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公开(公告)号：EP3436010A1
公开(公告)日：2019-02-06
申请号：EP17719380.2
申请日：2017-03-28
发明人： BURSTEIN, Ethan
IPC分类号： A61K31/445 , A61K31/4468 , A61K45/06 , A61K31/00 , G01N33/68 , A61P25/28
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2.发明授权Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases 有权选择性血清素2A / 2C受体反向激动剂作为用于神经变性疾病的治疗剂
公开(公告)号：EP2009000B1
公开(公告)日：2011-06-08
申请号：EP08015449.5
申请日：2004-01-15
发明人： Weiner, M.David , Davis, Robert E. , Brann, Mark R. , Nash, Norman , Andersson, Carl-Magnus A. , Uldam, Allan K.
IPC分类号： C07D211/06 , A61K31/4468 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/06
CPC分类号： A61K31/4468 , A61K9/20 , A61K31/194 , A61K45/06 , C07C59/255 , C07D211/58 , A61K2300/00
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3.发明公开USE OF PIMAVANSERIN IN THE TREATMENT OF PARKINSON AND SYMPTOMS THEREOF 审中-公开pimavanserin的帕金森氏症的IT的治疗，症状的用途
公开(公告)号：EP2173343A1
公开(公告)日：2010-04-14
申请号：EP08769520.1
申请日：2008-05-19
发明人： VANOVER, Kimberly, E. , VAN KAMMEN, Daniel, P. , TOLF, Bo-ragnar , SCHLIENGER, Nathalie , WILLIAMS, Hilde , DAVIS, Robert, E. , WEINER, David, M. , MAYALL, Eve, Taylor
IPC分类号： A61K31/4468 , A61P25/28 , A61K31/519
CPC分类号： A61K31/4468 , A61K31/519 , A61K2300/00
摘要： It is shown that pimavanserin can be administered with or without food without significant effect on absorption or pharmacokinetics. It is also shown that pimavanserin can be used to treat Parkinson's disease psychosis without significantly worsening motor symptoms.
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4.发明公开AZACYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF SEROTONIN RELATED DISEASES 有权用于疾病治疗的氮杂环化合物与血清素ASSOCIATED
公开(公告)号：EP1787984A3
公开(公告)日：2009-12-02
申请号：EP06026352.2
申请日：2001-03-06
IPC分类号： C07D211/58 , C07D207/14 , C07D409/06 , C07D407/06 , C07D401/06 , C07D487/08 , C07D407/12 , A61K31/454 , A61P25/18
CPC分类号： C07D207/14 , C07D211/58 , C07D401/06 , C07D407/06 , C07D407/12 , C07D409/06 , C07D487/08
摘要： Compound and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound of Formula II is administered to a patient in need of such treatment.
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5.发明授权HIGH THROUGHPUT FUNCTIONAL ASSAY FOR G-PROTEIN COUPLED RECEPTORS USING A RAP-RAS CHIMERIC PROTEIN 有权功能测定HIGH THROUGHPUT用于与嵌合RAP-Ras蛋白的G蛋白偶联受体
公开(公告)号：EP1692165B1
公开(公告)日：2009-01-07
申请号：EP04810260.2
申请日：2004-11-02
发明人： BURSTEIN, Ethan S. , PIU, Fabrice , MA, Jian-Nong , WEISSMAN, Jacques Thomas , WEINER, David, M. , SCULLY, Audra, L. , NASH, Norman , SPALDING, Tracy , CURRIER, Erika
CPC分类号： C07K14/82 , C12N9/16 , C12N15/1086 , G01N33/76
摘要： Disclosed herein are methods for enabling or improving functional assays of G-protein coupled receptors through the use of co-expression of helper genes. In some cases, chimeras linking the regulatory domain of the rap1B protein to the effector region of the ras oncogene are used in conjuction with existing functional assays for cellular proliferation. Furthermore, overexpression of other genes can further augment the enabling properties of ras/rap chimeras.
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6.发明公开Use of N-desmethylclozapine to treat human psychosis 审中-公开Verwendung von N-Desmethylclozapin zur Behandlung menschlicher Psychose
公开(公告)号：EP1994932A1
公开(公告)日：2008-11-26
申请号：EP08016004.7
申请日：2004-01-21
IPC分类号： A61K31/5513 , A61P25/18
CPC分类号： A61K31/5513
摘要： Disclosed herein is a method to treat psychosis. Treatment is carried out by administering a therapeutically effective amount of N-desmethylclozapine to a patient suffering from psychosis.
摘要翻译： 本文公开了治疗精神病的方法。 通过向患有精神病的患者施用治疗有效量的N-去甲基氯氮平来进行治疗。
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7.发明授权SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES 有权选择性血清素2A / 2C受体反相激动剂作为治疗神经退行性疾病
公开(公告)号：EP1587789B1
公开(公告)日：2008-09-03
申请号：EP04702584.6
申请日：2004-01-15
发明人： WEINER, David, M. , DAVIS, Robert, E. , BRANN, Mark, R. , NASH, Norman , ANDERSSON , Carl - Magnus A. , ULDAM , Allan K.
IPC分类号： C07D211/06 , A61K31/4468 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P25/24 , A61P25/06
CPC分类号： A61K31/4468 , A61K9/20 , A61K31/194 , A61K45/06 , C07C59/255 , C07D211/58 , A61K2300/00
摘要： Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
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公开(公告)号：EP1937677A1
公开(公告)日：2008-07-02
申请号：EP06826157.7
申请日：2006-10-17
IPC分类号： C07D419/12 , C07D267/20 , C07D245/06 , C07D225/08 , C07D295/18 , C07D337/14 , C07D281/16 , C07F7/08 , C07D419/04 , C07D417/04 , A61P25/00 , A61K31/5513 , A61K31/554 , A61K31/551
CPC分类号： C07D419/12 , C07D223/20 , C07D225/08 , C07D243/38 , C07D245/06 , C07D267/20 , C07D281/16 , C07D295/192 , C07D337/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D419/04
摘要： Disclosed herein is a compound of Formula (I). Also disclosed herein is a method of modulating the activity of a cannabinoid receptor using a compound of Formula (I). Furthermore, disclosed herein is a method of treating a disease or condition that would be alleviated, improved or prevented by administration of a compound that modulates a cannabinoid receptor comprising identifying a subject in need thereof and administering to said subject a therapeutically effective amount of a compound of Formula (I). Also disclosed herein are pharmaceutical compositions comprising a compound of Formula (I).
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9.发明公开AMINO SUBSTITUTED DIARYL [A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS 有权氨基取代的二芳基[A，D]环庚烯类似物AS毒蕈碱激动剂和方法的精神障碍NEURO于治疗
公开(公告)号：EP1696931A2
公开(公告)日：2006-09-06
申请号：EP04815318.3
申请日：2004-12-21
发明人： EK, Fredrik , OLSSON, Roger , OHLSSON, Jörgen
IPC分类号： A61K31/551 , A61P25/28 , C07D403/04
CPC分类号： C07D413/04
摘要： Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.
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10.发明公开HIGH TROUGHPUT FUNCTIONAL ASSAY FOR G-PROTEIN COUPLED RECEPTORS USING A RAP-RAS CHIMERIC PROTEIN 有权功能测定HIGH THROUGHPUT用于与嵌合RAP-Ras蛋白的G蛋白偶联受体
公开(公告)号：EP1692165A1
公开(公告)日：2006-08-23
申请号：EP04810260.2
申请日：2004-11-02
发明人： BURSTEIN, Ethan S. , PIU, Fabrice , MA, Jian-Nong , Weissman, Jacques Thomas , WEINER, David, M. , SCULLY, Audra, L. , NASH, Norman , SPALDING, Tracy , Currier, Erika
CPC分类号： C07K14/82 , C12N9/16 , C12N15/1086 , G01N33/76
摘要： Disclosed herein are methods for enabling or improving functional assays of G-protein coupled receptors through the use of co-expression of helper genes. In some cases, chimeras linking the regulatory domain of the rap1B protein to the effector region of the ras oncogene are used in conjuction with existing functional assays for cellular proliferation. Furthermore, overexpression of other genes can further augment the enabling properties of ras/rap chimeras.
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