公开(公告)号：US20180170908A1

公开(公告)日：2018-06-21

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

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

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：US20250129057A1

公开(公告)日：2025-04-24

申请号：US18685644

申请日：2022-08-25

Applicant: Pfizer Inc.

Inventor： Scott W. Bagley ,  Wesley Dewitt Clark ,  David Andrew Griffith ,  Wenhua Jiao ,  Brian Matthew Samas ,  Lisa Jane Taylor

IPC: C07D405/14 ,  A61K31/4545

Abstract: The invention provides solid forms of 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl) propan-2-amine salt for example, Form 1 or Form 2; as well as pharmaceutical compositions, and the uses thereof in treating diseases, conditions or disorders modulated by GLP-1R in a mammal, such as a human.

公开(公告)号：US20210047298A1

公开(公告)日：2021-02-18

申请号：US17085534

申请日：2020-10-30

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

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：US20190119255A1

公开(公告)日：2019-04-25

申请号：US16220184

申请日：2018-12-14

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 ,  A61K31/4545 ,  A61P43/00 ,  A61P1/16 ,  A61P25/02 ,  A61P3/04 ,  A61P19/02 ,  A61P3/10 ,  A61P13/12 ,  A61P25/18 ,  A61P1/00 ,  A61P15/00 ,  A61P25/16 ,  C07D405/14 ,  C07D471/04 ,  A61P15/10 ,  A61P3/00 ,  C07D487/04 ,  C07D413/14 ,  A61P17/06 ,  A61P9/10 ,  A61P19/06 ,  A61P25/28 ,  A61P25/30 ,  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：US11802121B2

公开(公告)日：2023-10-31

申请号：US18049052

申请日：2022-10-24

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

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：US11655252B2

公开(公告)日：2023-05-23

申请号：US17363494

申请日：2021-06-30

Applicant: Pfizer Inc.

Inventor： Brian Stephen Gerstenberger ,  Wenhua Jiao ,  Manjinder Singh Lall ,  Ricardo Lira ,  Mark Edward Schnute

IPC: C07D471/18 ,  A61K45/06

CPC classification number: C07D471/18 ,  A61K45/06 ,  C07B2200/13

Abstract: A compound of formula I:




or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen or hydroxy; wherein R1 and R2 are not both hydroxy. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.

公开(公告)号：US11512070B2

公开(公告)日：2022-11-29

申请号：US17085534

申请日：2020-10-30

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

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：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：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.