Cystic Fibrosis Foundation Therapeutics, Inc.

Cystic Fibrosis Foundation

Pfizer Corporation

David Christopher Limburg

Joseph Walter Strohbach

John Paul Mathias

Atli Thorarensen

Christoph Wolfgang Zapf

Rajiah Aldrin Denny

Ivan Viktorovich Efremov

John James Mousseau

Lori Krim Gavrin

Daniel Elbaum

Tsutomu Akama

Peter M Jones

Robert Toms Jacobs

Yasheen Zhou

Jacob J Plattner

Thean Yeoh

David Clive Blakemore

James John Mousseau

Matthew Alexander Perry

Martins Sunday Oderinde

Rubben Federico Torella

Thean Yeow Yeoh

Jacob John Plattner

The present invention relates to boron containing compounds of Formula (IA): that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.

Substituted 1,2-oxaborolan-2-ols as PDE4 inhibitors

The present invention relates to 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sj&#xf6;gren's Syndrome, and other CFTR associated disorders.

Bicyclic heteroaryl derivatives as CFTR potentiators

The present invention relates to methods of using compounds of Formula I, 

Pyrrolopyrimidines as CFTR potentiators

The present invention relates to compounds of Formula I, 

The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sj&#xf6;gren's Syndrome, and other CFTR associated disorders.

The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives, 5,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives or 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sj&#xf6;gren's Syndrome, and other CFTR associated disorders.

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Salem, CT, United States of America

David Christopher Limburg