公开(公告)号：EP3351248A1

公开(公告)日：2018-07-25

申请号：EP17200784.1

申请日：2009-12-30

Applicant: Ardelyx, Inc.

Inventor： Charmot, Dominique ,  Jacobs, Jeffrey W. ,  Leadbetter, Michael Robert ,  Navre, Marc ,  Carreras, Chris ,  Bell, Noah

IPC: A61K31/472 ,  A61K31/4725 ,  A61P1/00 ,  A61P7/10 ,  A61P9/04 ,  A61P9/12 ,  A61K45/06 ,  A61K47/55

CPC classification number: 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 ,  Y02A50/414

Abstract: 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

公开(公告)号：EP2590656B1

公开(公告)日：2017-11-15

申请号：EP11834773.1

申请日：2011-07-07

Applicant: Ardelyx, Inc.

Inventor： 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: A61K31/506

CPC classification number: 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

公开(公告)号：EP2591354A1

公开(公告)日：2013-05-15

申请号：EP11804371.0

申请日：2011-07-07

Applicant: Ardelyx, Inc.

Inventor： 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 ,  DU, Xunxiang ,  OSLOB, Johan

IPC: G01N33/48 ,  G01N31/00 ,  G01G23/01 ,  G06G7/58

CPC classification number: A61K33/24 ,  A61K31/19 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4418 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/465 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/522 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/706 ,  A61K31/785 ,  A61K33/10 ,  A61K45/06 ,  C07D213/81 ,  C07D295/155 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract translation: 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。 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。

公开(公告)号：EP2590656A2

公开(公告)日：2013-05-15

申请号：EP11834773.1

申请日：2011-07-07

Applicant: Ardelyx, Inc.

Inventor： 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: A61K31/506

CPC classification number: 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

Abstract: 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, 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.

Abstract translation: 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，A，R 1和R 2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。

公开(公告)号：EP4397366A2

公开(公告)日：2024-07-10

申请号：EP24159204.7

申请日：2018-08-06

Applicant: Ardelyx, Inc.

Inventor： LUEHR, Gary ,  DRAGOLI, Dean ,  LEADBETTER, Michael ,  CHEN, Tao ,  LEWIS, Jason

IPC: A61P5/44

CPC classification number: C07J63/008 ,  G02B3/0056 ,  G02B5/0215 ,  G02B5/0268 ,  G02B5/0294 ,  G02B27/0018 ,  G02B2207/12320130101 ,  G02F1/133502 ,  G02F1/133524 ,  G02F1/133526

Abstract: 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.

公开(公告)号：EP3972599A1

公开(公告)日：2022-03-30

申请号：EP20730955.0

申请日：2020-05-21

Applicant: Ardelyx, Inc.

Inventor： KING, Andrew

IPC: A61K31/4725 ,  A61K31/785 ,  A61K45/06 ,  A61K47/55 ,  A61P3/00 ,  A61P3/12

公开(公告)号：EP3565808A1

公开(公告)日：2019-11-13

申请号：EP18703655.3

申请日：2018-01-09

Applicant: Ardelyx, Inc.

Inventor： DRAGOLI, Dean ,  DOTSENKO, Irina ,  LEWIS, Jason

IPC: C07D317/26 ,  C07D225/02 ,  C07D249/04 ,  C07D207/12 ,  C07D295/033 ,  C07D211/56 ,  A61K31/40 ,  A61K31/41 ,  A61K31/435 ,  A61K31/445 ,  A61K31/4462

公开(公告)号：EP2983667B1

公开(公告)日：2019-03-20

申请号：EP14782884.2

申请日：2014-04-10

Applicant: Ardelyx, Inc.

Inventor： CARRERAS, Christopher ,  CHARMOT, Dominique ,  JACOBS, Jeffrey, W. ,  LABONTE, Eric ,  LEWIS, Jason, G.

IPC: A61K47/55 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4545 ,  A61P3/00

公开(公告)号：EP2590510B1

公开(公告)日：2016-09-28

申请号：EP11804373.6

申请日：2011-07-07

Applicant: Ardelyx, Inc.

Inventor： 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: A01N43/38 ,  A61K31/405

CPC classification number: A61K31/5377 ,  A61K31/454 ,  A61K31/59 ,  A61K45/06 ,  C07D209/12 ,  C07D209/14

公开(公告)号：EP3030252A2

公开(公告)日：2016-06-15

申请号：EP14755279.8

申请日：2014-08-08

Applicant: Ardelyx, Inc.

Inventor： CHARMOT, Dominique ,  LEWIS, Jason G. ,  JACOBS, Jeffrey W. ,  LANGSETMO, Ingrid ,  CARRERAS, Christopher

IPC: A61K38/10 ,  A61K31/197 ,  A61K31/437 ,  A61K31/4427 ,  A61P13/12

CPC classification number: A61K38/10 ,  A61K31/00 ,  A61K31/195 ,  A61K31/27 ,  A61K31/352 ,  A61K31/353 ,  A61K31/382 ,  A61K31/4045 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/475 ,  A61K31/506 ,  A61K31/7072 ,  A61K33/26 ,  A61K38/16 ,  A61K45/06 ,  G01N33/5038 ,  G01N33/5044 ,  G01N33/84 ,  A61K2300/00

Abstract: Provided are non-NHE3-binding agents having activity as phosphate transport/uptake inhibitors in the gastrointestinal tract, including in the small intestine, methods for their use as therapeutic or prophylactic agents, and related methods of drug discovery.

Abstract translation: 提供了在胃肠道中包括小肠中具有作为磷酸盐转运/摄取抑制剂活性的非NHE3结合剂，它们用作治疗剂或预防剂的方法以及药物发现的相关方法。