公开(公告)号：US20210163524A1

公开(公告)日：2021-06-03

申请号：US16636596

申请日：2018-08-06

Applicant: Ardelyx, Inc.

Inventor： Gary Luehr ,  Dean Dragoli ,  Michael Leadbetter ,  Tao Chen ,  Jason Lewis

IPC: C07J63/00 ,  A61P5/44

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：US09301951B2

公开(公告)日：2016-04-05

申请号：US14536509

申请日：2014-11-07

Applicant: Ardelyx, Inc.

Inventor： Jason G. Lewis ,  Jeffrey W. Jacobs ,  Nicholas Reich ,  Michael R. Leadbetter ,  Noah Bell ,  Han-Ting Chang ,  Tao Chen ,  Marc Navre ,  Dominique Charmot ,  Christopher Carreras ,  Eric Labonte

IPC: A61K31/4418 ,  A61K31/444 ,  A61K31/505 ,  A61K31/506 ,  C07D213/36 ,  C07D239/26 ,  C07D401/10 ,  C07D403/10 ,  C07D401/12 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/42 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/44 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/59 ,  A61K31/785 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/496 ,  A61K31/593

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: 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）：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。

公开(公告)号：US20240209019A1

公开(公告)日：2024-06-27

申请号：US18518267

申请日：2023-11-22

Applicant: ARDELYX, INC.

Inventor： Dean Dragoli ,  Gary Luehr ,  Tao Chen ,  Jason Lewis ,  Michael Leadbetter

IPC: C07J63/00 ,  A61K31/56 ,  A61K31/58 ,  A61P3/12 ,  A61P5/40

CPC classification number: C07J63/008 ,  A61K31/56 ,  A61K31/58 ,  A61P3/12 ,  A61P5/40

Abstract: The present invention provides a compound of formula (I) or a salt thereof:




wherein X, L, V, R1, R2, R3 and R4, are as defined herein.

公开(公告)号：US11858959B2

公开(公告)日：2024-01-02

申请号：US17429599

申请日：2020-02-06

Applicant: ARDELYX, INC.

Inventor： Dean Dragoli ,  Gary Luehr ,  Tao Chen ,  Jason Lewis ,  Michael Leadbetter

IPC: C07J63/00 ,  A61P3/12 ,  A61K31/56 ,  A61P5/40 ,  A61K31/58

CPC classification number: C07J63/008 ,  A61K31/56 ,  A61K31/58 ,  A61P3/12 ,  A61P5/40

Abstract: The present invention provides a compound of formula (I) or a salt thereof: (Formula (I)) wherein X, L, V, R1; R2, R3 and R4, are as defined herein. The claimed compounds inhibit the enzyme 11-hydroxysteroid dehydrogenase type 2 (11-HSD2) and as a result are useful in the treatment of hyperkalemia by preventing cortisol from being oxidised to cortisone and thus allowing it to occupy the mineralocorticoid receptor, thus stimulating potassium excretion.

公开(公告)号：US11768319B2

公开(公告)日：2023-09-26

申请号：US16636596

申请日：2018-08-06

Applicant: Ardelyx, Inc.

Inventor： Gary Luehr ,  Dean Dragoli ,  Michael Leadbetter ,  Tao Chen ,  Jason Lewis

IPC: C07J63/00 ,  A61P5/44 ,  G02B5/02 ,  G02B5/20 ,  G02B3/00 ,  G02F1/1335 ,  G02B27/00

CPC classification number: G02B5/0294 ,  A61P5/44 ,  C07J63/008 ,  G02B3/0056 ,  G02B5/0215 ,  G02B5/201 ,  G02B27/0018 ,  G02F1/133502 ,  G02B5/021 ,  G02B2207/123 ,  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：US10968246B2

公开(公告)日：2021-04-06

申请号：US16456661

申请日：2019-06-28

Applicant: Ardelyx, Inc.

Inventor： Jason G. Lewis ,  Michael Robert Leadbetter ,  Jeremy Caldwell ,  Dean Dragoli ,  Noah Bell ,  Jeffrey W. Jacobs ,  Patricia Finn ,  Rakesh Jain ,  Tao Chen ,  Matthew Siegel

IPC: 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

Abstract: 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：US20200062795A1

公开(公告)日：2020-02-27

申请号：US16456661

申请日：2019-06-28

Applicant: Ardelyx, Inc.

Inventor： Jason G. Lewis ,  Michael Robert Leadbetter ,  Jeremy Caldwell ,  Dean Dragoli ,  Noah Bell ,  Jeffrey W. Jacobs ,  Patricia Finn ,  Rakesh Jain ,  Tao Chen ,  Matthew Siegel

IPC: 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

Abstract: 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：US10392413B2

公开(公告)日：2019-08-27

申请号：US15382872

申请日：2016-12-19

Applicant: Ardelyx, Inc.

Inventor： Jason Gustaf Lewis ,  Michael Robert Leadbetter ,  Jeremy Caldwell ,  Dean Dragoli ,  Noah Bell ,  Jeffrey W. Jacobs ,  Patricia Finn ,  Rakesh Jain ,  Tao Chen ,  Matthew Siegel

IPC: 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

Abstract: 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：US20150164905A1

公开(公告)日：2015-06-18

申请号：US14337032

申请日：2014-07-21

Applicant: Ardelyx, Inc.

Inventor： Jason G. Lewis ,  Jeffrey W. Jacobs ,  Nicholas Reich ,  Michael R. Leadbetter ,  Noah Bell ,  Han-Ting Chang ,  Tao Chen ,  Marc Navre ,  Dominique Charmot ,  Christopher Carreras ,  Eric Labonte

IPC: A61K31/5377 ,  A61K31/454 ,  A61K45/06

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

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, 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: 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）：包括立体异构体，其药学上可接受的盐和前药，其中X，Y，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。

公开(公告)号：US20150148311A1

公开(公告)日：2015-05-28

申请号：US14310989

申请日：2014-06-20

Applicant: Ardelyx, Inc.

Inventor： Jason G. Lewis ,  Nicholas Reich ,  Tao Chen ,  Jeffrey W. Jacobs ,  Dominique Charmot ,  Marc Navre ,  Patricia Finn ,  Christopher Carreras ,  Andrew Spencer

IPC: C07D241/42 ,  C07D403/06 ,  C07D417/06 ,  A61K45/06 ,  C07D413/06 ,  A61K31/5377 ,  C07F9/6547 ,  A61K31/675 ,  A61K31/498 ,  A61K31/541

CPC classification number: C07D241/42 ,  A61K31/498 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/675 ,  A61K45/06 ,  C07C235/68 ,  C07C237/24 ,  C07D207/16 ,  C07D213/75 ,  C07D277/06 ,  C07D307/79 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07F9/6547

Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.

Abstract translation: 具有以下结构（I）的化合物或其立体异构体，互变异构体，药学上可接受的盐或前药，其中R1，R2，R3，R4，R8，R9，R10，R11，R12，A1，A2，X，Y和Z 如本文所定义。 还提供了这样的化合物如TGR5拮抗剂和治疗各种适应症的用途，包括II型糖尿病。