公开(公告)号：US20250134869A1

公开(公告)日：2025-05-01

申请号：US18772655

申请日：2024-07-15

Applicant: Pfizer Inc

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo

IPC: A61K31/437 ,  A61K31/439 ,  A61K31/519 ,  A61K31/551

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

公开(公告)号：US12077533B2

公开(公告)日：2024-09-03

申请号：US17393463

申请日：2021-08-04

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I Trujillo

IPC: A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC classification number: C07D471/04 ,  A61K31/4523 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure:




or a pharmaceutically acceptable salt thereof, as set forth in the Description.

公开(公告)号：US11661419B2

公开(公告)日：2023-05-30

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 ,  A61P17/00 ,  A61K45/06

CPC classification number: 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：US11111242B2

公开(公告)日：2021-09-07

申请号：US15446500

申请日：2017-03-01

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo

IPC: A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

公开(公告)号：US11702405B2

公开(公告)日：2023-07-18

申请号：US17227819

申请日：2021-04-12

Applicant: Pfizer Inc.

Inventor： Ariamala Gopalsamy ,  Shawn Cabral ,  Agustin Casimiro-Garcia ,  Ming Zhu Chen ,  Chulho Choi ,  Robert Lee Dow ,  Olugbeminiyi Omezia Fadeyi ,  David Hepworth ,  Jayasankar Jasti ,  Lyn Howard Jones ,  Arjun Venkat Narayanan ,  Mihir Dineshkumar Parikh ,  David Walter Piotrowski ,  Lee Richard Roberts ,  Ralph Pelton Robinson, Jr. ,  Hatice Gizem Yayla

IPC: C07D401/14 ,  A61P7/06 ,  C07D471/04 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61P7/06 ,  C07D471/04 ,  A61K45/06

Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
More particularly the invention relates to HbS modulators of formula (I)




or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description.

HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).

公开(公告)号：US20220348555A1

公开(公告)日：2022-11-03

申请号：US17227819

申请日：2021-04-12

Applicant: Pfizer Inc.

Inventor： Ariamala Gopalsamy ,  Shawn Cabral ,  Agustin Casimiro-Garcia ,  Ming Zhu Chen ,  Chulho Choi ,  Robert Lee Dow ,  Olugbeminiyi Omezia Fadeyi ,  David Hepworth ,  Jayasankar Jasti ,  Lyn Howard Jones ,  Arjun Venkat Narayanan ,  Mihir Dineshkumar Parikh ,  David Walter Piotrowski ,  Lee Richard Roberts ,  Ralph Pelton Robinson, Jr. ,  Hatice Gizem Yayla

IPC: C07D401/14 ,  A61P7/06 ,  C07D471/04

Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description.
HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).

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：US20190315715A1

公开(公告)日：2019-10-17

申请号：US16316688

申请日：2017-07-07

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Joseph Walter Strohbach ,  David Hepworth ,  Frank Eldridge Lovering ,  Chulho Choi ,  Christophe Philippe Allais ,  Stephen Wayne Wright

IPC: C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/10 ,  C07D498/18

Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20170247372A1

公开(公告)日：2017-08-31

申请号：US15446500

申请日：2017-03-01

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo

IPC: C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D471/08 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

公开(公告)号：US09617258B2

公开(公告)日：2017-04-11

申请号：US14559294

申请日：2014-12-03

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Jotham Wadsworth Coe ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jonathan David Langille ,  Justin Ian Montgomery ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo

IPC: A61K31/519 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.