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：US09035074B2

公开(公告)日：2015-05-19

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: C07D207/18 ,  C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。

公开(公告)号：US09018384B2

公开(公告)日：2015-04-28

申请号：US14447788

申请日：2014-07-31

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ye Che ,  Anthony Marfat ,  Michael Joesph Melnick ,  Justin Ian Montgomery ,  Usa Reilly

IPC: A61K31/44 ,  C07D401/00 ,  C07D213/64 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D211/86 ,  C07D403/04 ,  C07D401/14

CPC classification number: A61K31/4412 ,  A61K31/4439 ,  C07D211/86 ,  C07D213/64 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  Y02A50/473

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

公开(公告)号：US20140343031A1

公开(公告)日：2014-11-20

申请号：US14447788

申请日：2014-07-31

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ye Che ,  Anthony Marfat ,  Michael Joesph Melnick ,  Justin Ian Montgomery ,  Usa Reilly

IPC: C07D213/64 ,  C07D401/12 ,  C07D401/14 ,  C07D401/04 ,  C07D413/10 ,  C07D401/10 ,  C07D405/04

CPC classification number: A61K31/4412 ,  A61K31/4439 ,  C07D211/86 ,  C07D213/64 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  Y02A50/473

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

Abstract translation: 本发明涉及一类新的异羟肟酸衍生物，它们用作LpxC抑制剂，更具体地说是它们用于治疗细菌感染的用途。

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：US20240190869A1

公开(公告)日：2024-06-13

申请号：US18532547

申请日：2023-12-07

Applicant: Pfizer Inc.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28

Abstract: The present invention provides, in part, compounds of Formula I:




or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

公开(公告)号：US20210309659A1

公开(公告)日：2021-10-07

申请号：US17335666

申请日：2021-06-01

Applicant: PFIZER INC.

Inventor： Lei Zhang ,  Christopher Ryan Butler ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Matthew Frank Brown ,  Laura Ann McAllister ,  Erik Alphie LaChapelle ,  Adam Matthew Gilbert

IPC: C07D471/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61K31/437

Abstract: The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R1, R2, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

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.

公开(公告)号：US08846933B2

公开(公告)日：2014-09-30

申请号：US14154239

申请日：2014-01-14

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ye Che ,  Anthony Marfat ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Usa Reilly

IPC: A61K31/44 ,  C07D401/00 ,  C07D409/04 ,  C07D417/12 ,  C07D405/10 ,  C07D417/10 ,  C07D405/04 ,  C07D213/64 ,  C07D417/04 ,  C07D211/86 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D413/12 ,  C07D401/08 ,  C07D413/10 ,  C07D401/12

CPC classification number: A61K31/4412 ,  A61K31/4439 ,  C07D211/86 ,  C07D213/64 ,  C07D401/04 ,  C07D401/08 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  Y02A50/473

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

Abstract translation: 本发明涉及一类新的异羟肟酸衍生物，它们用作LpxC抑制剂，更具体地说是它们用于治疗细菌感染的用途。

公开(公告)号：US20140243312A1

公开(公告)日：2014-08-28

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez

IPC: C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。