公开(公告)号：US20240059679A1

公开(公告)日：2024-02-22

申请号：US18483311

申请日：2023-10-09

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  David James Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D405/12 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D405/12 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07B2200/13

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US20220387402A1

公开(公告)日：2022-12-08

申请号：US17612672

申请日：2020-05-15

Applicant: Pfizer Inc.

Inventor： Gary E. Aspnes ,  Scott W. Bagley ,  John M. Curto ,  Matthew Dowling ,  David James Edmonds ,  Dilinie Fernando ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David Andrew Griffith ,  Kim Huard ,  Gajendra Ingle ,  Wenhua Jiao ,  Shawn M. LaCasse ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David Walter Piotrowski ,  Roger B. Ruggeri ,  Kristin Wiglesworth

IPC: A61K31/438 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/46 ,  A61K45/06 ,  A61K38/26 ,  A61K38/28 ,  A61K38/17 ,  A61P1/16

Abstract: In part, the invention provides a new combination comprising (1) a GLP-1R agonist and (2) an ACC inhibitor or a DGAT2 inhibitor, or a KHK inhibitor or FXR agonist. The invention further provides new methods for treating diseases and disorders, for example, fatty liver, nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, nonalcoholic steatohepatitis with liver fibrosis, nonalcoholic steatohepotitis with cirrhosis, and nonalcoholic steatohepatitis with cirrhosis and with hepatocellular carcinoma or with a metabolic-related disease, obesity, and type 2 diabetes, for example, using the new combination described herein.

公开(公告)号：US20190382387A1

公开(公告)日：2019-12-19

申请号：US16535553

申请日：2019-08-08

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  David James Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D405/12 ,  C07D405/14 ,  C07C53/10 ,  C07D471/04 ,  C07C215/40 ,  C07C53/06 ,  C07D413/14

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US11034678B2

公开(公告)日：2021-06-15

申请号：US16793441

申请日：2020-02-18

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D401/04 ,  C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US20180258081A1

公开(公告)日：2018-09-13

申请号：US15977238

申请日：2018-05-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D401/14 ,  C07D409/14 ,  A61K31/506 ,  A61K45/06

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US20140315928A1

公开(公告)日：2014-10-23

申请号：US14253084

申请日：2014-04-15

Applicant: Pfizer Inc.

Inventor： Etzer Darout ,  Robert Dullea ,  Julie Jia Li Hawkins ,  Allyn T. Londregan ,  Paula M. Loria ,  Bruce Maguire ,  Kim F. McClure ,  Donna N. Petersen ,  David W. Piotrowski

IPC: C07D401/14 ,  A61K31/519 ,  A61K45/06 ,  C07D413/14 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4545 ,  C07D487/04 ,  C07D471/04

CPC classification number: A61K31/519 ,  A61K31/4545 ,  A61K31/4725 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract translation: 本发明涉及取代的酰胺化合物，含有这些化合物的药物组合物以及这些化合物用于降低血浆脂质水平的用途，例如LDL-胆固醇和甘油三酸酯，并因此治疗由高水平的LDL-胆固醇加重的疾病， 甘油三酸酯，如动脉粥样硬化和心血管疾病，包括人在内的哺乳动物。

公开(公告)号：US11866425B2

公开(公告)日：2024-01-09

申请号：US17345064

申请日：2021-06-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: A61K31/505 ,  A61P3/00 ,  A61P3/10 ,  A61P3/06 ,  C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  C07B2200/13

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US20210309646A1

公开(公告)日：2021-10-07

申请号：US17345064

申请日：2021-06-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US10683281B2

公开(公告)日：2020-06-16

申请号：US16535553

申请日：2019-08-08

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  David James Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D405/12 ,  C07D405/14 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D413/14 ,  C07D471/04

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US20200181127A1

公开(公告)日：2020-06-11

申请号：US16793441

申请日：2020-02-18

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D409/14 ,  A61K45/06 ,  A61K31/506 ,  C07D401/14

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.