公开(公告)号：US11059833B2

公开(公告)日：2021-07-13

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 ,  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：US20170073343A1

公开(公告)日：2017-03-16

申请号：US15262112

申请日：2016-09-12

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Matthew Richard Reese ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Martin Youngjin Pettersson ,  Michelle Renee Garnsey

IPC: C07D471/04 ,  C07D471/14 ,  C07D519/00

CPC classification number: A61K31/435 ,  A61K31/4745 ,  C07D215/38 ,  C07D215/42 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

Abstract translation: 其中R1，R1a，R1b，R2，R4，R5，R6，X和Z如说明书中所定义。 本发明还涉及包含式（I）化合物的药物组合物，以及该化合物在治疗与LRRK2相关的疾病中的应用，例如包括帕金森病或阿尔茨海默氏病，癌症，克罗恩病或麻风病的神经变性疾病。

公开(公告)号：US20250099424A1

公开(公告)日：2025-03-27

申请号：US18917336

申请日：2024-10-16

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Qingyi Yang

IPC: A61K31/403 ,  A61K31/401 ,  A61K31/427 ,  A61P31/14 ,  C07D403/12

Abstract: The invention relates to compounds of Formula I″ wherein R, R1, R2, R3, p, q and q′ are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

公开(公告)号：US20240366598A1

公开(公告)日：2024-11-07

申请号：US18634154

申请日：2024-04-12

Applicant: Pfizer Inc.

Inventor： Kevin James Filipski ,  Matthew Forrest Sammons ,  Samuel Michael Levi ,  Yang Wang ,  Advaita Panchagnula ,  Yanfei Guan ,  Matthew Richard Reese ,  Luis Angel Martinez Alsina ,  Steven Victor O'Neil ,  Lei Zhang ,  Qifang Li ,  Ethan Lawrence Fisher ,  Danica Antonia Rankic

IPC: A61K31/506 ,  A61K31/403 ,  A61K31/4439 ,  A61K31/444 ,  A61P3/04 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

Abstract: Described herein are compounds of Formula I: and their pharmaceutically acceptable salts, wherein R1, R2, R3, L1, T1, T2, T3, T4, t1, and t2 are defined herein; their use as GIPR antagonists; pharmaceutical compositions containing such compounds and salts; and the use of such compounds and salts to treat or prevent, for example, obesity, weight gain, and/or T2DM.

公开(公告)号：US11452711B2

公开(公告)日：2022-09-27

申请号：US17660270

申请日：2022-04-22

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Qingyi Yang

IPC: C07D403/12 ,  A61K31/403 ,  A61P31/14 ,  A61K31/427 ,  A61K31/401

Abstract: The invention relates to compounds of Formula I″ wherein R, R1, R2, R3, p, q and q′ are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

公开(公告)号：US11312713B2

公开(公告)日：2022-04-26

申请号：US16492558

申请日：2018-03-06

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Thomas Allen Chappie ,  Jinshan Michael Chen ,  Jotham Wadsworth Coe ,  Karen Jean Coffman ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Christopher John Helal ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Luis Angel Martinez-Alsina ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Colin Richard Rose ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager ,  Joseph Scott Warmus ,  Yuan Zhang

IPC: C07D471/04

Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.

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：US10039753B2

公开(公告)日：2018-08-07

申请号：US15262112

申请日：2016-09-12

Applicant: Pfizer Inc.

Inventor： Karen Jean Coffman ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest ,  Travis T. Wager

IPC: A61K31/435 ,  C07D215/38 ,  C07D471/04 ,  C07D519/00 ,  C07D471/14 ,  C07D215/42 ,  A61K31/4745

CPC classification number: A61K31/435 ,  A61K31/4745 ,  C07D215/38 ,  C07D215/42 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.