公开(公告)号：US11858916B2

公开(公告)日：2024-01-02

申请号：US17251929

申请日：2019-06-13

Applicant: Pfizer Inc.

Inventor： 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: C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  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：US20210332034A1

公开(公告)日：2021-10-28

申请号：US17251929

申请日：2019-06-13

Applicant: Pfizer Inc.

Inventor： 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: C07D405/14 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D403/14

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：US10683281B2

公开(公告)日：2020-06-16

申请号：US16535553

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 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40 ,  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：US20190382384A1

公开(公告)日：2019-12-19

申请号：US16436311

申请日：2019-06-10

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 ,  C07D471/04 ,  C07D405/14 ,  C07D413/14 ,  C07C53/06 ,  C07C53/10 ,  C07C215/40

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：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：US20140206651A1

公开(公告)日：2014-07-24

申请号：US14223061

申请日：2014-03-24

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Charles Francis Donovan ,  Edmund Lee Ellsworth ,  Denton Wade Hoyer ,  Timothy Allan Johnson ,  Manjinder Singh Lall ,  Chris Limberakis ,  Sean Timothy Murphy ,  Debra Ann Sherry ,  Clarke Bentley Taylor ,  Joseph Scott Warmus

IPC: C07C259/06 ,  C07D213/55 ,  C07F9/653 ,  C07D261/08 ,  C07D239/26 ,  C07D277/30 ,  C07D233/64 ,  C07D307/54

CPC classification number: C07C259/06 ,  C07C2601/04 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D213/55 ,  C07D231/12 ,  C07D233/64 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D307/54 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中：G为式（II）的基团：及其药学上可接受的盐，前体药物，水合物或溶剂合物，其中A， B，L1-L4，A，B，R1-R4和m如本文所定义。 本发明还涉及包含式（I）化合物及其在治疗细菌感染中的用途的药物组合物。