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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.
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![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](/abs-image/US/2023/02/09/US20230045419A1/abs.jpg.150x150.jpg)
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.
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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.
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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.
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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.
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Patent Agency Ranking
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.
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公开(公告)号：US20240059679A1
公开(公告)日：2024-02-22
申请号：US18483311
申请日：2023-10-09
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
CPC classification number: C07D405/12 , C07C53/06 , C07C53/10 , C07C215/40 , C07D405/14 , C07D413/14 , C07D471/04 , C07B2200/13
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.
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公开(公告)号：US20240034725A1
公开(公告)日：2024-02-01
申请号：US18477050
申请日：2023-09-28
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
CPC classification number: 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.
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公开(公告)号：US20220387402A1
公开(公告)日：2022-12-08
申请号：US17612672
申请日：2020-05-15
Applicant: Pfizer Inc.
Inventor： Gary E. Aspnes , Scott W. Bagley , John M. Curto , Matthew Dowling , David James Edmonds , Dilinie Fernando , Mark E. Flanagan , Kentaro Futatsugi , David Andrew Griffith , Kim Huard , Gajendra Ingle , Wenhua Jiao , Shawn M. LaCasse , Yajing Lian , Chris Limberakis , Allyn T. Londregan , Alan M. Mathiowetz , David Walter Piotrowski , Roger B. Ruggeri , Kristin Wiglesworth
IPC: A61K31/438 , A61K31/496 , A61K31/4545 , A61K31/454 , A61K31/5377 , A61K31/506 , A61K31/46 , A61K45/06 , A61K38/26 , A61K38/28 , A61K38/17 , A61P1/16
Abstract: In part, the invention provides a new combination comprising (1) a GLP-1R agonist and (2) an ACC inhibitor or a DGAT2 inhibitor, or a KHK inhibitor or FXR agonist. The invention further provides new methods for treating diseases and disorders, for example, fatty liver, nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, nonalcoholic steatohepatitis with liver fibrosis, nonalcoholic steatohepotitis with cirrhosis, and nonalcoholic steatohepatitis with cirrhosis and with hepatocellular carcinoma or with a metabolic-related disease, obesity, and type 2 diabetes, for example, using the new combination described herein.
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公开(公告)号：US10851081B2
公开(公告)日：2020-12-01
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 , C07D471/04 , 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 , A61K31/496
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.
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