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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: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:US20240109915A1
公开(公告)日:2024-04-04
申请号:US18359709
申请日:2023-07-26
Applicant: Pfizer Inc.
Inventor: Scott William Bagley , Andrea Nicole Bootsma , Chulho Choi , Robert Lee Dow , David James Edmonds , Carmen Noemi Garcia-Irizarry , Brian Stephen Gerstenberger , Gajendra Ingle , Jessica Gloria Katherine O'Brien , Mihir Dineshkumar Parikh , Gwenaella Christine Rescourio , Daniel Copley Schmitt
IPC: C07D513/10
CPC classification number: C07D513/10
Abstract: A compound having the structures:
or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein; R selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy and —(CH2)m—W, where W is C3-C8 cycloalkyl, bicycloalkyl, bridged bicycloalkyl, phenyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said alkyl, cycloalkyl, alkoxy, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R′, —SO2NR′R″, NR′R″ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; R1 selected from the group consisting of phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two, three or four heteroatoms selected from the group consisting of N, S and O atoms; and, a 9- or 10-membered bicyclic aryl, heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said phenyl, naphthyl, aryl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, phenyl, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R, —SO2NR′R″, —P(O)R′R″,
or NR′R″′ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly acne.-
公开(公告)号:US20180170908A1
公开(公告)日:2018-06-21
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: C07D401/14 , C07D471/04 , C07D405/14 , C07D413/14 , A61P3/10 , A61P25/28 , A61P25/02 , A61P13/12 , A61P43/00 , A61P3/04 , A61P1/16 , A61P9/10 , A61P19/02 , A61P25/16 , A61P19/06 , A61P15/10 , A61P17/06 , A61P25/18 , A61P1/00 , A61P15/00 , A61P25/30
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: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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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: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: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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