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：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。

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：US11034678B2

公开(公告)日：2021-06-15

申请号：US16793441

申请日：2020-02-18

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D401/04 ,  C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

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.

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：US20180258081A1

公开(公告)日：2018-09-13

申请号：US15977238

申请日：2018-05-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D401/14 ,  C07D409/14 ,  A61K31/506 ,  A61K45/06

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.

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。