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：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：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：US11161844B2

公开(公告)日：2021-11-02

申请号：US16492554

申请日：2018-03-01

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Christopher John Helal ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Luis Angel Martinez-Alsina ,  Martin Youngjin Pettersson ,  Antonia Friederike Stepan ,  Travis T. Wager

IPC: C07D471/04 ,  C07D471/14

Abstract: The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof; wherein R1, 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.

公开(公告)号：US20200039977A1

公开(公告)日：2020-02-06

申请号：US16492554

申请日：2018-03-01

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Paul Galatsis ,  Michelle Renee Garnsey ,  Christopher John Helal ,  Jaclyn Louise Henderson ,  Bethany Lyn Kormos ,  Ravi G. Kurumbail ,  Luis Angel Martinez-Alsina ,  Martin Youngjin Pettersson ,  Antonia Friederike Stepan ,  Travis T. Wager

IPC: C07D471/04 ,  C07D471/14

Abstract: The present invention provides novel cyclic substituted imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof, wherein R1, 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.

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.