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：US20220017548A1

公开(公告)日：2022-01-20

申请号：US17365213

申请日：2021-07-01

Applicant: Pfizer Inc.

Inventor： Robert Steven Kania ,  Padmavani Bezawada ,  Emma Louise Hawking ,  Rohit Jaini ,  Samir Kulkarni ,  Matthew Nathan O'Brien Laramy ,  Jonathan Richard Lillis ,  Suman Luthra ,  Dafydd Rhys Owen ,  Klimentina Dimitrova Pencheva ,  Martin Youngjin Pettersson ,  Anil Mahadeo Rane ,  Matthew Forrest Sammons ,  Bradley Paul Sullivan ,  Andrew John Thiel ,  Martyn David Ticehurst ,  Jamison Bryce Tuttle ,  Robert Louis Hoffman

IPC: C07F9/572 ,  A61P31/14

Abstract: The invention relates to compounds of formula I wherein R1, R2 and - - - - - are as defined herein, pharmaceutical compositions comprising the compounds and methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.

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.

公开(公告)号：US20170166566A1

公开(公告)日：2017-06-15

申请号：US15441882

申请日：2017-02-24

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  John Michael Humphrey ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Danica Antonia Rankic ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b,R5a, R5b, R6, R7, y and z are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US20160222007A1

公开(公告)日：2016-08-04

申请号：US15012954

申请日：2016-02-02

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Christopher William am Ende ,  Douglas Scott Johnson ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61K31/4985 ,  A61P25/28

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有式I的结构，其中X，R1，R2a，R2b，R4a，R4b，R5a，R5b，R6，R7，R10，R11和y定义如上 在规范中。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20150072990A1

公开(公告)日：2015-03-12

申请号：US14543020

申请日：2014-11-17

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。