公开(公告)号：US20150353508A1

公开(公告)日：2015-12-10

申请号：US14830015

申请日：2015-08-19

Applicant: Pfizer Inc.

Inventor： Mary Didiuk ,  Kevin J. Filipski ,  Angel Guzman-Perez ,  Esther C. Lee ,  Jeffrey A. Pfefferkorn ,  Benjamin Stevens ,  Meihua Tu

IPC: C07D239/84 ,  A61K31/517

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D215/38 ,  C07D217/22 ,  C07D239/94 ,  C07D241/44

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

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，A1，A2，A3，B1，B2，B3和B4如本文所定义。 已经发现式I的化合物用作胰高血糖素拮抗剂或反向激动剂。 因此，式I化合物及其药物组合物可用于治疗由胰高血糖素介导的疾病，病症或病症。

公开(公告)号：US20180162858A1

公开(公告)日：2018-06-14

申请号：US15883109

申请日：2018-01-30

Applicant: PFIZER INC.

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

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

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：US09139538B2

公开(公告)日：2015-09-22

申请号：US14564263

申请日：2014-12-09

Applicant: Pfizer Inc.

Inventor： Mary Didiuk ,  Kevin J. Filipski ,  Angel Guzman-Perez ,  Esther C. Lee ,  Jeffrey A. Pfefferkorn ,  Benjamin Stevens ,  Meihua Tu

IPC: C07D215/58 ,  C07D241/44 ,  C07D215/38 ,  C07D239/94 ,  C07D217/22 ,  C07D239/84

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D215/38 ,  C07D217/22 ,  C07D239/94 ,  C07D241/44

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

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：US10294225B2

公开(公告)日：2019-05-21

申请号：US15883109

申请日：2018-01-30

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

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：US20160347752A1

公开(公告)日：2016-12-01

申请号：US15236635

申请日：2016-08-15

Applicant: PFIZER INC.

Inventor： Mary 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.

Abstract translation: 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：US20150099882A1

公开(公告)日：2015-04-09

申请号：US14564263

申请日：2014-12-09

Applicant: Pfizer Inc.

Inventor： Mary Didiuk ,  Kevin J. Filipski ,  Angel Guzman-Perez ,  Esther C. Lee ,  Jeffrey A. Pfefferkorn ,  Benjamin Stevens ,  Meihua Tu

IPC: C07D241/44 ,  C07D217/22 ,  C07D215/38 ,  C07D239/84

CPC classification number: C07D239/84 ,  A61K31/517 ,  C07D215/38 ,  C07D217/22 ,  C07D239/94 ,  C07D241/44

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.