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：US20230382892A1

公开(公告)日：2023-11-30

申请号：US18322844

申请日：2023-05-24

Applicant: Pfizer Inc.

Inventor： Ariamala Gopalsamy ,  Shawn Cabral ,  Agustin Casimiro Garcia ,  Ming Zhu Chen ,  Chulho Choi ,  Robert Lee Dow ,  Olugbeminiyi Omezia Fadeyi ,  David Hepworth ,  Jayasankar Jasti ,  Lyn Howard Jones ,  Arjun Venkat Narayanan ,  Mihir Dineshkumar Parikh ,  David Walter Piotrowski ,  Lee Richard Roberts ,  Ralph Pelton Robinson, Jr. ,  Hatice Gizem Yayla

IPC: C07D401/14 ,  A61P7/06 ,  C07D471/04

CPC classification number: C07D401/14 ,  A61P7/06 ,  C07D471/04 ,  A61K45/06

Abstract: The invention relates to pyrazole 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 HbS modulators of formula (I)






or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description.




HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).

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：US11014908B2

公开(公告)日：2021-05-25

申请号：US16695709

申请日：2019-11-26

Applicant: Pfizer Inc.

Inventor： Ariamala Gopalsamy ,  Arjun Venkat Narayanan ,  Agustin Casimiro-Garcia ,  Chulho Choi ,  David Hepworth ,  David Walter Piotrowski ,  Hatice Gizem Yayla ,  Jayasankar Jasti ,  Lee Richard Roberts ,  Lyn Howard Jones ,  Mihir Dineshkumar Parikh ,  Ming Zhu Chen ,  Olugbeminiyi Omezia Fadeyi ,  Ralph Pelton Robinson, Jr. ,  Robert Lee Dow ,  Shawn Cabral

IPC: C07D401/14 ,  A61P7/06 ,  C07D471/04 ,  A61K45/06

Abstract: The invention relates to pyrazole 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 HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).

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.

公开(公告)号：US09879022B2

公开(公告)日：2018-01-30

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 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/14 ,  A61K31/47 ,  A61K31/517 ,  A61K31/4015 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D207/26 ,  C07D215/48 ,  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 ,  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：US09440949B2

公开(公告)日：2016-09-13

申请号：US14643210

申请日：2015-03-10

Applicant: PFIZER INC.

Inventor： Shawn Cabral ,  Kentaro Futatsugi ,  David Hepworth ,  Kim Huard ,  Daniel Wei-Shung Kung ,  Suvi Tuula Marjukka Orr ,  Kun Song

IPC: A61K31/5377 ,  A61K31/606 ,  A61K31/506 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/04 ,  C07D487/04 ,  C07D413/14 ,  C07D491/08 ,  C07D401/14 ,  C07D487/02

CPC classification number: A61K31/506 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/606 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D487/02 ,  C07D487/04 ,  C07D491/08

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

Abstract translation: 本文描述了抑制二酰基甘油酰基转移酶2（DGAT2）的活性的式I化合物及其在治疗与动物相关疾病中的用途。