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：US09296761B2

公开(公告)日：2016-03-29

申请号：US14829842

申请日：2015-08-19

Applicant: Pfizer Inc.

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

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  A61K31/53 ,  A61K31/4353

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.

公开(公告)号：US09145427B2

公开(公告)日：2015-09-29

申请号：US14549871

申请日：2014-11-21

Applicant: Pfizer Inc.

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

IPC: C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/53 ,  A61K31/4353 ,  A61P9/12 ,  C07D519/00

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：US09120788B2

公开(公告)日：2015-09-01

申请号：US14180463

申请日：2014-02-14

Applicant: Pfizer Inc.

Inventor： Thomas Allen Chappie ,  Patrick Robert Verhoest ,  Nandini Chaturbhai Patel ,  Matthew Merrill Hayward

IPC: C07D401/14 ,  A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，其中取代基如本文所定义。

公开(公告)号：US20150080401A1

公开(公告)日：2015-03-19

申请号：US14549871

申请日：2014-11-21

Applicant: Pfizer Inc.

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

IPC: C07D519/00 ,  C07D487/04

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.

公开(公告)号：US20140005183A1

公开(公告)日：2014-01-02

申请号：US13928696

申请日：2013-06-27

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: C07D487/04 ,  C07D519/00

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：US20230218616A1

公开(公告)日：2023-07-13

申请号：US17904537

申请日：2021-02-22

Applicant: Pfizer Inc.

Inventor： Neeta Balkrishan Amin ,  Arthur James Bergman ,  Roberto Arnaldo Calle ,  William Paul Esler ,  Albert Myung Kim ,  Jeffrey Allen Pfefferkorn ,  Patrick Robert Verhoest

IPC: A61K31/506 ,  A61K31/438 ,  A61P1/16 ,  A61P3/00

CPC classification number: A61K31/506 ,  A61K31/438 ,  A61P1/16 ,  A61P3/00 ,  C07B2200/13

Abstract: A method for treating fatty liver disease and related diseases or disorders with a therapeutically effective amount of a composition comprising from about 25 mg to about 1200 mg of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or a pharmaceutically acceptable salt thereof, and from about 5 mg to about 40 mg of 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4′-piperidine]-1′-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20230146535A1

公开(公告)日：2023-05-11

申请号：US17964491

申请日：2022-10-12

Applicant: PFIZER INC.

Inventor： Thomas Allen Chappie ,  Nandini Chaturbhai Patel ,  Patrick Robert Verhoest ,  Christopher John Helal ,  Simone Sciabola ,  Erik Alphie LaChapelle ,  Travis T. Wager ,  Ramalakshmi Yegna Chandrasekaran

IPC: C07D471/14 ,  C07D491/147 ,  C07D491/22 ,  C07D513/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/14 ,  C07D498/22 ,  C07D471/22

CPC classification number: C07D471/14 ,  C07D491/147 ,  C07D491/22 ,  C07D513/14 ,  C07D519/00 ,  C07D487/04 ,  C07D487/14 ,  C07D498/22 ,  C07D471/22

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

公开(公告)号：US11541034B2

公开(公告)日：2023-01-03

申请号：US17554091

申请日：2021-12-17

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Liuqing Wei ,  Qingyi Yang ,  Xiaojing Yang

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

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：US20220142976A1

公开(公告)日：2022-05-12

申请号：US17554091

申请日：2021-12-17

Applicant: Pfizer Inc.

Inventor： Dafydd Rhys Owen ,  Martin Youngjin Pettersson ,  Matthew Richard Reese ,  Matthew Forrest Sammons ,  Jamison Bryce Tuttle ,  Patrick Robert Verhoest ,  Liuqing Wei ,  Qingyi Yang ,  Xiaojing Yang

IPC: A61K31/403 ,  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.