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1.
公开(公告)号:US20140336176A1
公开(公告)日:2014-11-13
申请号:US14339123
申请日:2014-07-23
申请人: PFIZER INC.
发明人: 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分类号: C07D471/04
CPC分类号: C07D471/04 , A61K31/437 , C07D401/04 , C07D401/14 , C07D519/00
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20140128374A1
公开(公告)日:2014-05-08
申请号:US14072563
申请日:2013-11-05
申请人: PFIZER INC.
发明人: 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分类号: C07D471/04
CPC分类号: C07D471/04 , A61K31/437 , C07D401/04 , C07D401/14 , C07D519/00
摘要: 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.
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公开(公告)号:US20180037571A1
公开(公告)日:2018-02-08
申请号:US15729111
申请日:2017-10-10
申请人: PFIZER INC.
发明人: 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分类号: C07D401/14 , C07D401/12 , A61K31/513 , A61K31/506 , A61K31/501 , C07D405/14 , A61K31/444
CPC分类号: C07D401/14 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/513 , C07D401/12 , C07D403/12 , C07D405/14
摘要: 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.
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4.
公开(公告)号:US20170037053A1
公开(公告)日:2017-02-09
申请号:US15305372
申请日:2015-04-13
申请人: PFIZER INC.
发明人: 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分类号: C07D491/048 , C07D498/04 , C07D471/04
CPC分类号: C07D491/048 , C07D471/04 , C07D498/04
摘要: 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.
摘要翻译: 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。
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公开(公告)号:US20150196561A1
公开(公告)日:2015-07-16
申请号:US14638677
申请日:2015-03-04
申请人: PFIZER INC.
发明人: 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分类号: A61K31/513 , A61K31/501
CPC分类号: C07D401/14 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/513 , C07D401/12 , C07D403/12 , C07D405/14
摘要: 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.
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6.
公开(公告)号:US20150175573A1
公开(公告)日:2015-06-25
申请号:US14638608
申请日:2015-03-04
申请人: PFIZER INC.
发明人: 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分类号: C07D401/12
CPC分类号: C07D401/14 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/513 , C07D401/12 , C07D403/12 , C07D405/14
摘要: 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, MCI, 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.
摘要翻译: 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),ADHD,冲动性,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。
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公开(公告)号:US20190382359A1
公开(公告)日:2019-12-19
申请号:US16547037
申请日:2019-08-21
申请人: PFIZER INC.
发明人: 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分类号: C07D295/14 , C07D493/10 , C07D405/12 , C07D413/14 , C07D405/14 , C07F9/6561 , C07D515/10 , C07D471/08 , C07D211/48 , C07D487/04 , C07D471/10 , C07D401/12 , C07D491/107 , C07D498/10 , C07D403/04 , C07D401/04 , C07D401/14
摘要: 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.
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公开(公告)号:US20170044174A1
公开(公告)日:2017-02-16
申请号:US15305384
申请日:2015-04-14
申请人: PFIZER INC.
发明人: 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分类号: C07D491/048 , C07D403/12 , C07D491/052 , C07D471/04 , C07D487/04
CPC分类号: C07D491/048 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/052
摘要: 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.
摘要翻译: 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。
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9.
公开(公告)号:US20150344474A1
公开(公告)日:2015-12-03
申请号:US14819541
申请日:2015-08-06
申请人: PFIZER INC.
发明人: 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分类号: C07D471/04 , C07D519/00
CPC分类号: C07D471/04 , A61K31/437 , C07D401/04 , C07D401/14 , C07D519/00
摘要: 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.
摘要翻译: 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。
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10.
公开(公告)号:US20150291625A1
公开(公告)日:2015-10-15
申请号:US14435954
申请日:2013-10-29
申请人: PFIZER INC.
发明人: 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分类号: C07D519/00 , C07D495/04 , C07D491/048
CPC分类号: 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
摘要: 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.
摘要翻译: 本发明部分提供式I化合物及其药学上可接受的盐和其N-氧化物; 制备过程和中间体; 及其组合物和用途。 本发明还提供了具有降低的D1R脱敏作用的D1激动剂,相对于多巴胺,D1激动剂降低的D1激动剂,与Ser188相当显着的D1激动剂,但当与D1R D1结合时,与D1R的Ser202没有显着差异 激动剂与Asp103相互作用较弱,与D1R的Ser198相互作用较弱,与D1R的结合及其用途。
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