公开(公告)号：WO2017192485A1

公开(公告)日：2017-11-09

申请号：PCT/US2017/030501

申请日：2017-05-02

Applicant: AMGEN INC.

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

IPC: C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D471/04 ,  A61K31/4196 ,  A61P9/00

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.

Abstract translation: 式I和式II的化合物，其药学上可接受的盐，任何前述的立体异构体或其混合物是APJ受体的激动剂，并且可用于治疗心血管和其他病症。 式I和式II的化合物具有以下结构：其中变量的定义在本文中提供。

公开(公告)号：WO2016187308A1

公开(公告)日：2016-11-24

申请号：PCT/US2016/033088

申请日：2016-05-18

Applicant: AMGEN INC.

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

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  A61K31/4196 ,  A61K31/4439 ,  A61P9/00

CPC classification number: C07D401/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  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 ,  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.

Abstract translation: 式I和式II的化合物，其药学上可接受的盐，前述任何一种的立体异构体或其混合物是APJ受体的激动剂，并且可用于治疗心血管和其它病症。 式I和式II的化合物具有以下结构，其中本文提供变量的定义。

公开(公告)号：WO2013049250A1

公开(公告)日：2013-04-04

申请号：PCT/US2012/057389

申请日：2012-09-26

Applicant: AMGEN INC. ,  BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

Inventor： BARTBERGER, Michael D. ,  BECK, Hilary Plake ,  CHEN, Xiaoqi ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DUQUETTE, Jason A. ,  EKSTEROWICZ, John ,  FOX, Brian M. ,  FU, Jiasheng ,  GONZALEZ BUENROSTRO, Ana ,  GONZALEZ LOPEZ DE TURISO, Felix ,  GUSTIN, Darin J. ,  HEATH, Julie A. ,  JOHNSON, Michael G. ,  KAYSER, Frank ,  KOPECKY, David J. ,  LI, Yihong ,  LI, Zhihong ,  MA, Zhihua ,  MCINTOSH, Joel ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  REW, Yosup ,  ROVETO, Philip M. ,  SCHMITT, Michael J. ,  SUN, Daqing ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  WEATHERS, Christine ,  YAN, Xuelei

IPC: C07D265/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D413/12

CPC classification number: C07D413/04 ,  C07D265/06 ,  C07D265/32 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, 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.

Abstract translation: 本发明提供式I或II的MDM2抑制剂化合物或其药学上可接受的盐，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：WO2018097945A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/059824

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： CHEN, Ning ,  CHEN, Xiaoqi ,  CHEN, Yinhong ,  CHENG, Alan C. ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DRANSFIELD, Paul John ,  DU, Xiaohui ,  FU, Zice ,  HARVEY, James S. ,  HEATH, Julie Anne ,  HEUMANN, Lars V. ,  HORNE, Daniel B. ,  HOUZE, Jonathan ,  KALLER, Matthew R. ,  KAYSER, Frank ,  KHAKOO, Aarif Yusuf ,  KOPECKY, David J. ,  LAI, Su-Jen ,  MA, Zhihua ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  NISHIMURA, Nobuko ,  OLSON, Steven H. ,  PATTAROPONG, Vatee ,  SWAMINATH, Gayathri ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  YANG, Kevin ,  YEH, Wen-Chen

IPC: C07D401/14 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  A61K31/341 ,  A61K31/4196 ,  A61P9/00 ,  A61P9/02

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 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：WO2018097944A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/059822

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： BROWN, Matthew ,  CHEN, Ning ,  CHEN, Xiaoqi ,  CHEN, Yinhong ,  CHENG, Alan C. ,  CONNORS, Richard V. ,  DEIGNAN, Jeffrey ,  DRANSFIELD, Paul John ,  DU, Xiaohui ,  FU, Zice ,  HARVEY, James S. ,  HEATH, Julie Anne ,  HEUMANN, Lars V. ,  HOUZE, Jonathan ,  KAYSER, Frank ,  KHAKOO, Aarif Yusuf ,  KOPECKY, David J. ,  LAI, Su-Jen ,  MA, Zhihua ,  MEDINA, Julio C. ,  MIHALIC, Jeffrey T. ,  OLSON, Steven H. ,  PATTAROPONG, Vatee ,  SWAMINATH, Gayathri ,  WANG, Xiaodong ,  WANSKA, Malgorzata ,  YEH, Wen-Chen

IPC: C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  A61K31/341 ,  A61K31/4196 ,  A61P9/02 ,  A61P9/00

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：EP3300500A1

公开(公告)日：2018-04-04

申请号：EP16730076.3

申请日：2016-05-18

Applicant: Amgen Inc.

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

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  A61K31/4196 ,  A61K31/4439 ,  A61P9/00

CPC classification number: C07D401/14 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  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 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F7/08

Abstract: where the definitions of the variables are provided herein.

公开(公告)号：EP3452466A1

公开(公告)日：2019-03-13

申请号：EP17733197.2

申请日：2017-05-02

Applicant: Amgen Inc.

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

IPC: C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D471/04 ,  A61K31/4196 ,  A61P9/00