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：US09815832B2

公开(公告)日：2017-11-14

申请号：US14804644

申请日：2015-07-21

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Patrick Robert Verhoest ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward

IPC: A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.

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：US20170145022A1

公开(公告)日：2017-05-25

申请号：US15426423

申请日：2017-02-07

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

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：US20160130250A1

公开(公告)日：2016-05-12

申请号：US15000944

申请日：2016-01-19

Applicant: PFIZER, INC.

Inventor： Michael Joseph Luzzio ,  Kevin Daniel Freeman-Cook ,  Samit Kumar Bhattacharya ,  Matthew Merrill Hayward ,  Catherine Angela Hulford ,  Christopher Lowell Autry ,  Xumiao Zhao ,  Jun Xiao ,  Kendra Louise Nelson

IPC: C07D401/12

CPC classification number: C07D401/12 ,  C07D239/48 ,  C07D241/20 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D475/00

Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US20160039828A1

公开(公告)日：2016-02-11

申请号：US14817606

申请日：2015-08-04

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Patrick Robert Verhoest ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Joseph Michael Young

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R3, R6, R7, and b are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，其中取代基R 1，R 3，R 6，R 7和b如本文所定义。 本发明还涉及包含化合物的药物组合物，使用该化合物的治疗方法，以及制备化合物的方法。

公开(公告)号：US10738063B2

公开(公告)日：2020-08-11

申请号：US16427627

申请日：2019-05-31

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Matthew Merrill Hayward

IPC: C07D498/04 ,  C07D519/00

Abstract: The present invention is directed to PDE4B inhibitors of Formula I: (I) or a pharmaceutically acceptable salt thereof, wherein the substituents R1, R2, R3, and R4 are as defined herein. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.

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：US20200002310A1

公开(公告)日：2020-01-02

申请号：US16567675

申请日：2019-09-11

Applicant: Pfizer Inc.

Inventor： Michael Joseph Luzzio ,  Kevin Daniel Freeman-Cook ,  Samit Kumar Bhattacharya ,  Matthew Merrill Hayward ,  Catherine Angela Hulford ,  Christopher Lowell Autry ,  Xumiao Zhao ,  Jun Xiao ,  Kendra Louise Nelson

IPC: C07D401/12 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D241/20 ,  C07D475/00

Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.