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公开(公告)号：US10968246B2
公开(公告)日：2021-04-06
申请号：US16456661
申请日：2019-06-28
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 , C07C409/12 , A61K31/4545 , A61K31/506 , A61K31/4425 , A61K31/551 , C07D471/04 , C07B59/00 , C07D213/81 , C07D213/80 , C07D487/08 , A61K45/06
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：US20200062795A1
公开(公告)日：2020-02-27
申请号：US16456661
申请日：2019-06-28
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
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：US10392413B2
公开(公告)日：2019-08-27
申请号：US15382872
申请日：2016-12-19
申请人： Ardelyx, Inc.
发明人： Jason Gustaf 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
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：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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