公开(公告)号：US20240368144A1

公开(公告)日：2024-11-07

申请号：US18311266

申请日：2023-05-03

Applicant: Pfizer Inc.

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

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

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：US20210206757A1

公开(公告)日：2021-07-08

申请号：US17192968

申请日：2021-03-05

Applicant: Pfizer Inc.

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

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

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：US10975065B2

公开(公告)日：2021-04-13

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

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：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：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：US20170233371A1

公开(公告)日：2017-08-17

申请号：US15497862

申请日：2017-04-26

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Gõran Mattias Wennerstål ,  James Robert Blinn ,  Neelu Kaila ,  James Richard Kiefer, Jr. ,  Scot Richard Mente ,  Ravi G. Kurumbail ,  Marvin Jay Meyers ,  Atli Thorarensen ,  Li Xing ,  Christoph Wolfgang Zapf ,  Edouard Zamaratski ,  Andrew Christopher Flick ,  Peter Jones

IPC: C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D413/04 ,  C07D471/04 ,  C07D487/04 ,  C07D403/04 ,  C07D401/04 ,  C07D417/14

CPC classification number: C07D401/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  Y02A50/406 ,  A61K2300/00

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

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：US20160046597A1

公开(公告)日：2016-02-18

申请号：US14448220

申请日：2014-07-31

Applicant: PFIZER INC.

Inventor： Mark Edward Schnute ,  Göran Mattias Wennerstål ,  James Robert Blinn ,  Neelu Kaila ,  James Richard Kiefer, JR. ,  Scot Richard Mente ,  Ravi G. Kurumbail ,  Marvin Jay Meyers ,  Atli Thorarensen ,  Li Xing ,  Christoph Wolfgang Zapf ,  Edouard Zamaratski ,  Andrew Christopher Flick ,  Peter Jones

IPC: C07D401/04 ,  C07D413/14 ,  C07D403/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D401/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  Y02A50/406 ,  A61K2300/00

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

Abstract translation: 本发明提供化合物，药物组合物，抑制受试者的RORγ活性和/或减少IL-17的量的方法，以及使用这些化合物和药物组合物治疗各种医学病症的方法。

公开(公告)号：US10703756B2

公开(公告)日：2020-07-07

申请号：US15569874

申请日：2016-04-19

Applicant: Pfizer Inc.

Inventor： Atli Thorarensen ,  Matthew Frank Brown ,  Agustin Casimiro-Garcia ,  Ye Che ,  Mark Edward Flanagan ,  Adam Matthew Gilbert ,  Matthew Merrill Hayward ,  Jean-Baptiste Telliez ,  Rayomand Jal Unwalla ,  John I. Trujillo ,  Sidney Xi Liang

IPC: C07D487/04

Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, 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：US20200039960A1

公开(公告)日：2020-02-06

申请号：US16656702

申请日：2019-10-18

Applicant: Pfizer Inc.

Inventor： Mark Edward Schnute ,  Göran Mattias Wennerstål ,  James Robert Blinn ,  Neelu Kaila ,  James Richard Kiefer, Jr. ,  Scot Richard Mente ,  Ravi G. Kurumbail ,  Marvin Jay Meyers ,  Atli Thorarensen ,  Li Xing ,  Christoph Wolfgang Zapf ,  Edouard Zamaratski ,  Andrew Christopher Flick ,  Peter Jones

IPC: C07D401/14 ,  C07D413/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  C07D407/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14

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