公开(公告)号：US20150366874A1

公开(公告)日：2015-12-24

申请号：US14840528

申请日：2015-08-31

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Antonia Friederike Stepan ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 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: 本发明提供了式I的新的4,5-二取代的-7H-吡咯并[2,3-d]嘧啶衍生物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5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病，神经变性疾病或克罗恩病或麻风病的神经变性疾病。

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：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：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.

公开(公告)号：US09695171B2

公开(公告)日：2017-07-04

申请号：US15104659

申请日：2014-12-03

Applicant: Pfizer Inc.

Inventor： Paul Galatsis ,  Matthew Merrill Hayward ,  Bethany Lyn Kormos ,  Travis T. Wager ,  Lei Zhang ,  Jaclyn Louise Henderson ,  Ravi G. Kurumbail ,  Patrick Robert Verhoest ,  Antonia Friederike Stepan

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D491/08 ,  C07D498/08

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D519/00

Abstract: The present invention provides novel 3,4-disubstituted-1H-pyrrolo[2,3-b]pyridine derivatives and 4,5-disubstituted-7H-pyrrolo[2,3-c]pyridazine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and X 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：US20140329820A1

公开(公告)日：2014-11-06

申请号：US14265458

申请日：2014-04-30

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Christopher John Helal ,  Bethany Lyn Kormos ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest

IPC: C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D471/04

CPC classification number: C07D519/00 ,  A61K31/4353 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.

Abstract translation: 本发明涉及如下式I所述的新一类三嗪衍生物，其中A，X，R 1，R 2，R 3和R 4如本文所定义，以及该化合物作为PDE10抑制剂的用途。

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：US20200157098A1

公开(公告)日：2020-05-21

申请号：US16750505

申请日：2020-01-23

Applicant: PFIZER INC.

Inventor： Thomas Allen Chappie ,  Jaclyn Louise Henderson ,  Joseph Michael Young ,  Travis T. Wager ,  Bethany Lyn Kormos ,  Nandini Chaturbhai Patel ,  Simone Sciabola ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Joseph Walter Tucker

IPC: C07D471/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/18 ,  A61P25/16 ,  A61K31/55

Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, R4, R5, a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders including, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual disorders and depression.