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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:US20230280220A1
公开(公告)日:2023-09-07
申请号:US18301475
申请日:2023-04-17
Applicant: Pfizer Inc.
Inventor: Scott William Bagley , Agustin Casimiro Garcia , Xiayun Cheng , Jennifer Elizabeth Davoren , Rajiah Aldrin Denny , Brian Stephen Gerstenberger , Frank Eldridge Lovering , Mihir Dineshkumar Parikh , Joseph Walter Strohbach , John Isidro Trujillo
IPC: G01L1/25 , G01N23/207
CPC classification number: G01L1/25 , G01N23/207
Abstract: The invention relates to benzimidazoles of Formula (1)
and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (1) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.-
公开(公告)号:US20210206757A1
公开(公告)日:2021-07-08
申请号:US17192968
申请日:2021-03-05
Applicant: Pfizer Inc.
Inventor: Brian Stephen Gerstenberger , Andrew Christopher Flick , Daniel Wei-Shung Kung , Vincent Michael Lombardo , James John Mousseau , Philippe Marcel Nuhant , Ralph Pelton Robinson, JR. , Daniel Copley Schmitt , Mark Edward Schnute , Atli Thorarensen , John Isidro Trujillo , Rayomand Jal Unwalla , Huixian Wu
IPC: C07D413/14 , A61P29/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07F9/6558
Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
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公开(公告)号:US20200172537A1
公开(公告)日:2020-06-04
申请号:US16638271
申请日:2018-08-09
Applicant: Pfizer Inc.
Inventor: Brian Stephen Gerstenberger , Andrew Fensome , Dafydd Rhys Owen , Matthew Frank Brown , Matthew Merrill Hayward , Felix Vajdos , Li Huang Xing , Stephen Wayne Wright
IPC: C07D471/04 , C07D519/00 , C07D401/14 , C07D405/14 , C07D401/04
Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
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公开(公告)号:US20240336572A1
公开(公告)日:2024-10-10
申请号:US18626467
申请日:2024-04-04
Applicant: Pfizer Inc.
Inventor: Samit Kumar Bhattacharya , Edward Lee Conn , David Christopher Ebner , Brian Stephen Gerstenberger , Chan Woo Huh , Daniel Wei-Shung Kung , Alan Martin Mathiowetz , Jessica Gloria Katherine O'Brien , Meihua Mike Tu , Kimberly O'Keefe Cameron , Dilinie Prasadhini Fernando , Kevin James Filipski , Esther Cheng Yin Lee , Sarah Jane Mear , Aaron Christopher Smith
IPC: C07D231/56 , A61K31/416
CPC classification number: C07D231/56 , A61K31/416
Abstract: The invention relates to substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof that can activate adenosine 5′-monophosphate-activated protein kinase (AMPK). The invention further relates to pharmaceutical compositions comprising AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof and at least one pharmaceutically acceptable excipient, and methods of treating a condition comprising administering AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof.
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公开(公告)号:US20240245673A1
公开(公告)日:2024-07-25
申请号:US18532424
申请日:2023-12-07
Applicant: Pfizer Inc.
Inventor: James Matthew Frick , Michelle Renee Garnsey , Brian Stephen Gerstenberger , Xinjun Hou , Magdalena Korczynska , Alpha Albert Lee , Luong Tien Nguyen , Usa Reilly , Matthew Christopher Robinson , Alexandria Paige Taylor , Thomas Reynold Vargo , Lei Zhang
IPC: A61K31/4709 , A61K31/415 , A61K31/4178 , A61K31/4192 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D207/34 , C07D215/38 , C07D231/12 , C07D249/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D495/04
CPC classification number: A61K31/4709 , A61K31/415 , A61K31/4178 , A61K31/4192 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D207/34 , C07D215/38 , C07D231/12 , C07D249/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D495/04
Abstract: The invention relates to compounds of Formula (I)
and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.-
公开(公告)号:US20210188829A1
公开(公告)日:2021-06-24
申请号:US17126358
申请日:2020-12-18
Applicant: Pfizer Inc.
Inventor: Scott William Bagley , Agustin Casimiro-Garcia , Xiayun Cheng , Jennifer Elizabeth Davoren , Rajiah Aldrin Denny , Brian Stephen Gerstenberger , Frank Eldridge Lovering , Mihir Dineshkumar Parikh , Joseph Walter Strohbach , John Isidro Trujillo
IPC: C07D413/14 , A61K45/06 , A61P17/00
Abstract: The invention relates to benzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.-
公开(公告)号:US10975065B2
公开(公告)日:2021-04-13
申请号:US16576997
申请日:2019-09-20
Applicant: Pfizer Inc.
Inventor: Brian Stephen Gerstenberger , Andrew Christopher Flick , Vincent Michael Lombardo , James John Mousseau , Philippe Marcel Nuhant , Ralph Pelton Robinson, Jr. , Mark Edward Schnute , Daniel Wei-Shung Kung , Daniel Copley Schmitt , Atli Thorarensen , John Isidro Trujillo , Rayomand Jal Unwalla , Huixian Wu
IPC: C07D413/14 , A61P29/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07F9/6558
Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
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19.
公开(公告)号:US20200095239A1
公开(公告)日:2020-03-26
申请号:US16576997
申请日:2019-09-20
Applicant: Pfizer Inc.
Inventor: Brian Stephen Gerstenberger , Andrew Christopher Flick , Vincent Michael Lombardo , James John Mousseau , Philippe Marcel Nuhant , Ralph Pelton Robinson, JR. , Mark Edward Schnute , Daniel Wei-Shung Kung , Daniel Copley Schmitt , Atli Thorarensen , John Isidro Trujillo , Rayomand Jal Unwalla , Huixian Wu
IPC: C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D413/12 , C07D405/14 , C07D417/14 , C07F9/6558 , A61P29/00
Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
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公开(公告)号:US10144738B2
公开(公告)日:2018-12-04
申请号:US15437618
申请日:2017-02-21
Applicant: Pfizer Inc.
Inventor: Matthew Frank Brown , Alpay Dermenci , Andrew Fensome , Brian Stephen Gerstenberger , Matthew Merrill Hayward , Dafydd Rhys Owen , Stephen Wayne Wright , Li Huang Xing , Xiaojing Yang
IPC: C07D487/04 , A61K31/4985
Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, wherein A, A′ and A″ are independently O, C═O, etc.; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, etc.; R6, R7 and R8 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl), etc.; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
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