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1. 发明申请

WO2022120287A1 ORAL FORMULATIONS OF TENAPANOR 审中-公开
公开(公告)号：WO2022120287A1
公开(公告)日：2022-06-09
申请号：PCT/US2021/062069
申请日：2021-12-06
申请人： ARDELYX, INC. , ASTRAZENECA AB
发明人： GUNNARSSON, Cecilia
IPC分类号： A61K9/16 , A61K9/20 , A61K31/00
摘要： The present invention provides a pharmaceutical tablet formulation of tenapanor that is chemically stable and soluble comprising greater than about 6% w/w of amorphous tenapanor in its bis-HCl form, an acidifying agent, an antioxidant, a disintegrant, a lubricant, a glidant, a filler, and an immediate release coating, wherein the total chloride content of the active ingredient is greater than 5.82% and the particle diameter distribution D50 is from about from about 18μm to about 22μm.

2. 发明申请

WO2017106818A1 SUBSTITUTED 4-PHENYL PYRIDINE COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS 审中-公开
标题翻译：作为非系统性TGR5激动剂的取代的4-苯基吡啶化合物
公开(公告)号：WO2017106818A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/067460
申请日：2016-12-19
申请人： ARDELYX, INC.
发明人： LEWIS, Jason G. , LEADBETTER, Michael Robert , CALDWELL, Jeremy , DRAGOLI, Dean , BELL, Noah , JACOBS, Jeffrey W. , FINN, Patricia , JAIN, Rakesh , CHEN, Tao , SIEGEL, Matthew
IPC分类号： C07D401/12 , C07D405/12 , C07D213/38 , A61K31/4418 , A61K31/4427 , A61P3/00 , A61P9/10 , A61P11/06
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 , C07B2200/05 , 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
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: (I'), where R 1 , R 2 , R 2' , R 3 , R 4 , X 1 , X 2 , X 3 , X 4 , Q, and n are described herein.
摘要翻译：本发明涉及用于治疗化疗引起的腹泻，糖尿病，II型糖尿病，妊娠糖尿病，空腹血糖受损，葡萄糖耐量减低，胰岛素抵抗，高血糖症，肥胖症的非系统性TGR5激动剂，代谢综合征，溃疡性结肠炎，克罗恩氏病，与肠外营养相关的病症，特别是在短肠综合征期间和肠易激综合征（IBS）以及其他与TGR5相关的疾病和病症，具有下式：（I'），其中R < R 1，R 2，R 2，R 3，R 4，X 1，R 2，这里描述了X 1，X 1，X 2，X 3，X 4，Q和n。

3. 发明申请

WO2014169094A2 NHE3-BINDING COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译： NHE3-BINDING化合物和抑制磷酸盐运输的方法
公开(公告)号：WO2014169094A2
公开(公告)日：2014-10-16
申请号：PCT/US2014/033603
申请日：2014-04-10
申请人： ARDELYX, INC
发明人： CARRERAS, Christopher , CHARMOT, Dominique , JACOBS, Jeffrey, W. , LABONTE, Eric , LEWIS, Jason, G.
IPC分类号： A61K31/472
CPC分类号： A61K31/4725 , A61K31/4545 , A61K31/472 , A61K47/55
摘要： Provided are NHE3-binding and/or NHE3 -modulating agents having activity as phosphate transport inhibitors, including inhibitors of phosphate transport in the gastrointestinal tract and the kidneys, and methods for their use as therapeutic or prophylactic agent.
摘要翻译：提供具有作为磷酸盐转运抑制剂的活性的NHE3结合和/或NHE3调节剂，包括在胃肠道和肾中磷酸盐转运的抑制剂，以及用作治疗或预防剂的方法。

4. 发明申请

WO2018039386A1 HORMONE RECEPTOR MODULATORS FOR TREATING METABOLIC CONDITIONS AND DISORDERS 审中-公开
标题翻译：激素受体调节剂，用于治疗代谢性疾病和病症
公开(公告)号：WO2018039386A1
公开(公告)日：2018-03-01
申请号：PCT/US2017/048281
申请日：2017-08-23
申请人： ARDELYX, INC.
发明人： CHAO, Jianhua , JAIN, Rakesh , HU, Lily , LEWIS, Jason Gustaf , BARIBAULT, Helene , CALDWELL, Jeremy
IPC分类号： C07D413/14 , C07D413/12 , C07D417/14 , C07D493/08 , C07F9/38 , A61K31/422 , A61K31/4748 , A61P1/00 , A61P35/00 , A61P3/00 , A61P13/00 , A61P7/00 , A61P37/00
摘要： The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): (I), wherein L 1 , A, X 1 , X 2 , R 1 , R 2 , and R 3 are described herein.
摘要翻译：本发明涉及可用于治疗自身免疫病症，肝病，肠疾病，肾病，癌症和其中FXR起作用的其他疾病的FXR激活剂，具有式（I）：其中L 1，A，X 1，X 2，R 1，R 1，R 4，这里描述了R 2和R 3。。

5. 发明申请

WO2012054110A3 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
公开(公告)号：WO2012054110A3
公开(公告)日：2012-04-26
申请号：PCT/US2011/043267
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/165
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R 1 and R 2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

6. 发明申请

WO2012054110A2 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012054110A2
公开(公告)日：2012-04-26
申请号：PCT/US2011043267
申请日：2011-07-07
申请人： ARDELYX INC , LEWIS JASON G , JACOBS JEFFREY W , REICH NICHOLAS , LEADBETTER MICHAEL R , BELL NOAH , CHANG HAN-TING , CHEN TAO , NAVRE MARC , CHARMOT DOMINIQUE , CARRERAS CHRISTOPHER , LABONTE ERIC
发明人： LEWIS JASON G , JACOBS JEFFREY W , REICH NICHOLAS , LEADBETTER MICHAEL R , BELL NOAH , CHANG HAN-TING , CHEN TAO , NAVRE MARC , CHARMOT DOMINIQUE , CARRERAS CHRISTOPHER , LABONTE ERIC
IPC分类号： A61K31/506
CPC分类号： C07D213/81 , A61K31/44 , A61K31/4418 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/59 , A61K31/593 , A61K31/785 , A61K45/06 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/82 , C07D239/34 , C07D239/42 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：具有作为磷酸盐转运抑制剂的活性的化合物，更具体地，公开了肠顶膜Na /磷酸盐共转运的抑制剂。所述化合物具有以下结构（I）：（I），其包括立体异构体，其药学上可接受的盐和前药，其中X，Y，A，R 1和R 2如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

7. 发明申请

WO2012006473A1 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006473A1
公开(公告)日：2012-01-12
申请号：PCT/US2011/043261
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric
IPC分类号： A61K31/506 , A61K31/4965 , C07D401/00 , C07D403/00 , C07D211/68 , C07D413/00
CPC分类号： A61K31/5377 , A61K31/415 , A61K31/454 , A61K31/4545 , A61K31/4965 , A61K31/505 , A61K31/59 , A61K45/06 , C07D211/68 , C07D231/40 , C07D233/88 , C07D249/14 , C07D255/02 , C07D277/46 , C07D285/135 , C07D401/12 , A61K2300/00
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有作为磷酸盐转运抑制剂的活性的化合物，更具体地说，具有肠顶膜Na /磷酸盐共转运的抑制剂。所述化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中X，Y和A如本文所定义。还公开了与这些化合物的制备和使用有关的方法，以及包含这些化合物的药物组合物。

8. 发明申请

WO2010078449A2 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
标题翻译：用于抑制NHE介导的抗体治疗与流体保持或盐过载和胃肠疾病相关的疾病的化合物和方法
公开(公告)号：WO2010078449A2
公开(公告)日：2010-07-08
申请号：PCT/US2009/069852
申请日：2009-12-30
申请人： ARDELYX, INC. , CHARMOT, Dominique , JACOBS, Jeffrey, W. , LEADBETTER, Michael, Robert , NAVRE, Marc , CARRERAS, Chris , BELL, Noah
发明人： CHARMOT, Dominique , JACOBS, Jeffrey, W. , LEADBETTER, Michael, Robert , NAVRE, Marc , CARRERAS, Chris , BELL, Noah
IPC分类号： C07C311/29 , C07D401/12 , C07D217/04 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/62 , A61K31/18 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06
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 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.
摘要翻译：本公开涉及用于治疗与流体保留或盐过载相关的疾病的化合物和方法，例如心力衰竭（特别是充血性心力衰竭），慢性肾脏疾病，终末期肾病，肝脏疾病和过氧化物酶体增殖激活受体（PPAR）γ激动剂诱导的液体保留。本公开还涉及用于治疗高血压的化合物和方法。本公开还涉及用于治疗胃肠道疾病的化合物和方法，包括治疗或减少与胃肠道疾病相关的疼痛。所述方法通常包括向有需要的哺乳动物施用药学有效量的化合物或包含这种化合物的药物组合物，其被设计为在胃肠道（GI）道中基本上具有活性以抑制NHE介导的钠离子离子和氢离子。更具体地，该方法包括向有需要的哺乳动物施用药学有效量的化合物或包含这种化合物的药物组合物，其抑制NHE-3，-2和/或-8介导的钠和/或胃肠道中的氢离子被设计为对上皮细胞层，或更具体地，GI道的上皮基本上不可渗透。由于化合物基本上是不可渗透的，其不被吸收，因此基本上是全身非生物可利用的，以限制其上的其他内脏（例如肝，心，脑等）的暴露。本公开还涉及一种方法，其中将哺乳动物与吸收流体的聚合物一起施用这样的化合物，使得该组合如上所述起作用并进一步提供螯合胃肠道中存在的流体和/或盐的能力。

9. 发明申请

WO2019060051A1 GLYCYRRHETINIC ACID DERIVATIVES FOR TREATING HYPERKALEMIA 审中-公开
公开(公告)号：WO2019060051A1
公开(公告)日：2019-03-28
申请号：PCT/US2018/045421
申请日：2018-08-06
申请人： ARDELYX, INC. , LUEHR, Gary , DRAGOLI, Dean , LEADBETTER, Michael , CHEN, Tao , LEWIS, Jason
发明人： LUEHR, Gary , DRAGOLI, Dean , LEADBETTER, Michael , CHEN, Tao , LEWIS, Jason
IPC分类号： C07J63/00 , A61K31/575 , A61P5/44
摘要： The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R 1 , R 2 , R 3 and R 4 , are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.

10. 发明申请

WO2018129557A1 INHIBITORS OF NHE-MEDIATED ANTIPORT 审中-公开
公开(公告)号：WO2018129557A1
公开(公告)日：2018-07-12
申请号：PCT/US2018/013027
申请日：2018-01-09
申请人： ARDELYX, INC.
发明人： DOTSENKO, Irina , DRAGOLI, Dean , LEWIS, Jason
IPC分类号： C07D401/14 , C07D401/12 , A61P1/10 , A61P9/12 , A61K31/4725
摘要： The present disclosure is directed to compounds (Ι') and to their use in 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 (Ι') and their use in methods for the treatment of hypertension. The present disclosure is also directed to compounds (Ι') and to their use in methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

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