公开(公告)号：US11014909B2

公开(公告)日：2021-05-25

申请号：US16880632

申请日：2020-05-21

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Michael Eric Green ,  Jaclyn Louise Henderson ,  Chewah Lee ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Lei Zhang

IPC: A61K31/513 ,  A61K31/506 ,  A61K31/501 ,  A61K31/444 ,  A61P25/18 ,  A61P25/28 ,  A61P25/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), Parkinson's disease and chronic apathy.

公开(公告)号：US20210017172A1

公开(公告)日：2021-01-21

申请号：US16926933

申请日：2020-07-13

Applicant: Pfizer Inc.

Inventor： Omar Ahmad ,  Andrew Fensome ,  Erik Alphie LaChapelle ,  Ethan Lawrence Fisher ,  Rayomand J. Unwalla ,  Jun Xiao ,  Lei Zhang

IPC: C07D471/04 ,  A61K31/437

Abstract: The present invention relates to imidazo-pyridinyl compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.

公开(公告)号：US20190367485A1

公开(公告)日：2019-12-05

申请号：US16539865

申请日：2019-08-13

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Michael Eric Green ,  Jaclyn Louise Henderson ,  Chewah Lee ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Lei Zhang

IPC: C07D401/14 ,  C07D403/12 ,  A61K31/513 ,  A61K31/501 ,  A61K31/506 ,  A61K31/444 ,  C07D405/14 ,  C07D401/12

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.

公开(公告)号：US09771379B2

公开(公告)日：2017-09-26

申请号：US15272651

申请日：2016-09-22

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill

IPC: A01N43/00 ,  A61K31/553 ,  C07D498/04 ,  C07D498/10

CPC classification number: C07D498/04 ,  C07D498/10

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2, R3, R4 and X 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：US09688698B2

公开(公告)日：2017-06-27

申请号：US14694039

申请日：2015-04-23

Applicant: PFIZER INC.

Inventor： David Lawrence Firman Gray ,  Lei Zhang ,  Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  Scot Richard Mente ,  Chakrapani Subramanyam

IPC: C07D495/14 ,  C07D519/00 ,  C07D471/04 ,  C07D491/147 ,  C07D513/04 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  C07D491/048 ,  C07D495/04 ,  A61K31/4985

CPC classification number: C07D519/00 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  C07D471/04 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D495/14 ,  C07D513/04

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.

公开(公告)号：US20170088547A1

公开(公告)日：2017-03-30

申请号：US15272820

申请日：2016-09-22

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Patrick Robert Verhoest ,  Romelia del Carmen Salomon Ferrer

IPC: C07D417/14

CPC classification number: C07D417/14

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1, R2 and R3 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：US20160152637A1

公开(公告)日：2016-06-02

申请号：US15019342

申请日：2016-02-09

Applicant: Pfizer Inc.

Inventor： Michael Aaron Brodney ,  Elizabeth Mary Beck ,  Christopher Ryan Butler ,  Lei Zhang ,  Brian Thomas O'Neill ,  Gabriela Barreiro ,  Erik Alphie LaChapelle ,  Bruce Nelsen Rogers

IPC: C07D513/04 ,  C07D519/00

CPC classification number: A61K31/542 ,  C07D513/04 ,  C07D519/00

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

公开(公告)号：US09133190B2

公开(公告)日：2015-09-15

申请号：US14339123

申请日：2014-07-23

Applicant: PFIZER INC.

Inventor： Jennifer Elizabeth Davoren ,  Amy Beth Dounay ,  Ivan Viktorovich Efremov ,  David Lawrence Firman Gray ,  Scot Richard Mente ,  Steven Victor O'Neil ,  Bruce Nelsen Rogers ,  Chakrapani Subramanyam ,  Lei Zhang

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

CPC classification number: C07D471/04 ,  A61K31/437 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐和上述的N-氧化物; 制备过程; 中间体用于制备; 和含有这些化合物，盐或N-氧化物的组合物及其用于治疗D1介导的（或D1相关）疾病的用途，包括例如精神分裂症（例如，其认知和负面症状），认知障碍（例如，认知障碍相关 精神分裂症，AD，PD或药物治疗），ADHD，冲动，强迫性赌博，暴饮暴食，孤独症谱系障碍，MCI，年龄相关认知衰退，痴呆，RLS，帕金森病，亨廷顿舞蹈病，焦虑，抑郁，MDD，TRD 和双相情感障碍。

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：US20240245673A1

公开(公告)日：2024-07-25

申请号：US18532424

申请日：2023-12-07

Applicant: Pfizer Inc.

Inventor： James Matthew Frick ,  Michelle Renee Garnsey ,  Brian Stephen Gerstenberger ,  Xinjun Hou ,  Magdalena Korczynska ,  Alpha Albert Lee ,  Luong Tien Nguyen ,  Usa Reilly ,  Matthew Christopher Robinson ,  Alexandria Paige Taylor ,  Thomas Reynold Vargo ,  Lei Zhang

IPC: A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

CPC classification number: A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (I)




and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.