公开(公告)号：US20180346477A1

公开(公告)日：2018-12-06

申请号：US16100668

申请日：2018-08-10

Applicant: PFIZER INC.

Inventor： DAVID LAWRENCE FIRMAN GRAY ,  LEI ZHANG ,  JENNIFER ELIZABETH DAVOREN ,  AMY BETH DOUNAY ,  IVAN VIKTOROVICH EFREMOV ,  CHEWAH LEE ,  SCOT RICHARD MENTE ,  STEVEN VICTOR O'NEIL ,  BRUCE NELSEN ROGERS ,  CHAKRAPANI SUBRAMANYAM

IPC: C07D491/048 ,  C07D498/04 ,  C07D471/04

CPC classification number: C07D491/048 ,  C07D471/04 ,  C07D498/04

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：US20180072750A1

公开(公告)日：2018-03-15

申请号：US15822493

申请日：2017-11-27

Applicant: PFIZER INC.

Inventor： DAVID LAWRENCE FIRMAN GRAY ,  LEI ZHANG ,  JENNIFER ELIZABETH DAVOREN ,  AMY BETH DOUNAY ,  IVAN VIKTOROVICH EFREMOV ,  CHEWAH LEE ,  SCOT RICHARD MENTE ,  STEVEN VICTOR O'NEIL ,  BRUCE NELSEN ROGERS ,  CHAKRAPANI SUBRAMANYAM

IPC: C07D491/048 ,  C07D498/04 ,  C07D471/04

CPC classification number: C07D491/048 ,  C07D471/04 ,  C07D498/04

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：US20160016907A1

公开(公告)日：2016-01-21

申请号：US14799621

申请日：2015-07-15

Applicant: PFIZER INC.

Inventor： MICHAEL AARON BRODNEY ,  JENNIFER ELIZABETH DAVOREN ,  MICHELLE RENEE GARNSEY ,  LEI ZHANG ,  STEVEN VICTOR O'NEIL

IPC: C07D213/81 ,  C07D417/14 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D213/81 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention provides, in part, compounds of Formula I: N-oxides thereof, and pharmaceutically acceptable salts of the compounds or N-oxides; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M1-mediated (or M1-associated) disorders including, e.g., Alzheimer's disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

Abstract translation: 本发明部分提供式I的化合物：其N-氧化物和化合物或N-氧化物的药学上可接受的盐; 制备过程; 中间体用于制备; 以及含有这些化合物，N-氧化物或盐的组合物及其用于治疗M1介导的（或M1相关）疾病的用途，包括例如阿尔茨海默病，精神分裂症（例如其认知和阴性症状），疼痛，成瘾， 和睡眠障碍。

公开(公告)号：US20140336176A1

公开(公告)日：2014-11-13

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: C07D471/04

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：US20140128374A1

公开(公告)日：2014-05-08

申请号：US14072563

申请日：2013-11-05

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: C07D471/04

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.

公开(公告)号：US20170044174A1

公开(公告)日：2017-02-16

申请号：US15305384

申请日：2015-04-14

Applicant: PFIZER INC.

Inventor： DAVID LAWRENCE FIRMAN GRAY ,  LEI ZHANG ,  MICHAEL AARON BRODNEY ,  JENNIFER ELIZABETH DAVOREN ,  IVAN VIKTOROVICH EFREMOV ,  MICHAEL ERIC GREEN ,  STEVEN VICTOR O'NEIL ,  BRUCE NELSEN ROGERS

IPC: C07D491/048 ,  C07D403/12 ,  C07D491/052 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D491/048 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052

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.

Abstract translation: 本发明部分提供式（I）的化合物及其药学上可接受的盐; 制备过程; 中间体用于制备; 以及含有这些化合物或盐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（例如其认知和阴性症状），分裂型人格障碍，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，帕金森病，焦虑和抑郁。

公开(公告)号：US20150344474A1

公开(公告)日：2015-12-03

申请号：US14819541

申请日：2015-08-06

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: C07D471/04 ,  C07D519/00

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：US20150307494A1

公开(公告)日：2015-10-29

申请号：US14694333

申请日：2015-04-23

Applicant: PFIZER INC.

Inventor： DAVID LAWRENCE FIRMAN GRAY ,  LEI ZHANG ,  MICHAEL AARON BRODNEY ,  MICHAEL ERIC GREEN ,  CHAKRAPANI SUBRAMANYAM

IPC: C07D471/04 ,  C07D401/12

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D471/04

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.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐; 制备过程; 中间体用于制备; 和含有这些化合物或盐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（例如其认知和阴性症状），分裂型人格障碍，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，帕金森病，焦虑和抑郁。

公开(公告)号：US20150005313A1

公开(公告)日：2015-01-01

申请号：US14311963

申请日：2014-06-23

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 ,  C07D401/12

CPC classification number: C07D401/14 ,  A61K31/444 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  C07D401/12 ,  C07D403/12 ,  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), age-related cognitive decline, dementia, and Parkinson's disease.

Abstract translation: 本发明部分提供式I化合物及其药学上可接受的盐; 制备过程; 中间体用于制备; 和含有这些化合物或盐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，与精神分裂症相关的认知障碍，AD ，PD或药物治疗），年龄相关的认知衰退，痴呆和帕金森病。

公开(公告)号：US20240182468A1

公开(公告)日：2024-06-06

申请号：US18484527

申请日：2023-10-11

Applicant: PFIZER INC.

Inventor： GARY ERIK ASPNES ,  CHRISTOPHER RYAN BUTLER ,  MATTHEW FRANK PAUL CALABRESE ,  KIMBERLY O'KEEFE CAMERON ,  JOHN MARION CURTO ,  MICHAEL ERIC GREEN ,  XINJUN HOU ,  SHENPING LIU ,  CHRISTOPHER LEE MCCLENDON ,  JOHN CHARLES MURRAY ,  ADVAITA PANCHAGNULA ,  COLIN RICHARD ROSE ,  KYLE THOMAS TARANTINO ,  MEIHUA MIKE TU ,  RAYOMAND JAL UNWALLA ,  JOSEPH SCOTT WARMUS ,  JUN XIAO ,  QINGYI YANG ,  LEI ZHANG

IPC: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

Abstract: Described herein are compounds of Formula I,






wherein the variables are defined herein, their use as activators from AMPK, pharmaceutical compositions containing such compounds and their use to treat, for example, heart failure or peripheral vascular disease.