公开(公告)号：US20230167130A1

公开(公告)日：2023-06-01

申请号：US17922619

申请日：2021-05-05

Applicant: AMGEN INC.

Inventor： Austin G. SMITH ,  Jason S. TEDROW ,  Gabrielle ST-PIERRE ,  Oliver Ralf THIEL ,  Liang HUANG ,  Philipp C. ROOSEN ,  John T. COLYER ,  Kyle D. BAUCOM ,  Ari ERICSON ,  Matthew G. BEAVER ,  Rahul P. SANGODKAR ,  Michael A. LOVETTE ,  Robert Ronald MILBURN ,  Alan H. CHERNEY ,  Sheng CUI

IPC: C07D513/10 ,  C07D267/16

CPC classification number: C07D513/10 ,  C07D267/16

Abstract: Provided herein are processes for synthesizing Mcl-1 inhibitors and intermediates such as compound F that can be used to prepare them where the variable PG is as defined herein. In particular, provided herein are processes for synthesizing compound A1, and salts or solvates thereof and compound A2, and salts and solvates thereof.

公开(公告)号：US20210387977A1

公开(公告)日：2021-12-16

申请号：US17344939

申请日：2021-06-10

Applicant: AMGEN INC.

Inventor： BENJAMIN C. MILGRAM ,  Isaac E. MARX ,  John STELLWAGEN ,  Wei ZHAO ,  Alan H. CHERNEY

IPC: C07D413/12

Abstract: The present invention provides a compound of Formula (I): an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits 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 the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.