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：US20230019853A1

公开(公告)日：2023-01-19

申请号：US17341877

申请日：2021-06-08

Applicant: Pfizer Inc.

Inventor： Christopher Ryan Butler ,  Michelle Renee Garnsey ,  Kevin Alexander Ogilvie ,  Jana Polivkova ,  Matthew Forrest Sammons ,  Aaron Christopher Smith ,  Qingyi Yang

IPC: C07D471/20 ,  C07D519/00

Abstract: Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

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：US11643412B2

公开(公告)日：2023-05-09

申请号：US17341877

申请日：2021-06-08

Applicant: Pfizer Inc.

Inventor： Christopher Ryan Butler ,  Michelle Renee Garnsey ,  Kevin Alexander Ogilvie ,  Jana Polivkova ,  Matthew Forrest Sammons ,  Aaron Christopher Smith ,  Qingyi Yang

IPC: C07D471/20 ,  C07D519/00 ,  A61K31/438 ,  A61P1/08 ,  A61P3/04 ,  A61P19/00 ,  A61P21/00 ,  A61P29/00

CPC classification number: C07D471/20 ,  C07D519/00 ,  C07B2200/13

Abstract: Described herein are compounds of Formula I:




and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

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：US20250129048A1

公开(公告)日：2025-04-24

申请号：US18713747

申请日：2022-12-05

Applicant: Pfizer Inc.

Inventor： Michelle Renee Garnsey ,  David Andrew Griffith ,  Christopher John Helal ,  Daniel Wei-Shung Kung ,  Yajing Lian ,  Kevin Alexander Ogilvie ,  Jana Polivkova ,  Brian Raymer ,  Matthew Forrest Sammons ,  Aaron Christopher Smith ,  Qingyi Yang

IPC: C07D401/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

Abstract: Described herein are compounds of Formula I: I and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R7, RF, t1, Y1, and Y2 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

公开(公告)号：US12187727B2

公开(公告)日：2025-01-07

申请号：US18162052

申请日：2023-01-31

Applicant: Pfizer Inc.

Inventor： Christopher Ryan Butler ,  Michelle Renee Garnsey ,  Kevin Alexander Ogilvie ,  Jana Polivkova ,  Matthew Forrest Sammons ,  Aaron Christopher Smith ,  Qingyi Yang

IPC: A61K31/438 ,  A61P1/08 ,  A61P3/04 ,  A61P19/00 ,  A61P21/00 ,  A61P29/00 ,  C07D471/20 ,  C07D519/00

Abstract: Described herein are methods of treating MC4R-related conditions, diseases, or disorders by administering compounds of Formula I: or their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein. Such conditions, diseases, or disorders include cachexia, anorexia, or anorexia nervosa.