公开(公告)号：US20200095239A1

公开(公告)日：2020-03-26

申请号：US16576997

申请日：2019-09-20

Applicant: Pfizer Inc.

Inventor： Brian Stephen Gerstenberger ,  Andrew Christopher Flick ,  Vincent Michael Lombardo ,  James John Mousseau ,  Philippe Marcel Nuhant ,  Ralph Pelton Robinson, JR. ,  Mark Edward Schnute ,  Daniel Wei-Shung Kung ,  Daniel Copley Schmitt ,  Atli Thorarensen ,  John Isidro Trujillo ,  Rayomand Jal Unwalla ,  Huixian Wu

IPC: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D413/12 ,  C07D405/14 ,  C07D417/14 ,  C07F9/6558 ,  A61P29/00

Abstract: The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.

公开(公告)号：US20190387710A1

公开(公告)日：2019-12-26

申请号：US16563022

申请日：2019-09-06

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand Jal Unwalla

IPC: A01K5/01 ,  B65D25/18 ,  B65D25/04 ,  B65D1/36 ,  B65D1/34 ,  A01K7/00 ,  B65D77/20 ,  A23K20/00 ,  A23K50/48 ,  C07D471/04 ,  C07D401/14

Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

公开(公告)号：US20190150401A1

公开(公告)日：2019-05-23

申请号：US16268857

申请日：2019-02-06

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand Jal Unwalla

IPC: A01K5/01 ,  B65D77/20 ,  B65D25/04 ,  B65D1/34 ,  A01K7/00 ,  B65D25/18 ,  A23K20/00 ,  A23K50/48 ,  B65D1/36

CPC classification number: A01K5/0121 ,  A01K7/00 ,  A23K20/00 ,  A23K50/48 ,  B65D1/34 ,  B65D1/36 ,  B65D25/04 ,  B65D25/18 ,  B65D77/2024 ,  B65D85/70 ,  B65D2577/205 ,  C07D401/14 ,  C07D471/04

Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

公开(公告)号：US10227346B2

公开(公告)日：2019-03-12

申请号：US15889296

申请日：2018-02-06

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Andrew Christopher Flick ,  Peter Jones ,  Neelu Kaila ,  Scot Richard Mente ,  John David Trzupek ,  Michael L. Vazquez ,  Goran Mattias Wennerstal ,  Li Xing ,  Edouard Zamaratski ,  Liying Zhang ,  Rayomand Jal Unwalla

IPC: A61K31/437 ,  A61K31/4353 ,  C07D471/04 ,  C07D401/14

Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating RORγ activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.

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.