公开(公告)号：US20230124938A1

公开(公告)日：2023-04-20

申请号：US18049052

申请日：2022-10-24

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：US20230045419A1

公开(公告)日：2023-02-09

申请号：US17782478

申请日：2020-12-07

Applicant: Pfizer Inc.

Inventor： 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: C07D405/14

Abstract: 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

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：US10071992B2

公开(公告)日：2018-09-11

申请号：US15674914

申请日：2017-08-11

Applicant: Pfizer Inc.

Inventor： 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: C07D401/00 ,  C07D253/08 ,  C07D401/04 ,  A61K9/14 ,  C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14 ,  C07D401/14

Abstract: 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：US20180051012A1

公开(公告)日：2018-02-22

申请号：US15674914

申请日：2017-08-11

Applicant: Pfizer Inc.

Inventor： 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: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07B2200/13 ,  C07D401/14 ,  C07D409/14

Abstract: 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：US09278953B2

公开(公告)日：2016-03-08

申请号：US14506752

申请日：2014-10-06

Applicant: Pfizer Inc.

Inventor： Kevin Barry Bahnck ,  David James Edmonds ,  Kentaro Futatsugi ,  Esther Cheng Yin Lee ,  Alan Martin Mathiowetz ,  Elnaz Menhaji-Klotz ,  Robert Vernon Stanton

IPC: C07D213/63 ,  A61K31/44 ,  C07D401/14

CPC classification number: C07D401/14

Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.

Abstract translation: 本文提供前列腺素EP3受体的拮抗剂，制备所述拮抗剂的方法，以及包括向有需要的哺乳动物施用所述拮抗剂的方法。

公开(公告)号：US20150087585A1

公开(公告)日：2015-03-26

申请号：US14384508

申请日：2013-03-26

Applicant: Pfizer Inc.

Inventor： Kay Ahn ,  Markus Boehm ,  Shawn Cabral ,  Philip A. Carpino ,  Kentaro Futatsugi ,  David Hepworth ,  Daniel W. Kung ,  Suvi Orr ,  Jian Wang

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  A61K31/437 ,  A61K31/506

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine 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.

Abstract translation: 抑制二酰基甘油酰基转移酶2（DGAT2）活性的式I的嘌呤衍生物，3H-咪唑并[4,5-b]嘧啶和1H-咪唑并[4,5-d]吡嗪及其在治疗疾病中的用途 本文描述了与动物相连的动物。