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：US20250067907A1

公开(公告)日：2025-02-27

申请号：US18823388

申请日：2024-09-03

Applicant: Ardelyx, Inc.

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

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

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：US20250066410A1

公开(公告)日：2025-02-27

申请号：US18776075

申请日：2024-07-17

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 ,  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 ,  C07B59/00 ,  C07C409/12 ,  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: 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：US12084472B2

公开(公告)日：2024-09-10

申请号：US17185653

申请日：2021-02-25

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: A61K31/444 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/553 ,  A61K31/706 ,  A61K45/06 ,  C07B59/00 ,  C07C409/12 ,  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 ,  C07H15/26

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 ,  C07C409/12 ,  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 ,  C07B2200/05

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：US20220306672A1

公开(公告)日：2022-09-29

申请号：US17185653

申请日：2021-02-25

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 ,  C07C409/12

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.