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：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：US20210047325A1

公开(公告)日：2021-02-18

申请号：US17034295

申请日：2020-09-28

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  A61K31/435

Abstract: The invention provides a compound of Formula (1) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US09145416B2

公开(公告)日：2015-09-29

申请号：US14491016

申请日：2014-09-19

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: A61K31/44 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  A61K31/435

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐，其中R1，R2，R3，Z，A1，L和A2如本文所述; 其药物组合物; 以及其用于治疗通过抑制动物体内的乙酰辅酶A羧化酶调节的疾病，病症或病症的用途。

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：US20230322777A1

公开(公告)日：2023-10-12

申请号：US18311715

申请日：2023-05-03

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  A61K31/435 ,  A61K31/519 ,  C07D519/00 ,  C07D487/10 ,  C07D491/20 ,  A61K45/06 ,  A61K31/438

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/519 ,  C07D519/00 ,  C07D487/10 ,  C07D491/20 ,  A61K45/06 ,  A61K31/438

Abstract: The invention provides a compound of Formula (I)




or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

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：US20190218218A1

公开(公告)日：2019-07-18

申请号：US16371896

申请日：2019-04-01

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  C07D487/10 ,  A61K45/06 ,  C07D519/00 ,  A61K31/438 ,  A61K31/435 ,  A61K31/519 ,  C07D491/20

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use to thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US09908883B2

公开(公告)日：2018-03-06

申请号：US15236635

申请日：2016-08-15

Applicant: PFIZER INC.

Inventor： Mary Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: A61K31/44 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  A61K31/435

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US20150376185A1

公开(公告)日：2015-12-31

申请号：US14851572

申请日：2015-09-11

Applicant: PFIZER INC.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: C07D471/10 ,  A61K31/435 ,  A61K45/06

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.