公开(公告)号：US20200377482A1

公开(公告)日：2020-12-03

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: 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：US10787438B2

公开(公告)日：2020-09-29

申请号：US16744283

申请日：2020-01-16

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 ,  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：US20200148669A1

公开(公告)日：2020-05-14

申请号：US16744283

申请日：2020-01-16

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 ,  C07D401/14 ,  C07D401/04 ,  A61K31/403

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：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：US11634410B2

公开(公告)日：2023-04-25

申请号：US17209780

申请日：2021-03-23

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 ,  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：US20210309644A1

公开(公告)日：2021-10-07

申请号：US17209780

申请日：2021-03-23

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 ,  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：US20190106412A1

公开(公告)日：2019-04-11

申请号：US16211283

申请日：2018-12-06

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 ,  A61K31/403 ,  C07D401/04 ,  C07D401/14

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：US08889730B2

公开(公告)日：2014-11-18

申请号：US13831588

申请日：2013-03-15

Applicant: Pfizer Inc.

Inventor： Samit Bhattacharya ,  Kimberly Cameron ,  Matthew Dowling ,  Dilinie Fernando ,  David Ebner ,  Kevin Filipski ,  Daniel Kung ,  Esther Lee ,  Aaron Smith ,  Meihua Tu

IPC: A61K31/404 ,  C07D209/42 ,  A61P13/12 ,  A61P3/10 ,  C07D403/12 ,  C07D401/04 ,  A61K31/416 ,  C07D413/14 ,  C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D231/56 ,  C07D413/12 ,  C07D401/14 ,  C07D401/10

CPC classification number: C07D413/12 ,  A61K31/404 ,  A61K31/416 ,  C07D209/42 ,  C07D231/56 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.

Abstract translation: 本发明涉及活化5'腺苷单磷酸活化蛋白激酶（AMPK）的式（I）的吲哚和吲唑化合物。 本发明还包括含有这些化合物的药物组合物和用于治疗或预防通过AMPK活化改善的疾病，病症或障碍的方法。

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.