公开(公告)号：US20170247372A1

公开(公告)日：2017-08-31

申请号：US15446500

申请日：2017-03-01

申请人： Pfizer Inc.

发明人： 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分类号： C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D471/08 ,  C07D498/04

CPC分类号： C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

摘要： 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

申请人： Pfizer Inc.

发明人： 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分类号： A61K31/519 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC分类号： C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

摘要： 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：US10316021B2

公开(公告)日：2019-06-11

申请号：US15820679

申请日：2017-11-22

申请人： Pfizer Inc.

发明人： Natasha Mariam Kablaoui ,  Michael Eric Green ,  Justin Ian Montgomery ,  Michael Aaron Brodney ,  Patrick Robert Verhoest ,  Gregory Wayne Kauffman ,  Danica Antonia Rankic ,  Scot Richard Mente ,  Bruce Nelsen Rogers ,  Kapildev Kashmirilal Arora ,  Matthew Francis Dunn

IPC分类号： C07D403/04 ,  C07D231/20 ,  C07D413/04 ,  C07D417/04 ,  A61P25/00

摘要： The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R9, X, m and n are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating kappa opioid (κ-opioid) associated disorders including, e.g., a neurological disorder, or psychiatric disorder such as a neurocognitive disorder, substance abuse disorder, depressive disorder, anxiety disorder, trauma and stressor related disorder and feeding and eating disorder.

公开(公告)号：US09845301B2

公开(公告)日：2017-12-19

申请号：US15221658

申请日：2016-07-28

申请人： PFIZER INC.

发明人： Christopher Ryan Butler ,  Laura Ann McAllister ,  Elizabeth Mary Beck ,  Michael Aaron Brodney ,  Adam Matthew Gilbert ,  Christopher John Helal ,  Douglas Scott Johnson ,  Justin Ian Montgomery ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Patrick Robert Verhoest ,  Damien Webb

IPC分类号： C07D295/14 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D498/10 ,  C07D491/107 ,  C07D401/12 ,  C07D471/10 ,  C07D487/04 ,  C07D211/48 ,  C07D471/08 ,  C07D515/10 ,  C07F9/6561 ,  C07D405/14 ,  C07D413/14 ,  C07D405/12 ,  C07D493/10

CPC分类号： C07D295/14 ,  C07D211/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D493/10 ,  C07D498/10 ,  C07D515/10 ,  C07F9/6561

摘要： The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

公开(公告)号：US08846933B2

公开(公告)日：2014-09-30

申请号：US14154239

申请日：2014-01-14

申请人： Pfizer Inc.

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

IPC分类号： 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分类号： 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

摘要： 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.

摘要翻译： 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：US20140057919A1

公开(公告)日：2014-02-27

申请号：US14068956

申请日：2013-10-31

申请人： Pfizer Inc.

发明人： Usa Reilly ,  Michael Joseph Melnick ,  Matthew Frank Brown ,  Mark Stephen Plummer ,  Justin Ian Montgomery ,  Ye Che ,  Loren Michael Price

IPC分类号： C07D405/04 ,  C07D213/64 ,  C07D401/04 ,  C07D401/10

CPC分类号： C07D405/04 ,  C07D213/64 ,  C07D213/69 ,  C07D401/04 ,  C07D401/10 ,  C07D405/12 ,  C07D413/10 ,  C07D417/12

摘要： 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.

摘要翻译： 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，其用于治疗细菌感染。

公开(公告)号：US12077533B2

公开(公告)日：2024-09-03

申请号：US17393463

申请日：2021-08-04

申请人： Pfizer Inc.

发明人： 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分类号： A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC分类号： C07D471/04 ,  A61K31/4523 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

摘要： 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

申请人： Pfizer Inc.

发明人： 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分类号： C07F9/58 ,  A61P31/04 ,  C07F5/02

CPC分类号： C07F9/58 ,  A61P31/04 ,  C07F5/022

摘要： 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：US11111242B2

公开(公告)日：2021-09-07

申请号：US15446500

申请日：2017-03-01

申请人： Pfizer Inc.

发明人： 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分类号： A61K31/4523 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

摘要： 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

申请人： Pfizer Inc.

发明人： 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分类号： C07F9/6558 ,  C07F9/58 ,  C07F5/04 ,  A61P31/04

摘要： 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.