公开(公告)号：US09394285B2

公开(公告)日：2016-07-19

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 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61P13/12 ,  A61P3/10

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：US20150099782A1

公开(公告)日：2015-04-09

申请号：US14506752

申请日：2014-10-06

Applicant: PFIZER INC.

Inventor： Kevin Barry Bahnck ,  David James Edmonds ,  Kentaro Futatsugi ,  Esther Cheng Yin Lee ,  Alan Martin Mathiowetz ,  Elnaz Menhaji-Klotz ,  Robert Vernon Stanton

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.

Abstract translation: 本文提供前列腺素EP3受体的拮抗剂，制备所述拮抗剂的方法，以及包括向有需要的哺乳动物施用所述拮抗剂的方法。

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：US11866425B2

公开(公告)日：2024-01-09

申请号：US17345064

申请日：2021-06-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: A61K31/505 ,  A61P3/00 ,  A61P3/10 ,  A61P3/06 ,  C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  C07B2200/13

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US20210309646A1

公开(公告)日：2021-10-07

申请号：US17345064

申请日：2021-06-11

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D409/14

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US20200181127A1

公开(公告)日：2020-06-11

申请号：US16793441

申请日：2020-02-18

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  C07D409/14 ,  A61K45/06 ,  A61K31/506 ,  C07D401/14

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

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：US20240336572A1

公开(公告)日：2024-10-10

申请号：US18626467

申请日：2024-04-04

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Edward Lee Conn ,  David Christopher Ebner ,  Brian Stephen Gerstenberger ,  Chan Woo Huh ,  Daniel Wei-Shung Kung ,  Alan Martin Mathiowetz ,  Jessica Gloria Katherine O'Brien ,  Meihua Mike Tu ,  Kimberly O'Keefe Cameron ,  Dilinie Prasadhini Fernando ,  Kevin James Filipski ,  Esther Cheng Yin Lee ,  Sarah Jane Mear ,  Aaron Christopher Smith

IPC: C07D231/56 ,  A61K31/416

CPC classification number: C07D231/56 ,  A61K31/416

Abstract: The invention relates to substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof that can activate adenosine 5′-monophosphate-activated protein kinase (AMPK). The invention further relates to pharmaceutical compositions comprising AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof and at least one pharmaceutically acceptable excipient, and methods of treating a condition comprising administering AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof.

公开(公告)号：US20240140937A1

公开(公告)日：2024-05-02

申请号：US18520638

申请日：2023-11-28

Applicant: Pfizer Inc.

Inventor： Markus Boehm ,  Shawn Cabral ,  Matthew S. Dowling ,  Kentaro Futatsugi ,  Kim Huard ,  Esther Cheng Yin Lee ,  Allyn T. Londregan ,  Jana Polivkova ,  David A. Price ,  Qifang Li

IPC: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D405/14 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  A61P3/06

Abstract: Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.

公开(公告)号：US09738626B2

公开(公告)日：2017-08-22

申请号：US14970930

申请日：2015-12-16

Applicant: Pfizer Inc.

Inventor： Kevin Bahnck ,  Daniel Canterbury ,  David James Edmonds ,  Kentaro Futatsugi ,  Esther Cheng Yin Lee ,  Elnaz Menhaji-Klotz ,  Jana Polivkova ,  Robert Vernon Stanton

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.