公开(公告)号：US10208019B2

公开(公告)日：2019-02-19

申请号：US15839901

申请日：2017-12-13

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  Matthew S. Dowling ,  David Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Gajendra Ingle ,  Wenhua Jiao ,  Chris Limberakis ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14 ,  A61K31/496 ,  A61K31/4545 ,  A61P15/10 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  A61P3/00

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-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：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：US20170183328A1

公开(公告)日：2017-06-29

申请号：US15381295

申请日：2016-12-16

Applicant: Pfizer Inc.

Inventor： Matthew Dowling ,  Dilinie Fernando ,  Kentaro Futatsugi ,  Kim Huard ,  Thomas Victor Magee ,  Brian Raymer ,  Andre Shavnya ,  Aaron Smith ,  Benjamin Thuma ,  Andy Tsai ,  Meihua Tu

IPC: C07D403/14 ,  C07D403/04 ,  C07D401/04 ,  C07D401/14

CPC classification number: C07D403/14 ,  A61K31/403 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US09440949B2

公开(公告)日：2016-09-13

申请号：US14643210

申请日：2015-03-10

Applicant: PFIZER INC.

Inventor： Shawn Cabral ,  Kentaro Futatsugi ,  David Hepworth ,  Kim Huard ,  Daniel Wei-Shung Kung ,  Suvi Tuula Marjukka Orr ,  Kun Song

IPC: A61K31/5377 ,  A61K31/606 ,  A61K31/506 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/04 ,  C07D487/04 ,  C07D413/14 ,  C07D491/08 ,  C07D401/14 ,  C07D487/02

CPC classification number: A61K31/506 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/606 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/02 ,  C07D487/04 ,  C07D491/08

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.

Abstract translation: 本文描述了抑制二酰基甘油酰基转移酶2（DGAT2）的活性的式I化合物及其在治疗与动物相关疾病中的用途。

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：US20240034725A1

公开(公告)日：2024-02-01

申请号：US18477050

申请日：2023-09-28

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  Matthew S. Dowling ,  David Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Gajendra Ingle ,  Wenhua Jiao ,  Chris Limberakis ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D401/14 ,  A61K31/496 ,  A61K31/4545 ,  C07D487/04 ,  A61P3/00 ,  A61P15/10 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K31/4545 ,  C07D487/04 ,  A61P3/00 ,  A61P15/10 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-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：US10988463B2

公开(公告)日：2021-04-27

申请号：US16999295

申请日：2020-08-21

Applicant: Pfizer Inc.

Inventor： Matthew Dowling ,  Dilinie Fernando ,  Kentaro Futatsugi ,  Kim Huard ,  Thomas Victor Magee ,  Brian Raymer ,  Andre Shavnya ,  Aaron Smith ,  Benjamin Thuma ,  Andy Tsai ,  Meihua Tu

IPC: C07D401/14 ,  C07D403/14 ,  A61K31/403 ,  C07D401/04 ,  C07D403/04

Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.

公开(公告)号：US10851081B2

公开(公告)日：2020-12-01

申请号：US16861646

申请日：2020-04-29

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Scott W. Bagley ,  John M. Curto ,  Matthew S. Dowling ,  David Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Gajendra Ingle ,  Wenhua Jiao ,  Chris Limberakis ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC: C07D401/14 ,  C07D471/04 ,  A61K31/4545 ,  C07D487/04 ,  A61P3/00 ,  A61P15/10 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  C07D405/14 ,  C07D413/14 ,  A61K31/496

Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-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：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.