公开(公告)号：US20180200253A1

公开(公告)日：2018-07-19

申请号：US15923285

申请日：2018-03-16

Applicant: PFIZER INC.

Inventor： JOTHAM WADSWORTH COE ,  JOHN ARTHUR ALLEN ,  JENNIFER ELIZABETH DAVOREN ,  AMY BETH DOUNAY ,  IVAN VIKTOROVICH EFREMOV ,  DAVID LAWRENCE FIRMAN GRAY ,  EDWARD RAYMOND GUILMETTE ,  ANTHONY RICHARD HARRIS ,  CHRISTOPHER JOHN HELAL ,  JACLYN LOUISE HENDERSON ,  SCOT RICHARD MENTE ,  DEANE MILFORD NASON ,  STEVEN VICTOR O'NEIL ,  CHAKRAPANI SUBRAMANYAM ,  WENJIAN XU

IPC: A61K31/53 ,  A61K31/519 ,  A61K31/506 ,  A61K31/5025 ,  A61K31/501 ,  A61K31/4355 ,  A61K31/497 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/4985

CPC classification number: A61K31/53 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D519/04

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds and the uses of such compounds for the treatment of D1-mediated (or D1-associated) disorders including cognitive and motivational impairments and negative symptoms associated with illnesses such as schizophrenia, depression, bipolar disorder, Parkinson's disease, Mild cognitive impairment (MCI), Alzheimer's disease, lupus, Huntington's disease, Parkinson's, dyskinesia, ADHD, post-traumatic stress disorder, autism spectrum disorder, treatment-resistant depression, major depressive disorder (MDD), drug dependence, Tourette's syndrome, tardive dyskinesias as well as impairments associated with age, chronic stress, sleep deprivation, combat, chronic fatigue; endocrine or metabolic diseases such as hyperglycemia, dislipidemia, diabetes, obesity, and sepsis; and cardiovascular disorder such as hypertension.

公开(公告)号：US20170037049A1

公开(公告)日：2017-02-09

申请号：US15305390

申请日：2015-04-15

Applicant: PFIZER INC.

Inventor： DAVID LAWRENCE FIRMAN GRAY ,  JENNIFER ELIZABETH DAVOREN ,  AMY BETH DOUNAY ,  IVAN VIKTOROVICH EFREMOV ,  SCOT RICHARD MENTE ,  CHAKRAPANI SUBRAMANYAM

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D519/00

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：US20150344490A1

公开(公告)日：2015-12-03

申请号：US14820611

申请日：2015-08-07

Applicant: PFIZER INC.

Inventor： JOTHAM WADSWORTH COE ,  JOHN ARTHUR ALLEN ,  JENNIFER ELIZABETH DAVOREN ,  AMY BETH DOUNAY ,  IVAN VIKTOROVICH EFREMOV ,  DAVID LAWRENCE FIRMAN GRAY ,  EDWARD RAYMOND GUILMETTE ,  ANTHONY RICHARD HARRIS ,  CHRIS JOHN HELAL ,  JACLYN LOUISE HENDERSON ,  SCOT RICHARD MENTE ,  DEANE MILFORD NASON ,  STEVEN VICTOR O'NEIL ,  CHAKRAPANI SUBRAMANYAM ,  WENJIAN XU

IPC: C07D491/048 ,  C07D495/04 ,  C07D519/00

CPC classification number: A61K31/53 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61P25/00 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D519/04

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

公开(公告)号：US20150307522A1

公开(公告)日：2015-10-29

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: C07D519/00 ,  C07D471/04 ,  C07D491/147 ,  C07D495/14 ,  C07D513/04

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.