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：US20170165270A1

公开(公告)日：2017-06-15

申请号：US15446369

申请日：2017-03-01

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

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 (N-oxides thereof or or pharmaceutically acceptable salts of the compound or the N-oxides) and the uses of such compounds (N-oxides thereof or or pharmaceutically acceptable salts of the compound or the N-oxides) 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. The present invention further provides a D1 agonist with reduced D1R desensitization, a D1 agonist with a reduced β-arrestin recruitment activity relative to Dopamine, a D1 agonist interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, a D1 agonist interacting less strongly 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：US20170029390A1

公开(公告)日：2017-02-02

申请号：US15221658

申请日：2016-07-28

Applicant: PFIZER INC.

Inventor： CHRISTOPHER RYAN BUTLER ,  LAURA ANN MCALLISTER ,  ELIZABETH MARY BECK ,  MICHAEL AARON BRODNEY ,  ADAM MATTHEW GILBERT ,  CHRISTOPHER JOHN HELAL ,  DOUGLAS SCOTT JOHNSON ,  JUSTIN IAN MONTGOMERY ,  STEVEN VICTOR O'NEIL ,  BRUCE NELSEN ROGERS ,  PATRICK ROBERT VERHOEST ,  DAMIEN WEBB

IPC: C07D295/14 ,  C07D401/04 ,  C07D403/04 ,  C07D498/10 ,  C07D491/107 ,  C07D405/14 ,  C07D471/10 ,  C07D487/04 ,  C07D211/48 ,  C07D471/08 ,  C07D515/10 ,  C07F9/6561 ,  C07D401/14 ,  C07D401/12

CPC classification number: C07D295/14 ,  C07D211/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D493/10 ,  C07D498/10 ,  C07D515/10 ,  C07F9/6561

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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

Abstract translation: 和其药学上可接受的盐; 制备过程; 中间体用于制备; 含有这些化合物或盐的组合物及其用于治疗MAGL介导的疾病和病症的用途，包括例如疼痛，炎性疾病，创伤性脑损伤，抑郁症，焦虑症，阿尔茨海默病，代谢紊乱，中风或癌症。

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。