Patent number: 12612409
Abstract: The present invention relates to methods of using compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, 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, Sjögren's Syndrome, and other CFTR associated disorders.
Type:
Grant
Filed:
April 13, 2023
Date of Patent:
April 28, 2026
Assignee:
Cystic Fibrosis Foundation
Inventors:
Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov
Publication number: 20240124450
Abstract: A compound of formula I having the structure: or a pharmaceutically acceptable salt thereof, wherein A1 and A2 are independently O or S; X is selected from CH2, CD2, NR3, O, and S, where R3 is selected from hydrogen, C1-C4 linear or branched chain alkyl, halo(C1-C4)linear or branched chain alkyl, and hydroxyl(C1-C4)linear or branched chain alkyl; Y and Z are selected from C and N, where when Y is C, then Z is N, and when Y is N, then Z is C; R1 and R2 are independently selected from hydrogen, deuterium, C1-C4 linear or branched chain alkyl, etc.; or a C1-C2 alkyl substituted with a C3-C5 cycloalkyl ring; or taken together to form a C3-C6 cycloalkyl ring; or where X is CH2 or CD2, then R1 and R2 are independently selected from hydrogen, deuterium, halogen, hydroxyl, C1-C4 linear or branched chain alkyl, etc.; R4 is selected from hydrogen, deuterium, cyano, halogen, (C1-C3) alkoxy, etc.; R5 is selected from hydrogen, deuterium, halogen, C1-C3 alkoxy, amino, (C1-C4 linear or branched chain alkyl)amino, etc.
Type:
Application
Filed:
September 13, 2023
Publication date:
April 18, 2024
Applicant:
Pfizer Inc.
Inventors:
Andrea Nicole Bootsma, David Christopher Ebner, Daniel Wei-Shung Kung, Matthew Alexander Perry, Daniel Copley Schmitt, Joseph Walter Strohbach, Atli Thorarensen
Publication number: 20230250100
Abstract: The present invention relates to methods of using compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, 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, Sjögren's Syndrome, and other CFTR associated disorders.
Type:
Application
Filed:
April 13, 2023
Publication date:
August 10, 2023
Inventors:
Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov
Publication number: 20210171534
Abstract: The present invention relates to methods of using compounds of Formula I, wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, 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, Sjögren's Syndrome, and other CFTR associated disorders.
Type:
Application
Filed:
February 18, 2021
Publication date:
June 10, 2021
Inventors:
Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Daniel Elbaum, Lori Krim Gavrin, Ivan Viktorovich Efremov