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公开(公告)号:US20240150334A1
公开(公告)日:2024-05-09
申请号:US18482129
申请日:2023-10-06
Applicant: Pfizer Inc.
Inventor: Jan Antoinette Cusi Romero Adams , Bruce Michael Bechle , Jason Kenneth Dutra , Michelle Renee Garnsey , Xinjun Hou , Jisun Lee , Deane Milford Nason, II , Steven Victor O'Neil , Danica Antonia Rankic , Yang Wang , Ann Sorrentino Wright , Lei Zhang , Liying Zhang , David James Edmonds
IPC: C07D413/04 , C07D231/56 , C07D263/56 , C07D401/04 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04
CPC classification number: C07D413/04 , C07D231/56 , C07D263/56 , C07D401/04 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04
Abstract: Described herein are compounds of Formula I,
wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.-
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:US20220193063A1
公开(公告)日:2022-06-23
申请号:US17546228
申请日:2021-12-09
Applicant: Pfizer Inc.
IPC: A61K31/4545 , C07D405/14 , A61K31/506
Abstract: The present invention provides metabolites of Compound 1 or a compound of Formula I or 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 or III.
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公开(公告)号:US10683281B2
公开(公告)日:2020-06-16
申请号:US16535553
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 , C07C53/06 , C07C53/10 , C07C215/40 , 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: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.
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公开(公告)号:US20240391908A1
公开(公告)日:2024-11-28
申请号:US18789977
申请日:2024-07-31
Applicant: Pfizer Inc.
Inventor: Andrew John Bessire , David James Edmonds , David Andrew Griffith , Amit Sumant Kalgutkar , Timothy Frank Ryder
IPC: C07D405/14 , A61K45/06 , 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.
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17.
公开(公告)号:US20230405002A1
公开(公告)日:2023-12-21
申请号:US17904554
申请日:2021-02-22
Applicant: Pfizer Inc.
Inventor: Neeta Balkrishan Amin , Arthur James Bergman , Roberto Arnaldo Calle , Robert Gregory Dullea , David James Edmonds , William Paul Esler , Kevin James Filipski , James Richard Gosset , Albert Myung Kim , Jeffrey Allen Pfefferkorn , Patrick Robert Verhoest
IPC: A61K31/506 , A61K31/4545 , A61P1/16 , A61P3/04
CPC classification number: A61K31/506 , A61K31/4545 , A61P1/16 , A61P3/04
Abstract: Described herein are pharmaceutical compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto. Also described are compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto.
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公开(公告)号:US11471458B2
公开(公告)日:2022-10-18
申请号:US17062982
申请日:2020-10-05
Applicant: Pfizer Inc.
Inventor: David James Edmonds , Kevin James Filipski , Kentaro Futatsugi , Michelle Renee Garnsey , Jack Chang Hung Lee , Daniel Jonathan Smaltz
IPC: A61K31/506 , A61P3/06 , A61K31/155 , A61K31/4545 , C07D401/14 , A61K31/4985 , A61K31/7048 , A61K45/06
Abstract: Described herein are compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.
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公开(公告)号:US20210100798A1
公开(公告)日:2021-04-08
申请号:US17090619
申请日:2020-11-05
Applicant: Pfizer Inc.
Inventor: David James Edmonds , Kevin James Filipski , Kentaro Futatsugi , Michelle Renee Garnsey , Jack Chang Hung Lee , Daniel Jonathan Smaltz
IPC: A61K31/506 , A61K31/4545 , A61K31/155 , A61K31/7048 , A61K31/4985 , A61P3/06 , C07D401/14 , A61K45/06
Abstract: Described herein are compounds of Formula (1) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.
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公开(公告)号:US20210100796A1
公开(公告)日:2021-04-08
申请号:US17062982
申请日:2020-10-05
Applicant: Pfizer Inc.
Inventor: David James Edmonds , Kevin James Filipski , Kentaro Futatsugi , Michelle Renee Garnsey , Jack Chang Hung Lee , Daniel Jonathan Smaltz
IPC: A61K31/506 , C07D401/14 , A61K45/06 , A61P3/06 , A61K31/155 , A61K31/4985 , A61K31/7048 , A61K31/4545
Abstract: Described herein are compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein, their use as diacylglycerol acyltransferase 2 (DGAT2) inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, NASH.
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