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：US09636418B2

公开(公告)日：2017-05-02

申请号：US14207445

申请日：2014-03-12

Applicant: AMGEN INC.

Inventor： Justin K. Murray ,  Jerry Ryan Holder ,  Malgorzata Wanska ,  Christopher M. Tegley ,  James R. Falsey ,  Elizabeth M. Doherty ,  Leslie P. Miranda

IPC: C07K14/435 ,  A61K47/48 ,  C07K16/44 ,  C07K14/705 ,  A61K38/00

CPC classification number: A61K47/48438 ,  A61K38/00 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K14/43518 ,  C07K14/705 ,  C07K16/44

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

公开(公告)号：US10344060B2

公开(公告)日：2019-07-09

申请号：US14773756

申请日：2014-03-12

Applicant: AMGEN INC.

Inventor： Justin K. Murray ,  Jerry Ryan Holder ,  Malgorzata Wanska ,  Christopher M. Tegley ,  James R. Falsey ,  Elizabeth M. Doherty ,  Leslie P. Miranda ,  Kaustav Biswas ,  Bin Wu ,  Kelvin Sham ,  Jason C. Long

IPC: C07K14/00 ,  C07K14/435 ,  C07K16/00 ,  C07K19/00 ,  C07K14/46 ,  C07K14/47 ,  A61K38/00 ,  A61K38/16 ,  A61K38/17 ,  A61K47/64 ,  A61K47/68

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

公开(公告)号：US20140235629A1

公开(公告)日：2014-08-21

申请号：US14347628

申请日：2012-09-26

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Brian M. Fox ,  Jiasheng Fu ,  Ana Gonzalez Buenrostro ,  Felix Gonzalez Lopez De Turiso ,  Darin J. Gustin ,  Julie A. Heath ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  Yihong Li ,  Zhihong Li ,  Zhihua Ma ,  Joel Micintosh ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Michael J. Schmitt ,  Daqing Sun ,  Xiaodong Wang ,  Malgorzata Wanska ,  Christine Weathers ,  Xuelei Yan

IPC: C07D413/04 ,  C07D265/32 ,  C07D413/10 ,  C07D417/04

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：US11046680B1

公开(公告)日：2021-06-29

申请号：US16347910

申请日：2017-11-03

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 ,  James S. Harvey ,  Julie Anne Heath ,  Lars V. Heumann ,  Daniel B. Horne ,  Jonathan Houze ,  Matthew R. Kaller ,  Frank Kayser ,  Aarif Yusuf Khakoo ,  David J. Kopecky ,  Su-Jen Lai ,  Zhihua Ma ,  Julio C. Medina ,  Jeffrey T. Mihalic ,  Nobuko Nishimura ,  Steven H. Olson ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Xiaodong Wang ,  Malgorzata Wanska ,  Kevin Yang ,  Wen-Chen Yeh

IPC: C07D417/14 ,  A61P9/00 ,  C07D401/14 ,  C07D403/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

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：US09376425B2

公开(公告)日：2016-06-28

申请号：US14347628

申请日：2012-09-26

Applicant: AMGEN INC.

Inventor： Michael D. Bartberger ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette ,  John Eksterowicz ,  Brian M. Fox ,  Jiasheng Fu ,  Ana Gonzalez Buenrostro ,  Felix Gonzalez Lopez De Turiso ,  Darin J. Gustin ,  Julie A. Heath ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  Yihong Li ,  Zhihong Li ,  Zhihua Ma ,  Joel McIntosh ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yosup Rew ,  Philip M. Roveto ,  Michael J. Schmitt ,  Daqing Sun ,  Xiaodong Wang ,  Malgorzata Wanska ,  Christine Weathers ,  Xuelei Yan

IPC: C07D265/06 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D413/12 ,  C07D265/32

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。