Incyte Corporation

Xenon Pharmaceuticals Inc.

Joseph A Sclafani

Jiacheng Zhou

Bo Shen

Zhongjiang Jia

Osama Suleiman

Dengjin Wang

Daniel Carper

Robert Wilson

Mark Wright

Daniel Levy

Yi Wang

Ronen Ben-David

Michael A Christie

Linli He

Orel Yosef Mizrahi

Jian Chen

Harlan F Reese

Mina Gadelrab Dimitri

Graciela Noemi Gershon

Nelson G Landmesser

Partha S Mudipalli

This application relates to processes and intermediates for the preparation of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3'-((2-(difluoromethyl)-7-((3-hydroxypyrrolidin-1-yl)methyl)pyrido[3,2-d]pyrimidin-4-yl)amino)-2,2′-dimethyl-[1,1′-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)piperidine-4-carboxylic acid, and salts and crystalline forms thereof, where the PD-1/PD-L1 inhibitor and solid forms and salt forms thereof are useful in the treatment of various diseases including infectious diseases and cancer.

Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof

This application relates to processes and intermediates for the preparation of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-((2-(difluoromethyl)-7-((3-hydroxypyrrolidin-1-yl)methyl)pyrido[3,2-d]pyrimidin-4-yl)amino)-2,2′-dimethyl-[1,1′-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)piperidine-4-carboxylic acid, and salts and crystalline forms thereof, where the PD-1/PD-L1 inhibitor and solid forms and salt forms thereof are useful in the treatment of various diseases including infectious diseases and cancer.

This invention is directed to asymmetric synthesis of funapide, which is useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Asymmetric synthesis of funapide

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Malvern, PA, United States of America

Joseph A Sclafani