公开(公告)号：US20140243312A1

公开(公告)日：2014-08-28

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez

IPC: C07D487/04

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。

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：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：US09549929B2

公开(公告)日：2017-01-24

申请号：US14715046

申请日：2015-05-18

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  A61K31/5386 ,  C07D207/18

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。

公开(公告)号：US20150225408A1

公开(公告)日：2015-08-13

申请号：US14691606

申请日：2015-04-21

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

公开(公告)号：US20230009153A1

公开(公告)日：2023-01-12

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: C07D471/04 ,  A61K31/4523 ,  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：US20150158864A1

公开(公告)日：2015-06-11

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

IPC: C07D471/04 ,  C07D487/10 ,  C07D498/04 ,  C07D487/04 ,  C07D471/08

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.

Abstract translation: 本发明提供药学活性吡咯并[2,3-d]嘧啶基和吡咯并[2,3-d]吡啶基丙烯酰胺及其类似物。 这些化合物可用于抑制Janus Kinase（JAK）。 本发明还涉及包含制备这种化合物的方法的组合物，以及用于治疗和预防由JAK介导的病症的方法。

公开(公告)号：US09035074B2

公开(公告)日：2015-05-19

申请号：US14183946

申请日：2014-02-19

Applicant: Pfizer Inc.

Inventor： Matthew Frank Brown ,  Ashley Edward Fenwick ,  Mark Edward Flanagan ,  Andrea Gonzales ,  Timothy Allan Johnson ,  Neelu Kaila ,  Mark J. Mitton-Fry ,  Joseph Walter Strohbach ,  Ruth E. TenBrink ,  John David Trzupek ,  Rayomand Jal Unwalla ,  Michael L. Vazquez ,  Mihir D. Parikh

IPC: C07D207/18 ,  C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61K31/5386 ,  C07D207/18 ,  C07D487/04 ,  C07D519/00

Abstract: Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Abstract translation: 本文描述的是吡咯并[2,3-d]嘧啶衍生物，它们用作Janus Kinase（JAK）抑制剂，以及含有它们的药物组合物。

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.