公开(公告)号：EP3504205A1

公开(公告)日：2019-07-03

申请号：EP17768538.5

申请日：2017-08-23

Applicant: Ardelyx, Inc.

Inventor： CHAO, Jianhua ,  JAIN, Rakesh ,  HU, Lily ,  LEWIS, Jason Gustaf ,  BARIBAULT, Helene ,  CALDWELL, Jeremy

IPC: 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

公开(公告)号：EP2590965B1

公开(公告)日：2016-04-20

申请号：EP11804370.2

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: C07D403/02 ,  C07D239/42 ,  C07D241/20 ,  A61K45/06 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/59 ,  A61P13/00 ,  A61P13/12

CPC classification number: A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K31/59 ,  A61K45/06 ,  C07D239/42 ,  C07D241/20

公开(公告)号：EP2590965A4

公开(公告)日：2014-12-03

申请号：EP11804370

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: C07D403/02 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/59 ,  A61K45/06 ,  A61P13/00 ,  A61P13/12 ,  C07D239/42 ,  C07D241/20

CPC classification number: A61K31/5377 ,  A61K31/497 ,  A61K31/506 ,  A61K31/59 ,  A61K45/06 ,  C07D239/42 ,  C07D241/20

公开(公告)号：EP2590656A4

公开(公告)日：2014-01-01

申请号：EP11834773

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：EP2590655A4

公开(公告)日：2013-12-18

申请号：EP11804369

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 ,  A61K31/4965 ,  C07D211/68 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00

CPC classification number: 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

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 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.

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。

公开(公告)号：EP2384318A2

公开(公告)日：2011-11-09

申请号：EP09796924.0

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: 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 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

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.

Abstract translation: 本发明涉及的化合物和方法用于与体液潴留或盐的过载，：如心脏衰竭（特别是充血性心脏衰竭），慢性肾脏疾病，终末期肾脏疾病，肝脏疾病，和过氧化物酶体相关病症的治疗 增殖物激活受体（PPAR）γ激动剂诱导的体液潴留。 因此，本公开涉及用于治疗高血压的化合物和方法。 因此，本公开涉及用于胃肠道病症，包括用于治疗或减少与胃肠道病症相关的疼痛的治疗的化合物和方法。

公开(公告)号：EP3939964A1

公开(公告)日：2022-01-19

申请号：EP21178147.1

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: 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

Abstract: The present disclosure is directed to a pharmaceutical composition comprising a compound of formula (X), in combination with another active agent, and to the use of said composition in methods for the treatment of disorders associated with fluid retention or salt overload or gastrointestinal tract disorders, such as irritable bowel syndrome and constipation associated with cystic fibrosis. The methods generally comprise administering to a mammal in need thereof 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 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.

公开(公告)号：EP2887964B1

公开(公告)日：2019-07-03

申请号：EP13753904.5

申请日：2013-08-20

Applicant: Ardelyx, Inc.

Inventor： LEADBETTER, Michael ,  BELL, Noah ,  LEWIS, Jason ,  JACOBS, Jeffrey ,  CARRERAS, Christopher

IPC: A61K47/55 ,  A61K47/60 ,  A61P1/00 ,  A61P9/04 ,  A61P9/12 ,  A61P13/12 ,  A61K31/18 ,  A61K31/4025 ,  A61K31/4545 ,  C07D207/09 ,  C07D207/12 ,  C07D211/14 ,  C07D211/56

公开(公告)号：EP3492106A1

公开(公告)日：2019-06-05

申请号：EP18203276.3

申请日：2014-08-08

Applicant: Ardelyx, Inc.

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

IPC: A61K45/06 ,  A61K31/55 ,  A61K31/198 ,  A61K31/277 ,  A61K31/48 ,  A61P13/12

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.

公开(公告)号：EP3390382A1

公开(公告)日：2018-10-24

申请号：EP16822870.8

申请日：2016-12-19

Applicant: Ardelyx, Inc.

Inventor： LEWIS, Jason G. ,  LEADBETTER, Michael Robert ,  CALDWELL, Jeremy ,  DRAGOLI, Dean ,  BELL, Noah ,  JACOBS, Jeffrey W. ,  FINN, Patricia ,  JAIN, Rakesh ,  CHEN, Tao ,  SIEGEL, Matthew

IPC: C07D401/12 ,  C07D405/12 ,  C07D213/38 ,  A61K31/4418 ,  A61K31/4427 ,  A61P3/00 ,  A61P9/10 ,  A61P11/06

CPC classification number: 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

Abstract: where R1, R2, R2′, R3, R4, X1, X2, X3, X4, Q, and n are described herein.