公开(公告)号：US20150266859A1

公开(公告)日：2015-09-24

申请号：US14730562

申请日：2015-06-04

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Esther Cheng Yin Lee ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D403/04 ,  C07D401/04

CPC classification number: C07D401/04 ,  A61K31/506 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D239/28 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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，A4，L，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：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：US20140371467A1

公开(公告)日：2014-12-18

申请号：US14471576

申请日：2014-08-28

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Esther Cheng Yin Lee ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D231/12

CPC classification number: C07D401/04 ,  A61K31/506 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D239/28 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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，A4，L，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：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：US20150266861A1

公开(公告)日：2015-09-24

申请号：US14731632

申请日：2015-06-05

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D405/12 ,  C07D239/42 ,  C07D237/08 ,  C07D403/12 ,  C07D401/12 ,  C07D213/82 ,  C07D241/34

CPC classification number: C07D405/12 ,  A61K31/44 ,  A61K31/4427 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D237/08 ,  C07D239/42 ,  C07D241/28 ,  C07D241/34 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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：US20160362392A1

公开(公告)日：2016-12-15

申请号：US15248296

申请日：2016-08-26

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Esther Cheng Yin Lee ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D401/04

CPC classification number: C07D401/04 ,  A61K31/506 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D239/28 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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: 或其药学上可接受的盐，其中R1，R2，R3，A1，A2，A3，A4，L，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：US09452999B2

公开(公告)日：2016-09-27

申请号：US14730562

申请日：2015-06-04

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Esther Cheng Yin Lee ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: A61K31/506 ,  C07D239/28 ,  C07D403/04 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  C07D403/12

CPC classification number: C07D401/04 ,  A61K31/506 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D239/28 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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：US20130296355A1

公开(公告)日：2013-11-07

申请号：US13934322

申请日：2013-07-03

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Esther Cheng Yin Lee ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D487/04 ,  C07D401/12 ,  C07D231/12 ,  C07D401/04 ,  C07D231/18 ,  C07D405/14 ,  C07D249/08 ,  C07D261/08 ,  C07D231/56 ,  C07D403/12 ,  C07D401/14 ,  C07D233/64 ,  C07D207/34

CPC classification number: C07D401/04 ,  A61K31/506 ,  C07D207/34 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D231/56 ,  C07D233/61 ,  C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D239/28 ,  C07D249/06 ,  C07D249/08 ,  C07D261/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D487/04

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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：US09056834B2

公开(公告)日：2015-06-16

申请号：US14561879

申请日：2014-12-05

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D213/74 ,  C07D213/82 ,  A61K31/44 ,  C07D213/81 ,  C07D401/12 ,  C07D405/12

CPC classification number: C07D405/12 ,  A61K31/44 ,  A61K31/4427 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D237/08 ,  C07D239/42 ,  C07D241/28 ,  C07D241/34 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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，A4，L，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，病症或病状。

公开(公告)号：US20150094338A1

公开(公告)日：2015-04-02

申请号：US14561879

申请日：2014-12-05

Applicant: Pfizer Inc.

Inventor： Gary Erik Aspnes ,  Mary Theresa Didiuk ,  Kevin James Filipski ,  Angel Guzman-Perez ,  Jeffrey Allen Pfefferkorn ,  Benjamin Dawson Stevens ,  Meihua Mike Tu

IPC: C07D213/81 ,  C07D405/12 ,  C07D401/12

CPC classification number: C07D405/12 ,  A61K31/44 ,  A61K31/4427 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D237/08 ,  C07D239/42 ,  C07D241/28 ,  C07D241/34 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, 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，A4，L，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。