Amgen Inc.

Alan H Cherney

Isaac E Marx

Benjamin Charles Milgram

Sheng Cui

Liang Huang

Haoxuan Wang

John Stellwagen

Jason S Tedrow

Robert Ronald Milburn

Austin G Smith

Philipp C Roosen

Oliver Thiel

Matthew G Beaver

John T Colyer

Wei Zhao

Kyle D Baucom

Gabrielle St-pierre

Rahul P Sangodkar

Michael A Lovette

Ari Ericson

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.

Ring closing synthesis of macrocyclic MCL-1 inhibitor intermediates

The present invention provides a cyclobutyl dihydroquinoline sulfonamide 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.

Cyclobutyl dihydroquinoline sulfonamide compounds

The present invention provides a compound of Formula (I):

Cyclopropyl dihydroquinoline sulfonamide compounds

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Somerville, MA, United States of America

Alan H Cherney