公开(公告)号：US20140288049A1

公开(公告)日：2014-09-25

申请号：US14299497

申请日：2014-06-09

Applicant: Pfizer Inc.

Inventor： Philip A. Carpino ,  Edward L. Conn ,  Robert L. Dow ,  Matthew S. Dowling ,  David Hepworth ,  Daniel Wei-Shung Kung ,  Suvi Orr ,  Benjamin N. Rocke ,  Roger B. Ruggeri ,  Matthew F. Sammons ,  Joseph S. Warmus ,  Yan Zhang

IPC: C07D239/56 ,  C07D401/04 ,  C07D405/04 ,  C07D403/04 ,  C07D471/04 ,  A61K31/5377 ,  C07D417/04 ,  C07D403/06 ,  C07D403/10 ,  C07D401/06 ,  C07D413/06 ,  A61K31/513 ,  C07D409/04

CPC classification number: C07D239/56 ,  A61K31/352 ,  A61K31/37 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

公开(公告)号：US08841314B2

公开(公告)日：2014-09-23

申请号：US13875604

申请日：2013-05-02

Applicant: Pfizer Inc.

Inventor： David Hepworth ,  Roger B. Ruggeri

IPC: C07D239/56 ,  A61K31/513

CPC classification number: C07D239/56 ,  A61K31/352 ,  A61K31/37 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

Abstract translation: 髓过氧化物酶抑制剂，含有这些抑制剂的药物组合物以及这些抑制剂用于治疗例如心血管病症的用途。

公开(公告)号：US11702405B2

公开(公告)日：2023-07-18

申请号：US17227819

申请日：2021-04-12

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 ,  A61K45/06

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：US20220348555A1

公开(公告)日：2022-11-03

申请号：US17227819

申请日：2021-04-12

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

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：US20190315715A1

公开(公告)日：2019-10-17

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：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：US20160304469A1

公开(公告)日：2016-10-20

申请号：US15191943

申请日：2016-06-24

Applicant: Pfizer Inc.

Inventor： Philip A. Carpino ,  Edward L. Conn ,  Robert L. Dow ,  Matthew S. Dowling ,  David Hepworth ,  Daniel Wei-Shung Kung ,  Suvi Orr ,  Benjamin N. Rocke ,  Roger B. Ruggeri ,  Matthew F. Sammons ,  Joseph S. Warmus ,  Yan Zhang

IPC: C07D239/56 ,  A61K45/06 ,  C07D401/04 ,  C07D405/04 ,  C07D403/04 ,  C07D471/04 ,  C07D409/04 ,  C07D417/04 ,  C07D405/10 ,  C07D405/06 ,  C07D403/06 ,  C07D403/10 ,  C07D401/06 ,  C07D413/06 ,  A61K31/5377 ,  C07D403/12 ,  A61K31/513

CPC classification number: C07D239/56 ,  A61K31/352 ,  A61K31/37 ,  A61K31/513 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D409/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/04 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

公开(公告)号：US09296745B2

公开(公告)日：2016-03-29

申请号：US14384508

申请日：2013-03-26

Applicant: Pfizer Inc.

Inventor： Kay Ahn ,  Markus Boehm ,  Shawn Cabral ,  Philip A. Carpino ,  Kentaro Futatsugi ,  David Hepworth ,  Daniel W. Kung ,  Suvi Orr ,  Jian Wang

IPC: C07D471/04 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00

Abstract: Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine 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: 抑制二酰基甘油酰基转移酶2（DGAT2）活性的式I的嘌呤衍生物，3H-咪唑并[4,5-b]嘧啶和1H-咪唑并[4,5-d]吡嗪及其在治疗疾病中的用途 本文描述了与动物相连的动物。