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：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：US11981696B2

公开(公告)日：2024-05-14

申请号：US16980616

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Tamim Fehme Braish ,  Matthew Frank Brown ,  Ye Che ,  Richard Andrew Ewin ,  Timothy Allan Johnson ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Mark Stephen Plummer ,  Loren Michael Price ,  Usa Reilly ,  Daniel Uccello

IPC: C07F9/58 ,  A61P31/04 ,  C07F5/02

CPC classification number: C07F9/58 ,  A61P31/04 ,  C07F5/022

Abstract: The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III




wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US11472809B2

公开(公告)日：2022-10-18

申请号：US17014533

申请日：2020-09-08

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: A61K31/4985 ,  C07D487/04

Abstract: There is a method for treating a psoriasis. A compound is administered in a therapeutically effective amount to a subject suffering therefrom. The compound has the structure or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.

公开(公告)号：US11254668B2

公开(公告)日：2022-02-22

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 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D519/00

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：US11198692B2

公开(公告)日：2021-12-14

申请号：US16625202

申请日：2018-06-14

Applicant: Pfizer Inc.

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

IPC: C07D471/04

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)a, (R2)b, (R3)c, 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：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：US20210017206A1

公开(公告)日：2021-01-21

申请号：US16980473

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ye Che ,  Anthony Marfat ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Timothy Allan Johnson ,  Richard Andrew Ewin ,  Daniel Paul Uccello ,  Usa Reilly ,  Tamim Fehme Braish

IPC: C07F9/6558 ,  C07F9/58 ,  C07F5/04 ,  A61P31/04

Abstract: The present invention is directed to new pyridinone or pyrimidinone hydroxamic acid phosphates of Formula (1) and boronates of Formula (2), stereoisomers thereof; wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation; X is CH or N; and Z is as defined herein; and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US20210017205A1

公开(公告)日：2021-01-21

申请号：US16980616

申请日：2019-03-14

Applicant: Pfizer Inc.

Inventor： Tamim Fehme Braish ,  Matthew Frank Brown ,  Ye Che ,  Richard Andrew Ewin ,  Timothy Allan Johnson ,  Michael Joseph Melnick ,  Justin Ian Montgomery ,  Mark Stephen Plummer ,  Loren Michael Price ,  Usa Reilly ,  Daniel Uccello

IPC: C07F9/58 ,  C07F5/02 ,  A61P31/04

Abstract: The present invention is directed to a new fluoro-pyridinone hydroxamic acid phosphates and boronates of Formulae I, II and III wherein Q is selected from the group consisting of —P(O)(OH)2, —P(O)(OH)(O−M+), —P(O)(O−M+)2 and —P(O)(O−)2M2+; M+ at each occurrence is a pharmaceutically acceptable monovalent cation; and M2+ is a pharmaceutically acceptable divalent cation and their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

公开(公告)号：US20180002331A1

公开(公告)日：2018-01-04

申请号：US15637071

申请日：2017-06-29

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

CPC classification number: C07D471/04

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.