公开(公告)号：US20210163455A1

公开(公告)日：2021-06-03

申请号：US17171385

申请日：2021-02-09

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

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：US20200255406A1

公开(公告)日：2020-08-13

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 ,  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：US10676465B2

公开(公告)日：2020-06-09

申请号：US16535616

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 ,  C07D471/04 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  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.

公开(公告)号：US10669259B2

公开(公告)日：2020-06-02

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: 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

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：US20160058768A1

公开(公告)日：2016-03-03

申请号：US14939264

申请日：2015-11-12

Applicant: Pfizer Inc.

Inventor： Etzer Darout ,  Robert Dullea ,  Julie Jia Li Hawkins ,  Allyn T. Londregan ,  Paula M. Loria ,  Bruce Maguire ,  Kim F. McClure ,  Donna N. Petersen ,  David W. Piotrowski

IPC: A61K31/519 ,  A61K31/4725 ,  A61K31/4545

CPC classification number: A61K31/519 ,  A61K31/4545 ,  A61K31/4725 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention is directed at substituted amide compounds, pharmaceutical compositions containing such compounds and the use of such compounds to reduce plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract translation: 本发明涉及取代的酰胺化合物，含有这些化合物的药物组合物以及这些化合物用于降低血浆脂质水平的用途，例如LDL-胆固醇和甘油三酸酯，并因此治疗由高水平的LDL-胆固醇加重的疾病， 甘油三酸酯，如动脉粥样硬化和心血管疾病，包括人在内的哺乳动物。