公开(公告)号：US20240140937A1

公开(公告)日：2024-05-02

申请号：US18520638

申请日：2023-11-28

申请人： Pfizer Inc.

发明人： 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分类号： C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14

CPC分类号： C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/06

摘要： 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：US10934279B2

公开(公告)日：2021-03-02

申请号：US16436311

申请日：2019-06-10

申请人： Pfizer Inc.

发明人： 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分类号： C07D405/12 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： 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：US20210047298A1

公开(公告)日：2021-02-18

申请号：US17085534

申请日：2020-10-30

申请人： Pfizer Inc.

发明人： 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分类号： 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

摘要： 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：US20200377482A1

公开(公告)日：2020-12-03

申请号：US16999295

申请日：2020-08-21

申请人： Pfizer Inc.

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

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

摘要： 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：US20190382388A1

公开(公告)日：2019-12-19

申请号：US16535616

申请日：2019-08-08

申请人： Pfizer Inc.

发明人： 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分类号： C07D405/12 ,  C07D405/14 ,  C07C53/10 ,  C07D471/04 ,  C07C215/40 ,  C07C53/06 ,  C07D413/14

摘要： 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：US20190119255A1

公开(公告)日：2019-04-25

申请号：US16220184

申请日：2018-12-14

申请人： Pfizer Inc.

发明人： 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分类号： 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

摘要： 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：US20240132483A1

公开(公告)日：2024-04-25

申请号：US18513752

申请日：2023-11-20

申请人： Pfizer Inc.

发明人： Gary Erik Aspnes ,  Scott W. Bagley ,  Edward L. Conn ,  John M. Curto ,  David J. Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David A. Griffith ,  Kim Huard ,  Chris Limberakis ,  Alan M. Mathiowetz ,  David W. Piotrowski ,  Roger B. Ruggeri

IPC分类号： C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

CPC分类号： C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

摘要： 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：US20230124938A1

公开(公告)日：2023-04-20

申请号：US18049052

申请日：2022-10-24

申请人： Pfizer Inc.

发明人： 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分类号： 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

摘要： 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：US20230045419A1

公开(公告)日：2023-02-09

申请号：US17782478

申请日：2020-12-07

申请人： Pfizer Inc.

发明人： Gary E. Aspnes ,  Scott W. Bagley ,  Wesley Dewitt Clark ,  John M. Curto ,  David James Edmonds ,  Mark E. Flanagan ,  Kentaro Futatsugi ,  David Andrew Griffith ,  Kim Huard ,  Yajing Lian ,  Chris Limberakis ,  Allyn T. Londregan ,  Alan M. Mathiowetz ,  David Walter Piotrowski ,  Roger B. Ruggeri

IPC分类号： C07D405/14

摘要： The invention provides solid forms of 2-((4-((S)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt for example, a hydrate (e.g. a monohydrate) crystalline form (e.g. Form 2 or Form 3) or an amorphous form; 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：US20210163455A1

公开(公告)日：2021-06-03

申请号：US17171385

申请日：2021-02-09

申请人： Pfizer Inc.

发明人： 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分类号： C07D405/12 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

摘要： 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.