公开(公告)号：US09776995B2

公开(公告)日：2017-10-03

申请号：US14898070

申请日：2014-06-11

Applicant: AMGEN INC.

Inventor： Matthew Weiss ,  Erin F. DiMauro ,  Thomas Dineen ,  Russell Graceffa ,  Angel Guzman-Perez ,  Hongbing Huang ,  Charles Kreiman ,  Isaac E. Marx ,  Hanh Nho Nguyen ,  Emily Anne Peterson ,  Holly L. Deak

IPC: C07D417/14 ,  C07D471/04 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14 ,  C07D417/12 ,  C07C53/18 ,  C07D215/227 ,  C07D403/12 ,  C07D215/36 ,  C07D241/44 ,  C07D401/14

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

公开(公告)号：US10906890B2

公开(公告)日：2021-02-02

申请号：US16347955

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： Ning Chen ,  Yinhong Chen ,  Mikkel V. Debenedetto ,  Paul John Dransfield ,  James S. Harvey ,  Julie Anne Heath ,  Jonathan Houze ,  Aarif Yusuf Khakoo ,  Su-Jen Lai ,  Zhihua Ma ,  Nobuko Nishimura ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Wen-Chen Yeh ,  Charles Kreiman

IPC: C07D403/14 ,  C07D239/24 ,  C07D241/12 ,  C07D249/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D239/26 ,  A61P9/04 ,  C07D401/14

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: (I), (II) where the definitions of the variables are provided herein.

公开(公告)号：US09458152B2

公开(公告)日：2016-10-04

申请号：US14920833

申请日：2015-10-22

Applicant: AMGEN INC.

Inventor： Matthew Weiss ,  Alessandro Boezio ,  Christiane Boezio ,  John R. Butler ,  Margaret Yuhua Chu-Moyer ,  Erin F. Dimauro ,  Thomas Dineen ,  Russell Graceffa ,  Angel Guzman-Perez ,  Hongbing Huang ,  Charles Kreiman ,  Daniel La ,  Isaac E. Marx ,  Benjamin Charles Milgram ,  Hanh Nho Nguyen ,  Emily Anne Peterson ,  Karina R. Vaida ,  Brian Sparling

IPC: A61K31/00 ,  C07D417/14 ,  C07D471/04 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14 ,  C07D417/12 ,  C07C53/18 ,  C07D215/227 ,  C07D403/12 ,  C07D215/36 ,  C07D241/44 ,  C07D401/14

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

公开(公告)号：US09051311B2

公开(公告)日：2015-06-09

申请号：US14383880

申请日：2013-03-07

Applicant: AMGEN INC.

Inventor： Thomas Dineen ,  Charles Kreiman ,  Matthew Weiss ,  Stephanie Geuns-Meyer

IPC: C07D401/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/47 ,  C07D417/14

CPC classification number: C07D417/12 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav 1.7。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。

公开(公告)号：US20150018352A1

公开(公告)日：2015-01-15

申请号：US14383880

申请日：2013-03-07

Applicant: AMGEN INC.

Inventor： Thomas Dineen ,  Charles Kreiman ,  Matthew Weiss ,  Stephanie Geuns-Meyer

IPC: C07D417/12 ,  C07D401/14 ,  C07D471/04 ,  C07D417/14

CPC classification number: C07D417/12 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav 1.7。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。

公开(公告)号：US10689367B2

公开(公告)日：2020-06-23

申请号：US16347970

申请日：2017-11-03

Applicant: AMGEN INC.

Inventor： Yinhong Chen ,  Alan C. Cheng ,  Mikkel V. Debenedetto ,  Paul John Dransfield ,  James S. Harvey ,  Jonathan Houze ,  Aarif Yusuf Khakoo ,  Su-Jen Lai ,  Zhihua Ma ,  Vatee Pattaropong ,  Gayathri Swaminath ,  Charles Kreiman ,  David C. Moebius ,  Ankit Sharma

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61P9/04 ,  C07D417/14 ,  A61K45/06 ,  C07D401/12

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 structures where the definitions of the variables are provided herein.

公开(公告)号：US09212182B2

公开(公告)日：2015-12-15

申请号：US14302337

申请日：2014-06-11

Applicant: AMGEN INC.

Inventor： Matthew Weiss ,  Alessandro Boezio ,  Christiane Boezio ,  John R. Butler ,  Margaret Yuhua Chu-Moyer ,  Erin F. Dimauro ,  Thomas Dineen ,  Russell Graceffa ,  Angel Guzman-Perez ,  Hongbing Huang ,  Charles Kreiman ,  Daniel La ,  Isaac E. Marx ,  Benjamin Charles Milgrim ,  Hanh Nho Nguyen ,  Emily Peterson ,  Karina Romero ,  Brian Sparling

IPC: A61K31/00 ,  C07D215/00 ,  C07D471/04 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14 ,  C07D417/12 ,  C07C53/18 ,  C07D215/227 ,  C07D403/12 ,  C07D215/36 ,  C07D241/44

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗与钠通道活性相关的疾病，例如疼痛障碍和瘙痒。 还提供含有本发明化合物的药物组合物。

公开(公告)号：US09012443B2

公开(公告)日：2015-04-21

申请号：US13707096

申请日：2012-12-06

Applicant: Amgen Inc.

Inventor： Christiane Boezio ,  Howard Bregman ,  James R. Coats ,  Erin F. Dimauro ,  Thomas Dineen ,  Bingfan Du ,  Russell Graceffa ,  Charles Kreiman ,  Daniel La ,  Isaac E. Marx ,  Nagasree Chakka ,  Hanh Nho Nguyen ,  Emily Anne Peterson ,  Matthew Weiss ,  Katrina W. Copeland ,  Holly L. Deak ,  Alessandro Boezio

IPC: C07D498/04 ,  C07D417/12 ,  C07D417/14 ,  C07D401/14 ,  C07D471/04 ,  A61K31/433 ,  C07D403/12 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D239/42 ,  C07D409/14 ,  C07D413/12 ,  C07D277/52 ,  C07D285/08

CPC classification number: C07D498/04 ,  C07D239/42 ,  C07D277/52 ,  C07D285/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav 1.7。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。