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：US20150353508A1

公开(公告)日：2015-12-10

申请号：US14830015

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Mary Didiuk ,  Kevin J. Filipski ,  Angel Guzman-Perez ,  Esther C. Lee ,  Jeffrey A. Pfefferkorn ,  Benjamin Stevens ,  Meihua Tu

IPC: C07D239/84 ,  A61K31/517

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D215/38 ,  C07D217/22 ,  C07D239/94 ,  C07D241/44

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其中R1，R2，R3，A1，A2，A3，B1，B2，B3和B4如本文所定义。 已经发现式I的化合物用作胰高血糖素拮抗剂或反向激动剂。 因此，式I化合物及其药物组合物可用于治疗由胰高血糖素介导的疾病，病症或病症。

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：US09139538B2

公开(公告)日：2015-09-22

申请号：US14564263

申请日：2014-12-09

Applicant: Pfizer Inc.

Inventor： Mary Didiuk ,  Kevin J. Filipski ,  Angel Guzman-Perez ,  Esther C. Lee ,  Jeffrey A. Pfefferkorn ,  Benjamin Stevens ,  Meihua Tu

IPC: C07D215/58 ,  C07D241/44 ,  C07D215/38 ,  C07D239/94 ,  C07D217/22 ,  C07D239/84

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D215/38 ,  C07D217/22 ,  C07D239/94 ,  C07D241/44

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

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：US10174007B2

公开(公告)日：2019-01-08

申请号：US15729885

申请日：2017-10-11

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: A61K31/403 ,  C07D403/14 ,  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：US20180037575A1

公开(公告)日：2018-02-08

申请号：US15729885

申请日：2017-10-11

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

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：US09809579B2

公开(公告)日：2017-11-07

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

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.