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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.
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公开(公告)号：US20210047298A1
公开(公告)日：2021-02-18
申请号：US17085534
申请日：2020-10-30
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：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.
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公开(公告)号：US20190119255A1
公开(公告)日：2019-04-25
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: C07D401/14 , A61K31/4545 , A61P43/00 , A61P1/16 , A61P25/02 , A61P3/04 , A61P19/02 , A61P3/10 , A61P13/12 , A61P25/18 , A61P1/00 , A61P15/00 , A61P25/16 , C07D405/14 , C07D471/04 , A61P15/10 , A61P3/00 , C07D487/04 , C07D413/14 , A61P17/06 , A61P9/10 , A61P19/06 , A61P25/28 , A61P25/30 , 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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公开(公告)号：US20150266861A1
公开(公告)日：2015-09-24
申请号：US14731632
申请日：2015-06-05
Applicant: Pfizer Inc.
Inventor： Gary Erik Aspnes , Mary Theresa Didiuk , Kevin James Filipski , Angel Guzman-Perez , Jeffrey Allen Pfefferkorn , Benjamin Dawson Stevens , Meihua Mike Tu
IPC: C07D405/12 , C07D239/42 , C07D237/08 , C07D403/12 , C07D401/12 , C07D213/82 , C07D241/34
CPC classification number: C07D405/12 , A61K31/44 , A61K31/4427 , C07D213/74 , C07D213/81 , C07D213/82 , C07D237/08 , C07D239/42 , C07D241/28 , C07D241/34 , C07D401/12 , C07D403/12
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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Patent Agency Ranking
公开(公告)号：US11802121B2
公开(公告)日：2023-10-31
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: 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
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.
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公开(公告)号：US11512070B2
公开(公告)日：2022-11-29
申请号：US17085534
申请日：2020-10-30
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：US10208019B2
公开(公告)日：2019-02-19
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: C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D401/14 , A61K31/496 , A61K31/4545 , 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 , A61P3/00
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：US20150266859A1
公开(公告)日：2015-09-24
申请号：US14730562
申请日：2015-06-04
Applicant: Pfizer Inc.
Inventor： Gary Erik Aspnes , Mary Theresa Didiuk , Kevin James Filipski , Angel Guzman-Perez , Esther Cheng Yin Lee , Jeffrey Allen Pfefferkorn , Benjamin Dawson Stevens , Meihua Mike Tu
IPC: C07D403/04 , C07D401/04
CPC classification number: C07D401/04 , A61K31/506 , C07D207/34 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D231/56 , C07D233/61 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/84 , C07D239/28 , C07D249/06 , C07D249/08 , C07D261/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D487/04
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R1，R2，R3，A1，A2，A3，A4，L，B1，B2，B3和B4如本文所定义。 已经发现式I的化合物用作胰高血糖素拮抗剂或反向激动剂。 因此，式I化合物及其药物组合物可用于治疗由胰高血糖素介导的疾病，病症或病症。
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公开(公告)号：US20140371467A1
公开(公告)日：2014-12-18
申请号：US14471576
申请日：2014-08-28
Applicant: Pfizer Inc.
Inventor： Gary Erik Aspnes , Mary Theresa Didiuk , Kevin James Filipski , Angel Guzman-Perez , Esther Cheng Yin Lee , Jeffrey Allen Pfefferkorn , Benjamin Dawson Stevens , Meihua Mike Tu
IPC: C07D231/12
CPC classification number: C07D401/04 , A61K31/506 , C07D207/34 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/54 , C07D231/56 , C07D233/61 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/84 , C07D239/28 , C07D249/06 , C07D249/08 , C07D261/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D487/04
Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R1，R2，R3，A1，A2，A3，A4，L，B1，B2，B3和B4如本文所定义。 已经发现式I的化合物用作胰高血糖素拮抗剂或反向激动剂。 因此，式I化合物及其药物组合物可用于治疗由胰高血糖素介导的疾病，病症或病症。
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