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公开(公告)号：US20210163524A1
公开(公告)日：2021-06-03
申请号：US16636596
申请日：2018-08-06
申请人： Ardelyx, Inc.
发明人： Gary Luehr , Dean Dragoli , Michael Leadbetter , Tao Chen , Jason Lewis
摘要： The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.
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公开(公告)号：US20230273354A1
公开(公告)日：2023-08-31
申请号：US18101009
申请日：2023-01-24
申请人： Ardelyx, Inc.
发明人： Gary Luehr , Dean Dragoli , Michael Leadbetter , Tao Chen , Jason Lewis
CPC分类号： G02B5/0294 , G02B5/201 , G02B3/0056 , G02F1/133502 , G02B5/0215 , G02B27/0018 , A61P5/44 , C07J63/008 , G02B5/021 , G02B2207/123 , G02F1/133526
摘要： The present invention provides a compound of formula (I) or a salt thereof:
wherein X, L, V, R1, R2, R3 and R4, are as defined herein.-
公开(公告)号：US20220106354A1
公开(公告)日：2022-04-07
申请号：US17429599
申请日：2020-02-06
申请人： ARDELYX, INC.
发明人： Dean Dragoli , Gary Leuhr , Tao Chen , Jason Lewis , Michael Leadbetter
摘要： The present invention provides a compound of formula (I) or a salt thereof: (Formula (I)) wherein X, L, V, R1; R2, R3 and R4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.
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公开(公告)号：US11242337B2
公开(公告)日：2022-02-08
申请号：US16476836
申请日：2018-01-09
申请人： Ardelyx, Inc.
发明人： Dean Dragoli , Irina Dotsenko , Jason Lewis
IPC分类号： C07D403/14 , A61K47/55 , A61P1/10 , A61P9/12 , A61P1/00 , A61P9/04 , A61P29/00 , A61P3/12 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D487/08
摘要： The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
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公开(公告)号：US12084472B2
公开(公告)日：2024-09-10
申请号：US17185653
申请日：2021-02-25
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Michael Robert Leadbetter , Jeremy Caldwell , Dean Dragoli , Noah Bell , Jeffrey W. Jacobs , Patricia Finn , Rakesh Jain , Tao Chen , Matthew Siegel
IPC分类号： A61K31/444 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K31/706 , A61K45/06 , C07B59/00 , C07C409/12 , C07D213/30 , C07D213/38 , C07D213/80 , C07D213/81 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07H15/04 , C07H15/18 , C07H15/234 , C07H15/26
CPC分类号： C07H15/26 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K31/553 , A61K31/706 , A61K45/06 , C07B59/002 , C07C409/12 , C07D213/30 , C07D213/38 , C07D213/80 , C07D213/81 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/08 , C07H15/04 , C07H15/18 , C07H15/234 , C07B2200/05
摘要： The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula:
where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.-
公开(公告)号：US20220306672A1
公开(公告)日：2022-09-29
申请号：US17185653
申请日：2021-02-25
申请人： Ardelyx, Inc.
发明人： Jason G. Lewis , Michael Robert Leadbetter , Jeremy Caldwell , Dean Dragoli , Noah Bell , Jeffrey W. Jacobs , Patricia Finn , Rakesh Jain , Tao Chen , Matthew Siegel
IPC分类号： C07H15/26 , A61K31/4418 , C07D213/38 , A61K31/4427 , C07D405/12 , A61K31/443 , A61K31/444 , C07D213/30 , C07D405/04 , A61K31/4433 , A61K31/4439 , C07D413/12 , A61K31/553 , A61K31/496 , A61K31/706 , C07H15/04 , C07H15/18 , C07D401/12 , A61K31/5377 , C07H15/234 , A61K31/4436 , C07D409/12 , A61K31/4545 , A61K31/506 , A61K31/4425 , A61K31/551 , C07D471/04 , C07B59/00 , C07D213/81 , C07D213/80 , C07D487/08 , A61K45/06 , C07C409/12
摘要： The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, diabetes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.
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公开(公告)号：US10376481B2
公开(公告)日：2019-08-13
申请号：US15402213
申请日：2017-01-09
申请人： ARDELYX, INC
发明人： Noah Bell , Christopher Carreras , Michael Robert Leadbetter , Jason Gustaf Lewis , Jeffrey W. Jacobs , Irina Dotsenko , Dean Dragoli , Ying He , Andrew King , Matthew Siegel
IPC分类号： A61K31/17 , A61K31/4545 , A61K31/25 , A61K31/18 , A61K31/167 , A61K31/03 , A61K31/10 , A61K31/015 , A61K31/40 , A61K31/4453
摘要： The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
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公开(公告)号：US20240209019A1
公开(公告)日：2024-06-27
申请号：US18518267
申请日：2023-11-22
申请人： ARDELYX, INC.
发明人： Dean Dragoli , Gary Luehr , Tao Chen , Jason Lewis , Michael Leadbetter
CPC分类号： C07J63/008 , A61K31/56 , A61K31/58 , A61P3/12 , A61P5/40
摘要： The present invention provides a compound of formula (I) or a salt thereof:
wherein X, L, V, R1, R2, R3 and R4, are as defined herein.-
公开(公告)号：US11858959B2
公开(公告)日：2024-01-02
申请号：US17429599
申请日：2020-02-06
申请人： ARDELYX, INC.
发明人： Dean Dragoli , Gary Luehr , Tao Chen , Jason Lewis , Michael Leadbetter
CPC分类号： C07J63/008 , A61K31/56 , A61K31/58 , A61P3/12 , A61P5/40
摘要： The present invention provides a compound of formula (I) or a salt thereof: (Formula (I)) wherein X, L, V, R1; R2, R3 and R4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.
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公开(公告)号：US11768319B2
公开(公告)日：2023-09-26
申请号：US16636596
申请日：2018-08-06
申请人： Ardelyx, Inc.
发明人： Gary Luehr , Dean Dragoli , Michael Leadbetter , Tao Chen , Jason Lewis
CPC分类号： G02B5/0294 , A61P5/44 , C07J63/008 , G02B3/0056 , G02B5/0215 , G02B5/201 , G02B27/0018 , G02F1/133502 , G02B5/021 , G02B2207/123 , G02F1/133526
摘要： The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.
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