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公开(公告)号：US10759785B2
公开(公告)日：2020-09-01
申请号：US16312158
申请日：2017-06-21
发明人： Clive McCarthy , Jonathan David Hargrave , Duncan Alexander Hay , Thomas Beauregard Schofield , Naomi Went
IPC分类号： C07D403/12 , C07D403/14 , C07D401/14 , C07D405/14
摘要： The invention relates to compounds of general formula (I): wherein R1, R2, R3, R10 and X− are as defined herein. The compounds are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions.
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![Bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives as ENaC inhibitors for treating respiratory diseases](/abs-image/US/2022/06/28/US11370778B2/abs.jpg.150x150.jpg)
公开(公告)号：US11370778B2
公开(公告)日：2022-06-28
申请号：US16756416
申请日：2018-10-17
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , A61P11/00 , A61K45/06
摘要： The present invention discloses bis(pentahydroxyhexyl)amino substituted 2-{[(3-amino-pyrazin-2-yl)formamido]methyl}-1H-1,3-benzodiazol-3-ium derivatives of formula (I) as inhibitors of ENaC and are of use in the treatment of respiratory diseases and conditions, skin conditions or ocular conditions, wherein the respiratory disease or condition is e.g. cystic fibrosis, chronic obstructive pulmonary disease (COPD), chronic bronchitis, emphysema, bronchiectasis, including non-cystic fibrosis bronchiectasis, and asthma; the skin condition is e.g. psoriasis, atopic dermatitis and ichthyosis; and the ocular condition is e.g. dry eye disease.
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公开(公告)号：US10941149B2
公开(公告)日：2021-03-09
申请号：US16462794
申请日：2017-11-22
发明人： Clive McCarthy , Jonathan David Hargrave , Duncan Alexander Hay , Thomas Beauregard Schofield , Naomi Went
IPC分类号： A61K31/4985 , C07D487/04 , A61P11/12 , A61K9/00 , A61K45/06
摘要： Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
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公开(公告)号：US12037336B2
公开(公告)日：2024-07-16
申请号：US17056370
申请日：2019-05-17
IPC分类号： C07D487/04 , A61K45/06 , C07C53/06 , C07C53/18 , C07D235/08 , C07D401/12
CPC分类号： C07D487/04 , A61K45/06 , C07C53/06 , C07C53/18 , C07D235/08 , C07D401/12
摘要： Compounds of general formula (I) wherein R1, R2, R3, R4 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
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公开(公告)号：US11739094B2
公开(公告)日：2023-08-29
申请号：US17103559
申请日：2020-11-24
发明人： Clive McCarthy , Jonathan David Hargrave , Duncan Alexander Hay , Thomas Beauregard Schofield , Naomi Went
IPC分类号： C07D487/04 , A61P11/12 , A61K9/00 , A61K45/06
CPC分类号： C07D487/04 , A61K9/007 , A61P11/12 , A61K45/06
摘要： Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
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