公开(公告)号：US20190308973A1

公开(公告)日：2019-10-10

申请号：US16327790

申请日：2017-08-23

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08 ,  A61P1/16

摘要： The disclosure 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): wherein L1, L2, A, B, R1, R2, R3, and R4 are described herein.

公开(公告)号：US20190233420A1

公开(公告)日：2019-08-01

申请号：US16327791

申请日：2017-08-23

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08

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 L1, A, X1, X2, R1, R2, and R3 are described herein.

公开(公告)号：US10968246B2

公开(公告)日：2021-04-06

申请号：US16456661

申请日：2019-06-28

申请人： Ardelyx, Inc.

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

IPC分类号： 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

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: 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

申请人： Ardelyx, Inc.

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

IPC分类号： 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

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: 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

申请人： Ardelyx, Inc.

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

IPC分类号： 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

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

公开(公告)号：US11718619B2

公开(公告)日：2023-08-08

申请号：US17224518

申请日：2021-04-07

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08 ,  A61P1/16

CPC分类号： C07D471/08 ,  A61P1/16

摘要： The disclosure 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):




wherein L1, L2, A, B, R1, R2, R3, and R4 are described herein.

公开(公告)号：US20230139597A1

公开(公告)日：2023-05-04

申请号：US17858917

申请日：2022-07-06

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08 ,  C07D493/08 ,  C07D413/14 ,  C07F9/6558 ,  C07D417/14 ,  C07D413/12

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): wherein L1, A, X1, X2, R1, R2, and R3 are described herein.

公开(公告)号：US10793568B2

公开(公告)日：2020-10-06

申请号：US16327791

申请日：2017-08-23

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08 ,  C07D493/08 ,  C07D413/14 ,  C07F9/6558 ,  C07D417/14 ,  C07D413/12

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 L1, A, X1, X2, R1, R2, and R3 are described herein.

公开(公告)号：US11091482B2

公开(公告)日：2021-08-17

申请号：US16327790

申请日：2017-08-23

申请人： ARDELYX, INC.

发明人： Jianhua Chao ,  Rakesh Jain ,  Lily Hu ,  Jason Gustaf Lewis ,  Helene Baribault ,  Jeremy Caldwell

IPC分类号： C07D471/08 ,  A61P1/16

摘要： The disclosure 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): wherein L1, L2, A, B, R1, R2, R3, and R4 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

申请人： Ardelyx, Inc.

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

IPC分类号： 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 ,  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

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:






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