公开(公告)号：US11542270B2

公开(公告)日：2023-01-03

申请号：US16912828

申请日：2020-06-26

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04 ,  A61K31/155 ,  A61K31/4985 ,  A61K31/7048 ,  A61K45/06

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US20220213072A1

公开(公告)日：2022-07-07

申请号：US17546207

申请日：2021-12-09

Applicant: Pfizer Inc.

Inventor： Andrew John Bessire ,  David James Edmonds ,  David Andrew Griffith ,  Amit Sumant Kalgutkar ,  Timothy Frank Ryder

IPC: C07D405/14 ,  C07D401/14

Abstract: The present invention provides compounds of Formula XA-1, XA-2, XA-3, XA-4, XA-5, or XA-6, or metabolites of Compound 1 or metabolites of a compound of Formula I, PA-I, or PA-III, including compositions and salts thereof, which are useful in the prevention and/or treatment of a disease or disorder such as T2DM, obesity, or NASH, as well as analytical methods related to the administration of Compound 1 or a compound of Formula I, PA-1, or PA-III.

公开(公告)号：US20210087204A1

公开(公告)日：2021-03-25

申请号：US17078257

申请日：2020-10-23

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US10822335B2

公开(公告)日：2020-11-03

申请号：US16371896

申请日：2019-04-01

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  A61K31/435

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US11673890B2

公开(公告)日：2023-06-13

申请号：US17034295

申请日：2020-09-28

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: A61K31/435 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (1)




or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

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：US20210024536A1

公开(公告)日：2021-01-28

申请号：US16912828

申请日：2020-06-26

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US20180162858A1

公开(公告)日：2018-06-14

申请号：US15883109

申请日：2018-01-30

Applicant: PFIZER INC.

Inventor： Mary Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  A61K31/519 ,  C07D491/20 ,  A61K31/435 ,  A61K31/438 ,  C07D519/00 ,  A61K45/06 ,  C07D487/10

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US09139587B2

公开(公告)日：2015-09-22

申请号：US14273912

申请日：2014-05-09

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  David Andrew Griffith ,  Daniel Wei-Shung Kung

IPC: C07D471/10 ,  C07D519/00

CPC classification number: C07D471/10 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

公开(公告)号：US08802690B2

公开(公告)日：2014-08-12

申请号：US13939450

申请日：2013-07-11

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  David Andrew Griffith ,  Daniel Wei-Shung Kung

IPC: C07D487/10 ,  A61K31/438

CPC classification number: C07D471/10 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。