paul John DRANSFIELD ,  Zice FU ,  James S. HARVEY ,  Julie Anne HEATH ,  Simon J. HEDLEY ,  Jonathan HOUZE ,  Ted C. JUDD ,  Aarif Yusuf KHAKOO ,  David John KOPECKY ,  Su-Jen LAI ,  Zhihua MA ,  Nobuko NISHIMURA ,  Steven H. OLSON ,  Vatee PATTAROPONG ,  Gayathri SWAMINATH ,  Xiaodong WANG ,  Wen-Chen YEH

IPC: C07D405/14 ,  C07D471/04 ,  C07D405/04 ,  A61K31/5383 ,  A61K31/437 ,  A61K31/506 ,  A61K31/497 ,  A61K31/4439 ,  C07D498/04 ,  A61K45/06

CPC classification number: C07D405/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D471/04 ,  C07D498/04

Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.