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：US11542270B2

公开(公告)日：2023-01-03

申请号：US16912828

申请日：2020-06-26

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04 ,  A61K31/155 ,  A61K31/4985 ,  A61K31/7048 ,  A61K45/06

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US11203594B2

公开(公告)日：2021-12-21

申请号：US16849329

申请日：2020-04-15

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Douglas Carl Behenna ,  Kimberly O. Cameron ,  Ping Chen ,  John M. Curto ,  Kevin Daniel Freeman-Cook ,  Mehran Jalaie ,  Robert Steven Kania ,  Yajing Lian ,  Sajiv Krishnan Nair ,  Cynthia Louise Palmer ,  Martin Youngjin Pettersson ,  Eugene Yuanjin Rui ,  Matthew Sammons ,  Qingyi Yang ,  Liying Zhang

IPC: C07D471/04 ,  A61P9/12

Abstract: This invention relates to compounds of general Formula I in which A, R1, R2, R3 and R4 are as defined herein, and the pharmaceutically acceptable salts thereof; to pharmaceutical compositions comprising such compounds and salts; to methods of using such compounds, salts and compositions for treating pulmonary hypertension and related diseases, like pulmonary arterial hypertension; to methods of using such compounds, salts and compositions for treating abnormal cell growth, such as cancer; and to processes to make such compounds, salts and compositions.

公开(公告)号：US20210087204A1

公开(公告)日：2021-03-25

申请号：US17078257

申请日：2020-10-23

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US20160130250A1

公开(公告)日：2016-05-12

申请号：US15000944

申请日：2016-01-19

Applicant: PFIZER, INC.

Inventor： Michael Joseph Luzzio ,  Kevin Daniel Freeman-Cook ,  Samit Kumar Bhattacharya ,  Matthew Merrill Hayward ,  Catherine Angela Hulford ,  Christopher Lowell Autry ,  Xumiao Zhao ,  Jun Xiao ,  Kendra Louise Nelson

IPC: C07D401/12

CPC classification number: C07D401/12 ,  C07D239/48 ,  C07D241/20 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D475/00

Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US20220251066A1

公开(公告)日：2022-08-11

申请号：US17458862

申请日：2021-08-27

Applicant: Pfizer Inc.

Inventor： Michael Joseph Luzzio ,  Kevin Daniel Freeman-Cook ,  Samit Kumar Bhattacharya ,  Matthew Merrill Hayward ,  Catherine Angela Hulford ,  Christopher Lowell Autry ,  Xumiao Zhao ,  Jun Xiao ,  Kendra Louise Nelson

IPC: C07D401/12 ,  C07D239/48 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D241/20 ,  C07D475/00

Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US20210024536A1

公开(公告)日：2021-01-28

申请号：US16912828

申请日：2020-06-26

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Leanne Marie Buzon ,  Kevin James Filipski ,  David Andrew Griffith ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D495/04

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US20220363673A1

公开(公告)日：2022-11-17

申请号：US17619912

申请日：2020-06-24

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Christopher Ryan Butler ,  Kevin James Filipski ,  Bethany Lyn Kormos ,  Luis Angel Martinez-Alsina ,  Russell Alan Miller ,  Kiyoyuki Omoto ,  Brian Raymer ,  Matthew Richard Reese ,  Rachel Jane Roth Flach ,  Yuan Zhang

IPC: C07D409/04 ,  A61K45/06 ,  A61K31/41 ,  A61P3/10 ,  A61P9/04

Abstract: Described herein are compounds of Formula I, wherein R1, R2, and R3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.

公开(公告)号：US20170001981A1

公开(公告)日：2017-01-05

申请号：US15263041

申请日：2016-09-12

Applicant: PFIZER, INC.

Inventor： Michael Joseph Luzzio ,  Kevin Daniel Freeman-Cook ,  Samit Kumar Bhattacharya ,  Matthew Merrill Hayward ,  Catherine Angela Hulford ,  Christopher Lowell Autry ,  Xumiao Zhao ,  Jun Xiao ,  Kendra Louise Nelson

IPC: C07D401/12

CPC classification number: C07D401/12 ,  C07D239/48 ,  C07D241/20 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D475/00

Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

Abstract translation: 其中R1至R6，A，B，n和m如本文所定义。 这种新型磺酰基酰胺衍生物可用于治疗哺乳动物中异常细胞生长，如癌症。 本发明还涉及使用这些化合物治疗哺乳动物，特别是人类异常细胞生长的方法以及含有这些化合物的药物组合物。

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。