公开(公告)号：US20190270751A1

公开(公告)日：2019-09-05

申请号：US16411679

申请日：2019-05-14

Applicant: Pfizer Inc.

Inventor： John David Trzupek ,  Katherine Lin Lee ,  Mark Edward Bunnage ,  Seungil Han ,  David Hepworth ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Nikolaos Papaioannou ,  Betsy Susan Pierce ,  Joseph Walter Strohbach ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf ,  Lori Krim Gavrin ,  Arthur Lee ,  David Randolph Anderson ,  Kevin Joseph Curran ,  Christoph Martin Dehnhardt ,  Eddine Saiah ,  Joel Adam Goldberg ,  Xiaolun Wang ,  Horng-Chih Huang ,  Richard Vargas ,  Michael Dennis Lowe ,  Akshay Patny

IPC: C07D491/056 ,  C07F7/18 ,  A61K31/4015 ,  C07D207/267 ,  C07D207/08 ,  C07D209/52 ,  C07D498/04 ,  C07D207/273 ,  C07D263/24 ,  C07D239/88 ,  C07D239/86 ,  C07C69/94 ,  C07D217/24 ,  C07D217/22 ,  C07D217/02 ,  C07D405/14 ,  C07D401/14 ,  C07D487/04 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D207/26 ,  C07D215/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  A61K31/40

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US10316018B2

公开(公告)日：2019-06-11

申请号：US16206166

申请日：2018-11-30

Applicant: PFIZER INC.

Inventor： Katherine Lin Lee ,  Christophe Philippe Allais ,  Christoph Martin Dehnhardt ,  Lori Krim Gavrin ,  Seungil Han ,  David Hepworth ,  Arthur Lee ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Dafydd Rhys Owen ,  Nikolaos Papaioannou ,  Eddine Saiah ,  Joseph Walter Strohbach ,  John David Trzupek ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf

IPC: A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/4015 ,  A61K45/06 ,  C07D401/12 ,  C07D413/04 ,  C07D207/273 ,  C07D491/18 ,  C07D471/04 ,  C07D413/14 ,  C07D401/14

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US10174000B2

公开(公告)日：2019-01-08

申请号：US15754650

申请日：2016-08-16

Applicant: PFIZER INC.

Inventor： Katherine Lin Lee ,  Christophe Philippe Allais ,  Christoph Martin Dehnhardt ,  Lori Krim Gavrin ,  Seungil Han ,  David Hepworth ,  Arthur Lee ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Dafydd Rhys Owen ,  Nikolaos Papaioannou ,  Eddine Saiah ,  Joseph Walter Strohbach ,  John David Trzupek ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf

IPC: C07D207/273 ,  C07D401/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D491/18 ,  A61K31/4015 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4745 ,  A61K45/06

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09518052B2

公开(公告)日：2016-12-13

申请号：US14710631

申请日：2015-05-13

Applicant: Pfizer Inc.

Inventor： Jotham Wadsworth Coe ,  Christoph Martin Dehnhardt ,  Peter Jones ,  Yogesh Anil Sabnis ,  Joseph Walter Strohbach ,  Florian Michel Wakenhut ,  Gavin Alistair Whitlock

IPC: C07D471/04 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/437 ,  A61K31/4725 ,  C07D471/04 ,  C07D487/04

Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A′ are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR″SO2—R′, etc., where R′ and R″ are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and R0 and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2′ are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.

公开(公告)号：US20150284405A1

公开(公告)日：2015-10-08

申请号：US14678114

申请日：2015-04-03

Applicant: Pfizer Inc.

Inventor： John David Trzupek ,  Katherine Lin Lee ,  Mark Edward Bunnage ,  Seungil Han ,  David Hepworth ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Nikolaos Papaioannou ,  Betsy Susan Pierce ,  Joseph Walter Strohbach ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf ,  Lori Krim Gavrin ,  Arthur Lee ,  David Randolph Anderson ,  Kevin Joseph Curran ,  Christoph Martin Dehnhardt ,  Eddine Saiah ,  Joel Adam Goldberg ,  Xiaolun Wang ,  Horng-Chih Huang ,  Richard Vargas ,  Michael Dennis Lowe ,  Akshay Patny

IPC: C07D491/056 ,  A61K31/4709 ,  A61K45/06 ,  C07D405/12 ,  C07D215/48 ,  A61K31/47 ,  A61K31/4725 ,  C07D417/12 ,  A61K31/541 ,  C07D413/12 ,  A61K31/5377 ,  C07D207/26 ,  A61K31/4015 ,  C07D407/14 ,  C07D487/04 ,  C07D403/12 ,  A61K31/517 ,  C07D401/12

CPC classification number: C07D491/056 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07C69/94 ,  C07D207/08 ,  C07D207/26 ,  C07D207/267 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04 ,  C07F7/1804

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有如说明书中定义的式Ia结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20240124439A1

公开(公告)日：2024-04-18

申请号：US18257195

申请日：2021-12-13

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  Agustin Casimiro-Garcia ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Katherine Lin Lee ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The invention relates to imidazopyridines of Formula (I)




and pharmaceutically acceptable salts thereof, wherein R0 to R5 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.

公开(公告)号：US10906888B2

公开(公告)日：2021-02-02

申请号：US16316688

申请日：2017-07-07

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Joseph Walter Strohbach ,  David Hepworth ,  Frank Eldridge Lovering ,  Chulho Choi ,  Christophe Philippe Allais ,  Stephen Wayne Wright

IPC: C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D498/10 ,  C07D498/18

Abstract: Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09458168B2

公开(公告)日：2016-10-04

申请号：US14678114

申请日：2015-04-03

Applicant: Pfizer Inc.

Inventor： John David Trzupek ,  Katherine Lin Lee ,  Mark Edward Bunnage ,  Seungil Han ,  David Hepworth ,  Frank Eldridge Lovering ,  John Paul Mathias ,  Nikolaos Papaioannou ,  Joseph Walter Strohbach ,  Stephen Wayne Wright ,  Christoph Wolfgang Zapf ,  Lori Krim Gavrin ,  Arthur Lee ,  Kevin Joseph Curran ,  Christoph Martin Dehnhardt ,  Eddine Saiah ,  Joel Adam Goldberg ,  Xiaolun Wang ,  Richard Vargas ,  Michael Dennis Lowe ,  Akshay Patny

IPC: C07D207/26 ,  C07D401/12 ,  A61K31/44 ,  C07D491/056 ,  A61K31/4015 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D215/48 ,  C07D403/12 ,  C07D405/12 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07C69/94 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D207/273 ,  C07D498/04 ,  C07D209/52 ,  C07F7/18

CPC classification number: C07D491/056 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07C69/94 ,  C07D207/08 ,  C07D207/26 ,  C07D207/267 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04 ,  C07F7/1804

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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：US20240132477A1

公开(公告)日：2024-04-25

申请号：US18257136

申请日：2021-12-13

Applicant: PFIZER INC.

Inventor： Scott William Bagley ,  Agustin Casimiro Garcia ,  Jennifer Elizabeth Davoren ,  Rajiah Aldrin Denny ,  Brian Stephen Gerstenberger ,  Frank Eldridge Lovering ,  Mihir Dineshkumar Parikh ,  Joseph Walter Strohbach ,  John Isidro Trujillo

IPC: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: The invention relates to benzimidazoles of Formula (I)




and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes.
The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.