公开(公告)号：US20240238425A1

公开(公告)日：2024-07-18

申请号：US18541015

申请日：2023-12-15

Applicant: Pfizer Inc.

Inventor： Jan Antoinette Cusi Romero Adams ,  Yotam Ashkenazi ,  Matthew Frank Brown ,  Jason Kenneth Dutra ,  Michelle Renee Garnsey ,  Xinjun Hou ,  Jisun Lee ,  Yajing Lian ,  Deane Milford Nason, II ,  Steven Victor O'Neil ,  Amanda Brooke Pecora ,  Alistair Dean Richardson ,  Matthew Forrest Sammons ,  Yang Wang ,  Ann Sorrentino Wright ,  Jun Xiao ,  Lei Zhang ,  Liying Zhang

IPC: A61K47/55 ,  A61K45/06

CPC classification number: A61K47/55 ,  A61K45/06

Abstract: Described herein are 3-fluoro-4-hydroxybenzamide-containing inhibitors and/or degraders, and pharmaceutical compositions containing 3-fluoro-hydroxybenzamide-containing inhibitors and/or degraders. In some embodiments, the 3-fluoro-4-hydroxybenzamide-containing compounds of the disclosure can be used to treat a condition, for example, nonalcoholic fatty liver disease and nonalcoholic steatohepatitis.

公开(公告)号：US11905284B2

公开(公告)日：2024-02-20

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

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：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.

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.

公开(公告)号：US09340493B2

公开(公告)日：2016-05-17

申请号：US14223061

申请日：2014-03-24

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Charles Francis Donovan ,  Edmund Lee Ellsworth ,  Denton Wade Hoyer ,  Timothy Allan Johnson ,  Manjinder Singh Lall ,  Chris Limberakis ,  Sean Timothy Murphy ,  Debra Ann Sherry ,  Clarke Bentley Taylor ,  Joseph Scott Warmus

IPC: A61K31/685 ,  A61K31/19 ,  A61K31/415 ,  A61K31/44 ,  A61K31/34 ,  A61K31/42 ,  A61K31/425 ,  A61K31/535 ,  C07D233/64 ,  C07D213/55 ,  C07D307/54 ,  C07C259/06 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D231/12 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653 ,  C07D277/30

CPC classification number: C07C259/06 ,  C07C2601/04 ,  C07D207/267 ,  C07D213/30 ,  C07D213/38 ,  C07D213/55 ,  C07D231/12 ,  C07D233/64 ,  C07D237/04 ,  C07D239/26 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/08 ,  C07D261/10 ,  C07D263/32 ,  C07D271/06 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D285/06 ,  C07D307/14 ,  C07D307/42 ,  C07D307/54 ,  C07D309/10 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07F9/653

Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中：G为式（II）的基团：及其药学上可接受的盐，前体药物，水合物或溶剂合物，其中A， B，L1-L4，A，B，R1-R4和m如本文所定义。 本发明还涉及包含式（I）化合物及其在治疗细菌感染中的用途的药物组合物。

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。