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：US20190002439A1

公开(公告)日：2019-01-03

申请号：US16123072

申请日：2018-09-06

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

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), and Parkinson's disease.

公开(公告)号：US20180208608A1

公开(公告)日：2018-07-26

申请号：US15876698

申请日：2018-01-22

Applicant: PFIZER INC.

Inventor： MICHAEL AARON BRODNEY ,  CHRISTOPHER RYAN BUTLER ,  LAURA ANN MCALLISTER ,  CHRISTOPHER JOHN HELAL ,  STEVEN VICTOR O'NEIL ,  PATRICK ROBERT VERHOEST

IPC: C07D513/10 ,  C07D221/20 ,  A61P35/00 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00

Abstract: The present invention provides, in part, heterocyclic spiro 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, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

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：US20180065943A1

公开(公告)日：2018-03-08

申请号：US15808242

申请日：2017-11-09

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

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.

公开(公告)号：US20170057947A1

公开(公告)日：2017-03-02

申请号：US15349075

申请日：2016-11-11

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 ,  C07D405/14 ,  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), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCl, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, bipolar disorder, chronic apathy, anhedonia, chronic fatigue, post-traumatic stress disorder, seasonal affective disorder, social anxiety disorder, post-partum depression, serotonin syndrome, substance abuse and drug dependence, drug abuse relapse, Tourette's syndrome, tardive dyskinesia, drowsiness, excessive daytime sleepiness, cachexia, inattention, sexual dysfunction, migraine, SLE, hyperglycemia, atherosclerosis, dislipidemia, obesity, diabetes, sepsis, post-ischemic tubular necrosis, renal failure, hyponatremia, resistant edema, narcolepsy, hypertension, congestive heart failure, postoperative ocular hypotonia, sleep disorders, and pain.

Abstract translation: 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），ADHD，冲动性，强迫性赌博，暴饮暴食，孤独症谱系障碍，MCl，年龄相关认知衰退，痴呆，RLS，帕金森病，亨廷顿舞蹈症，焦虑症，抑郁症，MDD，TRD，双相情感障碍， 慢性冷漠，慢性疲劳，创伤后应激障碍，季节性情绪障碍，社会焦虑症，产后抑郁症，血清素综合征，药物滥用和毒品依赖，药物滥用复发，Tourette综合征，迟发性运动障碍，嗜睡，白天过度 嗜睡，恶病质，注意力不集中，性功能障碍，偏头痛，SLE，高血糖症，动脉粥样硬化，血脂异常，肥胖，糖尿病，败血症，缺血后小管 坏死，肾衰竭，低钠血症，抗性水肿，发作性睡病，高血压，充血性心力衰竭，术后眼睛低血压，睡眠障碍和疼痛。

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：US20190276472A1

公开(公告)日：2019-09-12

申请号：US16420544

申请日：2019-05-23

Applicant: PFIZER INC.

Inventor： MICHAEL AARON BRODNEY ,  CHRISTOPHER RYAN BUTLER ,  LAURA ANN MCALLISTER ,  CHRISTOPHER JOHN HELAL ,  STEVEN VICTOR O'NEIL ,  PATRICK ROBERT VERHOEST

IPC: C07D513/10 ,  C07D295/185 ,  C07D491/10 ,  C07D221/20 ,  C07D401/08 ,  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 MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

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：US20180208607A1

公开(公告)日：2018-07-26

申请号：US15874987

申请日：2018-01-19

Applicant: PFIZER INC.

Inventor： MICHAEL AARON BRODNEY ,  CHRISTOPHER RYAN BUTLER ,  LAURA ANN MCALLISTER ,  CHRISTOPHER JOHN HELAL ,  STEVEN VICTOR O'NEIL ,  PATRICK ROBERT VERHOEST

IPC: C07D513/10 ,  C07D221/20

CPC classification number: C07D513/10 ,  C07D221/20 ,  C07D295/185 ,  C07D401/08 ,  C07D401/12 ,  C07D491/10

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, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.