公开(公告)号：US20240360079A1

公开(公告)日：2024-10-31

申请号：US18291285

申请日：2022-08-17

Applicant: AMGEN INC.

Inventor： Adrian ORTIZ ,  Jaika DOERFLER ,  Karina R. VAIDA

IPC: C07C319/12 ,  C07C321/26 ,  C12P13/00

CPC classification number: C07C319/12 ,  C07C321/26 ,  C12P13/001

Abstract: The present invention relates to precious metal (Pd/Pt/Rh/Ru) free, preferably Pd free, processes for preparing a compound having formula (1) wherein: R1, R2, and X are as defined in the specification, or a salt thereof. Preferably, the compound is an iodo acrylate compound.

公开(公告)号：US20180369226A1

公开(公告)日：2018-12-27

申请号：US16062602

申请日：2016-12-19

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Thomas DINEEN ,  Karina R. VAIDA

IPC: A61K31/4704 ,  A61K31/501 ,  A61P11/14 ,  A61P29/02

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, cough, and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

公开(公告)号：US20160046626A1

公开(公告)日：2016-02-18

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: C07D471/04 ,  C07D417/12 ,  C07D413/14 ,  C07D413/12 ,  C07D401/12

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。