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1. 发明授权

US08969377B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
标题翻译：用于抑制NHE介导的止痒剂用于治疗与流体保留或盐过载和胃肠道疾病相关的疾病的化合物和方法
公开(公告)号：US08969377B2
公开(公告)日：2015-03-03
申请号：US13804752
申请日：2013-03-14
申请人： Ardelyx, Inc.
发明人： Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W Jacobs , Michael Robert Leadbetter , Marc Navre
IPC分类号： A61K31/18 , C07F9/60 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07C311/29 , C07D217/04 , C07D217/14 , C07D401/12 , C07F9/38 , C07F9/576 , C07F9/6558 , C07D217/16 , C07D215/14
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , A61K47/55 , A61P1/00 , A61P7/10 , A61P9/04 , A61P9/12 , C07C311/29 , C07D215/14 , C07D217/04 , C07D217/14 , C07D217/16 , C07D401/12 , C07F9/3808 , C07F9/3834 , C07F9/3882 , C07F9/5765 , C07F9/60 , C07F9/65583
摘要： The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
摘要翻译：本公开涉及结构（X）的化合物：其中：n为2或3; NHE具有以下结构：其中：R1是H或-SO2-NR7R8-; R2选自H，-NR7（CO）R8，-SO2-NR7R8-和-NR7R8; R3是氢; R7是氢; R8是连接L的键; L是聚亚烷基二醇连接体; 和Core具有以下结构：其中：X选自键，-O - ， - NH - ，NHC（= O） - ， - NHC（= O）NH-和-NHSO 2 - ; 和Y选自由以下组成的组：任选取代的C 1-6亚烷基，任选取代的苯，吡啶基，聚乙二醇连接体和 - （CH 2）1-6 O（CH 2）1-6 - 用于治疗肠易激综合征，慢性肾脏疾病和终末期肾病的化合物。

2. 发明授权

US09408840B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorder 有权
标题翻译：用于抑制NHE介导的止痒剂用于治疗与流体滞留或盐过载和胃肠道疾病相关的疾病的化合物和方法
公开(公告)号：US09408840B2
公开(公告)日：2016-08-09
申请号：US14592200
申请日：2015-01-08
申请人： Ardelyx, Inc.
发明人： Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W. Jacobs , Michael Robert Leadbetter , Marc Navre
IPC分类号： A61K31/18 , A61K31/4725 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07C311/29 , C07D217/04 , C07D217/14 , C07D401/12 , C07F9/38 , C07F9/576 , C07F9/6558 , C07D217/16 , C07D215/14 , C07F9/60
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , A61K47/55 , A61P1/00 , A61P7/10 , A61P9/04 , A61P9/12 , C07C311/29 , C07D215/14 , C07D217/04 , C07D217/14 , C07D217/16 , C07D401/12 , C07F9/3808 , C07F9/3834 , C07F9/3882 , C07F9/5765 , C07F9/60 , C07F9/65583
摘要： The present disclosure is directed to compounds of the structure (X): CoreL-NHE)n (X) wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
摘要翻译：本公开涉及结构（X）的化合物：CoreL-NHE）n（X）其中：n为2或3; NHE具有以下结构：其中：R1是H或-SO2-NR7R8-; R2选自H，-NR7（CO）R8，-SO2-NR7R8-和-NR7R8; R3是氢; R7是氢; R8是连接L的键; L是聚亚烷基二醇连接体; 和Core具有以下结构：其中：X选自键，-O - ， - NH - ，NHC（= O） - ， - NHC（= O）NH-和-NHSO 2 - ; 和Y选自由以下组成的组：任选取代的C 1-6亚烷基，任选取代的苯，吡啶基，聚乙二醇连接体和 - （CH 2）1-6 O（CH 2）1-6 - 用于治疗肠易激综合征，慢性肾脏疾病和终末期肾病的化合物。

3. 发明授权

US09006281B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
标题翻译：用于抑制NHE介导的止痒剂用于治疗与流体保留或盐过载和胃肠道疾病相关的疾病的化合物和方法
公开(公告)号：US09006281B2
公开(公告)日：2015-04-14
申请号：US13826186
申请日：2013-03-14
申请人： Ardelyx, Inc.
发明人： Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W Jacobs , Michael Robert Leadbetter , Marc Navre
IPC分类号： A61K31/18 , C07F9/60 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07C311/29 , C07D217/04 , C07D217/14 , C07D401/12 , C07F9/38 , C07F9/576 , C07F9/6558 , C07D217/16 , C07D215/14
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , A61K47/55 , A61P1/00 , A61P7/10 , A61P9/04 , A61P9/12 , C07C311/29 , C07D215/14 , C07D217/04 , C07D217/14 , C07D217/16 , C07D401/12 , C07F9/3808 , C07F9/3834 , C07F9/3882 , C07F9/5765 , C07F9/60 , C07F9/65583
摘要： The present disclosure is directed to compounds and methods for treating irritable bowel syndrome, chronic kidney disease and end stage renal disease by administering to a subject in need thereof a compound or a pharmaceutically acceptable salt thereof, wherein the compound has the structure
摘要翻译：本公开涉及通过向有需要的受试者施用化合物或其药学上可接受的盐来治疗肠易激综合征，慢性肾脏疾病和终末期肾病的化合物和方法，其中所述化合物具有结构

4. 发明授权

US10543207B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
公开(公告)号：US10543207B2
公开(公告)日：2020-01-28
申请号：US15402211
申请日：2017-01-09
申请人： ARDELYX, INC.
发明人： Dominique Charmot , Marc Navre , Christopher Carreras , Noah Bell , Michael Robert Leadbetter , Jeffrey W. Jacobs
IPC分类号： A61K31/4725 , A61K45/06 , A61K9/00
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. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

5. 发明授权

US10376481B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
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.

6. 发明授权

US10968246B2 Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists 有权
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.

7. 发明申请

US20200268741A1 COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS 审中-公开
公开(公告)号：US20200268741A1
公开(公告)日：2020-08-27
申请号：US16773723
申请日：2020-01-27
申请人： Ardelyx, Inc.
发明人： Dominique Charmot , Marc Navre , Christopher Carreras , Noah Bell , Michael Robert Leadbetter , Jeffrey W. Jacobs
IPC分类号： A61K31/4725 , A61K45/06 , A61K9/00 , A61K31/472 , A61K47/60 , A61K31/18 , C07D217/04 , C07F9/62 , C07F9/38 , A61K31/675 , C07F9/40 , C07D217/14 , A61K31/517 , C07D217/16 , A61K31/662
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. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

8. 发明申请

US20200062795A1 SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS 审中-公开
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.

9. 发明授权

US10392413B2 Substituted 4-phenyl pyridine compounds as non-systemic TGR5 agonists 有权
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.

10. 发明申请

US20220306672A1 SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS 有权
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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