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：US09227956B2

公开(公告)日：2016-01-05

申请号：US14253084

申请日：2014-04-15

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: C07D401/14 ,  A61K31/519 ,  A61K45/06 ,  C07D413/14 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4545 ,  C07D487/04 ,  C07D471/04

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。

公开(公告)号：US20240140937A1

公开(公告)日：2024-05-02

申请号：US18520638

申请日：2023-11-28

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 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/06

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：US10934279B2

公开(公告)日：2021-03-02

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 ,  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：US20190382388A1

公开(公告)日：2019-12-19

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 ,  C07C53/10 ,  C07D471/04 ,  C07C215/40 ,  C07C53/06 ,  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：US20140080756A1

公开(公告)日：2014-03-20

申请号：US14083275

申请日：2013-11-18

Applicant: Pfizer Inc.

Inventor： Samit K. Bhattacharya ,  Kimberly O. Cameron ,  Dilinie P. Fernando ,  Kim F. McClure ,  Daniel W. Kung ,  Allyn T. Londregan ,  Suvi T.M. Orr

IPC: C07D471/10 ,  A61K31/506 ,  A61K31/53 ,  A61K31/435 ,  A61K31/497 ,  C07D491/056 ,  C07D513/04 ,  A61K45/06

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K45/06 ,  C07D491/056 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention provides a compound of Formula (I) a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.

Abstract translation: 本发明提供了其作为Ghrelin拮抗剂或反向激动剂的其中R 1，R 2，R a，L，Z，Z 1和Z 2如本文所定义的药用盐的式（I）化合物; 其药物组合物; 以及治疗由Ghrelin受体的拮抗作用介导的疾病，病症或病症的方法。

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：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：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.