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公开(公告)号：US20190016728A1
公开(公告)日：2019-01-17
申请号：US16132960
申请日：2018-09-17
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
CPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US20190330219A1
公开(公告)日：2019-10-31
申请号：US16506883
申请日：2019-07-09
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US10377762B2
公开(公告)日：2019-08-13
申请号：US16132960
申请日：2018-09-17
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US20210171534A1
公开(公告)日：2021-06-10
申请号：US17179062
申请日：2021-02-18
发明人： 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
IPC分类号： C07D487/04 , A61P11/12 , A61K31/519 , A61K45/06
摘要： 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.
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公开(公告)号：US10131670B2
公开(公告)日：2018-11-20
申请号：US15841902
申请日：2017-12-14
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US20230250100A1
公开(公告)日：2023-08-10
申请号：US18134455
申请日：2023-04-13
发明人： 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
IPC分类号： C07D487/04 , A61P11/12 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61P11/12 , A61K31/519 , A61K45/06
摘要： 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.-
公开(公告)号：US10301315B2
公开(公告)日：2019-05-28
申请号：US15815809
申请日：2017-11-17
发明人： 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
IPC分类号： A61K31/519 , C07D487/04 , A61K45/06
摘要： The present invention relates to 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.
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公开(公告)号：US10208053B2
公开(公告)日：2019-02-19
申请号：US16132894
申请日：2018-09-17
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US20190016727A1
公开(公告)日：2019-01-17
申请号：US16132894
申请日：2018-09-17
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjögren's Syndrome, and other CFTR associated disorders.
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公开(公告)号：US20180170938A1
公开(公告)日：2018-06-21
申请号：US15841902
申请日：2017-12-14
发明人： Joseph Walter Strohbach , David Christopher Limburg , John Paul Mathias , Atli Thorarensen , John James Mousseau , Rajiah Aldrin Denny , Christoph Wolfgang Zapf , Ivan Viktorovich Efremov
IPC分类号： C07D487/04 , A61P11/00
CPC分类号： C07D487/04 , A61P11/00
摘要： 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, Sjôgren's Syndrome, and other CFTR associated disorders.
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