公开(公告)号：US12103921B2

公开(公告)日：2024-10-01

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 ,  A61K45/06 ,  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：US20200172512A1

公开(公告)日：2020-06-04

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 ,  C07D471/04 ,  A61P7/06

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：US11866425B2

公开(公告)日：2024-01-09

申请号：US17345064

申请日：2021-06-11

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: A61K31/505 ,  A61P3/00 ,  A61P3/10 ,  A61P3/06 ,  C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  C07B2200/13

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：US20210309646A1

公开(公告)日：2021-10-07

申请号：US17345064

申请日：2021-06-11

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 ,  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：US20200181127A1

公开(公告)日：2020-06-11

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

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：US20220184041A1

公开(公告)日：2022-06-16

申请号：US17533592

申请日：2021-11-23

Applicant: Pfizer Inc.

Inventor： Shawn Cabral ,  Daniel Paul Canterbury ,  Robert Lee Dow ,  Andrew Fensome ,  Magdalena Korczynska ,  Sophie Yvette Lavergne ,  Allyn Timothy Londregan ,  Vincent Mascitti ,  David Walter Piotrowski ,  Andre Shavnya ,  Meihua Mike Tu ,  Tao Wang ,  Hanna Maria Wisniewska

IPC: A61K31/428 ,  C07D417/04 ,  C07D513/04 ,  A61K31/437 ,  A61K31/353 ,  A61K31/423 ,  A61K31/415 ,  A61K31/192 ,  A61K31/12 ,  A61K31/7105

Abstract: This application includes a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein the variables R1a, R1b, R2, R3, X, Y and Z are as defined herein, pharmaceutical compositions comprising the compounds of Formula I and methods of treatment comprising administering to a patient in need thereof a compound of Formula I for the treatment of transthyretin amyloidosis and diseases related thereto.

公开(公告)号：US10071992B2

公开(公告)日：2018-09-11

申请号：US15674914

申请日：2017-08-11

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: C07D401/00 ,  C07D253/08 ,  C07D401/04 ,  A61K9/14 ,  C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14 ,  C07D401/14

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：US20180051012A1

公开(公告)日：2018-02-22

申请号：US15674914

申请日：2017-08-11

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 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07B2200/13 ,  C07D401/14 ,  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：US20150087585A1

公开(公告)日：2015-03-26

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 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/538 ,  C07D487/04 ,  A61K31/437 ,  A61K31/506

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：US20240140937A1

公开(公告)日：2024-05-02

申请号：US18520638

申请日：2023-11-28

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 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/06

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.