Vertex Pharmaceuticals, Inc.

Alios Biopharma, Inc.

William Aloysius Nugent

Gerald J Tanoury

Young Chun Jung

Peter Jamison Rose

Benjamin Joseph Littler

Robert Michael Hughes

Ales Medek

Michael Waldo

Lori Ann Ferris

Praveen Mudunuri

Cristian Harrison

Anuj K Kuldipkumar

David Richard Willcox

Vadims Dvornikovs

John R Studley

David Andrew Siesel

Paul Angell

David Smith

Berenice Lewandowski

Adam R Looker

Vito Melillo

Elaine Chungmin Lee

Daniel T Belmont

Raymond E Forslund

Theodore A Martinot

Shereen Ibrahim

The disclosure provides processes for preparing a compound of Formula (I). 

Processes for making modulators of cystic fibrosis transmembrane conductance regulator

Processes for preparing 5,5-dimethyl-3-methylenepyrrolidin-2-one, (S)-3,5,5-trimethylpyrrolidine-2-one, (R)-3,5,5-trimethylpyrrolidine-2-one, (S)-2,4,4-trimethylpyrrolidine, and (R)-2,4,4-trimethylpyrrolidine, and their salt forms are disclosed. 

Processes for preparing pyrrolidine compounds

A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.

Methods of preparing inhibitors of influenza viruses replication

The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.

Process of producing cycloalkylcarboxamido-indole compounds

The present application relates to solid state forms, for example, crystalline forms of 2'-C-methyluridine-5&#x2032;-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.

Solid forms of a thiophosphoramidate nucleotide prodrug

The present application relates to solid state forms, for example, crystalline forms of 2'-C-methyluridine-5&#x2032;-(O-phenyl-N&#x2014;(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N&#x2014;(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N&#x2014;(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2&#x2032;-C-methyluridine-5&#x2032;-(O-phenyl-N&#x2014;(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.

The invention provides &#x3b2;-sulfonamide &#x3b1;-keto esters and amides in which the &#x3b1;-keto is protected as a 1,3-dithiolane derivative. Also provided are methods for preparing such esters and amides and for incorporating them into peptides.

Preparation of protected alpha-keto beta-amino esters and amides

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Manomet, MA, United States of America

William Aloysius Nugent