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：US08735396B2

公开(公告)日：2014-05-27

申请号：US13899851

申请日：2013-05-22

Applicant: Pfizer Inc.

Inventor： Jeffrey Allen Pfefferkorn ,  Anthony Lai Ling

IPC: A61K31/497

CPC classification number: C07D405/14

Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.

Abstract translation: 本发明提供了作为葡糖激酶活化剂的式（I）化合物; 其药物组合物; 以及治疗由葡萄糖激酶介导的疾病，病症或病症的方法。

公开(公告)号：US20230218616A1

公开(公告)日：2023-07-13

申请号：US17904537

申请日：2021-02-22

Applicant: Pfizer Inc.

Inventor： Neeta Balkrishan Amin ,  Arthur James Bergman ,  Roberto Arnaldo Calle ,  William Paul Esler ,  Albert Myung Kim ,  Jeffrey Allen Pfefferkorn ,  Patrick Robert Verhoest

IPC: A61K31/506 ,  A61K31/438 ,  A61P1/16 ,  A61P3/00

CPC classification number: A61K31/506 ,  A61K31/438 ,  A61P1/16 ,  A61P3/00 ,  C07B2200/13

Abstract: A method for treating fatty liver disease and related diseases or disorders with a therapeutically effective amount of a composition comprising from about 25 mg to about 1200 mg of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof, and from about 5 mg to about 40 mg of 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or a pharmaceutically acceptable salt thereof.

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。

公开(公告)号：US20140329862A1

公开(公告)日：2014-11-06

申请号：US14334718

申请日：2014-07-18

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: C07D213/82

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。

公开(公告)号：US08859591B2

公开(公告)日：2014-10-14

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: A61K31/415 ,  A61K31/4427 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  C07D231/00 ,  C07D233/00 ,  C07D237/06 ,  C07D239/24 ,  C07D241/10 ,  C07D233/61 ,  C07D231/54 ,  C07D207/34 ,  C07D487/04 ,  C07D403/12 ,  C07D249/08 ,  C07D231/16 ,  C07D231/14 ,  C07D233/68 ,  C07D231/12 ,  C07D249/06 ,  C07D233/84 ,  C07D405/14 ,  C07D401/12 ,  C07D403/04 ,  C07D233/64 ,  C07D231/18 ,  C07D401/14 ,  C07D261/08 ,  C07D401/04 ,  C07D231/56 ,  C07D233/70

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：US09073871B2

公开(公告)日：2015-07-07

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: A61K31/415 ,  C07D231/12 ,  C07D207/34 ,  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 ,  C07D403/04 ,  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：US08933104B2

公开(公告)日：2015-01-13

申请号：US14334718

申请日：2014-07-18

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: C07D401/12 ,  A61K31/44 ,  C07D213/82

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。