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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：US20180141954A1
公开(公告)日：2018-05-24
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： C07D487/04 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , 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：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：US08513242B2
公开(公告)日：2013-08-20
申请号：US13139009
申请日：2009-12-11
申请人： Phoebe Chiang , Shomir Ghosh
发明人： Phoebe Chiang , Shomir Ghosh
IPC分类号： A61K31/535 , A61K31/505
CPC分类号： C07D403/14 , C07D239/12 , C07D239/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D413/04
摘要： Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
摘要翻译： 本文公开了被认为是囊性纤维化跨膜调节剂（CFTR）的调节剂的嘧啶基化合物及其制备和使用方法。 还提供了治疗与囊性纤维化跨膜调节剂相关的病症的药物组合物和方法，例如气道炎症，囊性纤维变性等。
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公开(公告)号：US08334292B1
公开(公告)日：2012-12-18
申请号：US13159689
申请日：2011-06-14
申请人： Phoebe Chiang
发明人： Phoebe Chiang
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D405/12 , C07D405/14
摘要： Disclosed herein are pyrimidinyl compounds that are contemplated to be modulators of cystic fibrosis transmembrane regulators (CFTR), and methods of making and using same. Also provided are pharmaceutical compositions and methods of treating disorders associated with cystic fibrosis transmembrane regulators, such as airway inflammation, cystic fibrosis, and the like.
摘要翻译： 本文公开了被认为是囊性纤维化跨膜调节剂（CFTR）的调节剂的嘧啶基化合物及其制备和使用方法。 还提供了治疗与囊性纤维化跨膜调节剂相关的病症的药物组合物和方法，例如气道炎症，囊性纤维变性等。
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公开(公告)号：US20100196344A1
公开(公告)日：2010-08-05
申请号：US12754183
申请日：2010-04-05
CPC分类号： A61K38/46 , A61K38/47 , A61K38/48 , A61K2300/00
摘要： The present invention relates to compositions for the treatment of conditions, including pancreatic insufficiency. The compositions of the present invention comprise lipase, protease and amylase in a particular ratio that provides beneficial results in patients, such as those afflicted with pancreatic insufficiency. This invention also relates to methods using such compositions for the treatment of pancreatic insufficiency.
摘要翻译： 本发明涉及用于治疗包括胰腺功能不全的病症的组合物。 本发明的组合物以特定的比率包含脂肪酶，蛋白酶和淀粉酶，这在患者（例如患有胰腺功能不全的患者）中提供有益的结果。 本发明还涉及使用这种组合物治疗胰腺功能不全的方法。
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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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