公开(公告)号：US11407721B2

公开(公告)日：2022-08-09

申请号：US16048677

申请日：2018-07-30

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Hilary Plake Beck ,  Michael R. Degraffenreid ,  Brian M. Fox ,  Felix Gonzalez Lopez De Turiso ,  Lisa D. Julian ,  Frank Kayser ,  Julio C. Medina ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xuelei Yan

IPC: C07D265/32 ,  C07D413/06 ,  C07D487/04 ,  C07D279/12 ,  C07D413/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, or the pharmaceutically acceptable salts thereof, 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：US10736883B2

公开(公告)日：2020-08-11

申请号：US16347903

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： Matthew Brown ,  Ning Chen ,  Xiaoqi Chen ,  Yinhong Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Jeffrey Deignan ,  Paul John Dransfield ,  Xiaohui Du ,  Zice Fu ,  James S. Harvey ,  Julie Anne Heath ,  Lars V. Heumann ,  Jonathan Houze ,  Frank Kayser ,  Aarif Yusuf Khakoo ,  David j. Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Julio C. Medina ,  Jeffrey T. Mihalic ,  Steven H. Olson ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Xiaodong Wang ,  Malgorzata Wanska ,  Wen-Chen Yeh

IPC: A61K31/4196 ,  A61K31/341 ,  C07D405/04 ,  C07D405/14 ,  A61K31/421 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/506 ,  C07D239/26 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07F7/08 ,  A61P9/00 ,  A61P9/02 ,  C07D307/54

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: (I); (II). Intermediates (V) are also claimed.

公开(公告)号：US10221162B2

公开(公告)日：2019-03-05

申请号：US16033632

申请日：2018-07-12

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

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：US09988369B2

公开(公告)日：2018-06-05

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

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.

公开(公告)号：US09745286B2

公开(公告)日：2017-08-29

申请号：US15297487

申请日：2016-10-19

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 B. 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 ,  A61K31/501 ,  A61K31/444 ,  A61K31/506 ,  A61K31/497 ,  C07D401/14 ,  A61K31/437 ,  A61K31/513 ,  A61K31/695 ,  A61K45/06 ,  C07B57/00 ,  C07B59/00 ,  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 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

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：US09656997B2

公开(公告)日：2017-05-23

申请号：US15297940

申请日：2016-10-19

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Xiaoqi Chen ,  Alan C. Cheng ,  Richard V. Connors ,  Jeffrey Deignan ,  Paul John Dransfield ,  Xiaohui Du ,  Zice Fu ,  Julie Anne Heath ,  Daniel B. Horne ,  Jonathan Houze ,  Matthew R. Kaller ,  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 ,  Mikkel V. Debenedetto ,  Robert P. Farrell ,  Simon J. Hedley ,  Ted C. Judd ,  Frank Kayser

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

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：US20170042897A1

公开(公告)日：2017-02-16

申请号：US15298686

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 B. 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: A61K31/506 ,  C07D213/82 ,  A61K31/497 ,  C07D241/24 ,  C07D401/12 ,  A61K45/06 ,  A61K31/4439

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：US20140315895A1

公开(公告)日：2014-10-23

申请号：US14316586

申请日：2014-06-26

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 ,  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 ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

IPC: C07D279/02

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。