公开(公告)号：US20160368919A1

公开(公告)日：2016-12-22

申请号：US15184097

申请日：2016-06-16

Applicant: Pfizer Inc.

Inventor： Agustin Casimiro-Garcia ,  Bruce Allen Lefker ,  Nikolaos Papaioannou ,  Arjun Venkat Narayanan ,  Jotham Wadsworth Coe

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Disclosed are novel pyridine pyrazinones or pharmaceutically acceptable salts thereof. Pharmaceutical compositions and the use of the compounds to treat diseases or disorders that are BET family bromodomain-dependent are also disclosed. Methods for preparing and using these compounds are further described.

Abstract translation: 公开了新的吡啶吡嗪酮或其药学上可接受的盐。 还公开了药物组合物和化合物用于治疗作为BET家族溴结构域依赖性的疾病或病症的用途。 进一步描述制备和使用这些化合物的方法。

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：US10793579B2

公开(公告)日：2020-10-06

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

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：US20180127432A1

公开(公告)日：2018-05-10

申请号：US15862691

申请日：2018-01-05

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 ,  C07D239/88 ,  C07D239/86 ,  C07D263/24 ,  C07D207/267 ,  A61K31/40 ,  C07D207/08 ,  C07F7/18 ,  C07D209/52 ,  C07D498/04 ,  C07D207/273 ,  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 ,  C07D407/14 ,  C07D215/48 ,  C07D207/26 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4015

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：US20160347760A1

公开(公告)日：2016-12-01

申请号：US15232892

申请日：2016-08-10

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 ,  C07D405/12 ,  C07D215/48 ,  A61K31/47 ,  A61K31/4725 ,  C07D417/12 ,  A61K31/541 ,  C07D413/12 ,  A61K31/5377 ,  C07D207/267 ,  A61K31/4015 ,  C07D207/08 ,  A61K31/40 ,  C07D407/14 ,  C07D487/04 ,  C07D403/12 ,  A61K31/517 ,  A61K45/06 ,  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: 如说明书中所定义。 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：US12202836B2

公开(公告)日：2025-01-21

申请号：US18342977

申请日：2023-06-28

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 ,  A61K31/40 ,  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 ,  C07F7/18

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. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.

公开(公告)号：US11702424B2

公开(公告)日：2023-07-18

申请号：US16996117

申请日：2020-08-18

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

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：US20200377511A1

公开(公告)日：2020-12-03

申请号：US16996117

申请日：2020-08-18

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 ,  C07D401/14 ,  C07D405/14 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07C69/94 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D207/273 ,  C07D498/04 ,  C07D209/52 ,  A61K31/4015 ,  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 ,  C07D487/04 ,  A61K31/40 ,  C07D207/08 ,  C07D207/267

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：US20190270778A1

公开(公告)日：2019-09-05

申请号：US16319985

申请日：2017-07-17

Applicant: Pfizer Inc.

Inventor： Ye Che ,  Yiqing Feng ,  Matthew Merrill Hayward ,  David Hepworth ,  Peter Jones ,  Kaila Neelu ,  Nikolaos Papaioannou

IPC: C07K7/56 ,  A61K38/08 ,  A61P13/12

Abstract: The invention relates to cyclic peptide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to cyclic peptide C5a receptor antagonists of formula (Ia) or formula (Ib), or pharmaceutically acceptable salts thereof, wherein R1a, R1b, R2, R3 and R4 areas defined in the description. C5a receptor antagonists are potentially useful in the treatment of a wide range of 1 disorders, including inflammatory disorders and immune disorders.

公开(公告)号：US10329302B2

公开(公告)日：2019-06-25

申请号：US15862691

申请日：2018-01-05

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: C07D401/04 ,  A61K31/47 ,  C07D491/056 ,  C07F7/18 ,  A61K31/4015 ,  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 ,  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 ,  A61K31/40 ,  C07D207/08 ,  C07D207/267

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.