公开(公告)号：US20240124439A1

公开(公告)日：2024-04-18

申请号：US18257195

申请日：2021-12-13

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  Agustin Casimiro-Garcia ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Katherine Lin Lee ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The invention relates to imidazopyridines of Formula (I)




and pharmaceutically acceptable salts thereof, wherein R0 to R5 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：US20230009153A1

公开(公告)日：2023-01-12

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: C07D471/04 ,  A61K31/4523 ,  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：US10906888B2

公开(公告)日：2021-02-02

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：US20200172512A1

公开(公告)日：2020-06-04

申请号：US16695709

申请日：2019-11-26

Applicant: Pfizer Inc.

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

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

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：US20160368919A1

公开(公告)日：2016-12-22

申请号：US15184097

申请日：2016-06-16

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Bruce Allen Lefker ,  Nikolaos Papaioannou ,  Arjun Venkat Narayanan ,  Jotham Wadsworth Coe

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Disclosed are novel pyridine pyrazinones or pharmaceutically acceptable salts thereof. Pharmaceutical compositions and the use of the compounds to treat diseases or disorders that are BET family bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.

Abstract translation: 公开了新的吡啶吡嗪酮或其药学上可接受的盐。 还公开了药物组合物和化合物用于治疗作为BET家族溴结构域依赖性的疾病或病症的用途。 进一步描述制备和使用这些化合物的方法。

公开(公告)号：US20150158864A1

公开(公告)日：2015-06-11

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

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

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.

Abstract translation: 本发明提供药学活性吡咯并[2,3-d]嘧啶基和吡咯并[2,3-d]吡啶基丙烯酰胺及其类似物。 这些化合物可用于抑制Janus Kinase（JAK）。 本发明还涉及包含制备这种化合物的方法的组合物，以及用于治疗和预防由JAK介导的病症的方法。

公开(公告)号：US11014908B2

公开(公告)日：2021-05-25

申请号：US16695709

申请日：2019-11-26

Applicant: Pfizer Inc.

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

IPC: 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：US10703756B2

公开(公告)日：2020-07-07

申请号：US15569874

申请日：2016-04-19

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo ,  Sidney Xi Liang

IPC: C07D487/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, 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：US20190292157A1

公开(公告)日：2019-09-26

申请号：US16380256

申请日：2019-04-10

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Jeffrey Scott Condon ,  Andrew Christopher Flick ,  Ariamala Gopalsamy ,  Steven J. Kirincich ,  John Paul Mathias ,  Joseph Walter Strohbach ,  Jason Shaoyun Xiang ,  Li Huang Xing ,  Xiaolun Wang

IPC: C07D239/42 ,  A61P35/00 ,  A61P1/04 ,  A61P1/00 ,  C07D405/10 ,  A61K31/505 ,  C07D401/12 ,  C07D241/14 ,  C07D239/28 ,  C07D403/12

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

公开(公告)号：US10308615B2

公开(公告)日：2019-06-04

申请号：US15574625

申请日：2016-05-16

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Jeffrey Scott Condon ,  Andrew Christopher Flick ,  Ariamala Gopalsamy ,  Steven J. Kirincich ,  John Paul Mathias ,  Joseph Walter Strobach ,  Jason Shaoyun Xiang ,  Li Huang Xing ,  Xiaolun Wang

IPC: C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  A61K31/505 ,  C07D239/28 ,  C07D241/14 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  C07D405/10

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