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：US20160016940A1

公开(公告)日：2016-01-21

申请号：US14773954

申请日：2013-09-24

Applicant: PFIZER INC.

Inventor： Samit Kumar Bhattacharya ,  Kimberly O'Keefe Cameron ,  Matthew Scott Dowling ,  David Christopher Ebner ,  David James Edmonds ,  Dilinie Prasadhini Fernando ,  Kevin James Filipski ,  Daniel Wei-Shung Kung ,  Esther Cheng Yin Lee ,  Aaron Christopher Smith ,  Meihua Mike Tu

IPC: C07D405/12 ,  C07D401/12 ,  C07D403/12 ,  C07D401/04

CPC classification number: C07D405/12 ,  A61K31/4439 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.

Abstract translation: 本发明涉及活化5'腺苷单磷酸活化蛋白激酶（AMPK）的式（I）的吲哚和吲唑化合物。 本发明还包括含有这些化合物的药物组合物和用于治疗或预防通过AMPK活化改善的疾病，病症或障碍的方法。

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：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：US20130165452A1

公开(公告)日：2013-06-27

申请号：US13774204

申请日：2013-02-22

Applicant: Pfizer Inc.

Inventor： John William Benbow ,  Jihong Lou ,  Jeffrey Allen Pfefferkorn ,  Meihua Mike Tu

IPC: C07D403/12 ,  C07D413/12 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D231/40 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D513/04

Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.

Abstract translation: 本发明提供作为葡糖激酶活化剂的式（1A）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。 X，Y，Z，R 1，R 2，R 3和R 4如本文所述。