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1. 发明申请

US20120302619A1 Novel 1-aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders 有权
标题翻译：新型1-芳基-3-氮杂双环[3.1.0]己烷：制备和用于治疗神经精神障碍
公开(公告)号：US20120302619A1
公开(公告)日：2012-11-29
申请号：US13366219
申请日：2012-02-03
申请人： Phil SKOLNICK , Anthony Basile , Zhengming Chen , Joseph W. Epstein
发明人： Phil SKOLNICK , Anthony Basile , Zhengming Chen , Joseph W. Epstein
IPC分类号： A61K31/403 , A61P25/22 , A61P25/24 , C07D209/52 , A61P25/00
CPC分类号： A61K31/403 , C07D209/52
摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
摘要翻译：本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法神经系统（CNS）障碍，包括抑郁和焦虑。

2. 发明申请

US20090233978A1 Novel 1-Aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders 审中-公开
标题翻译：新型1-芳基-3-氮杂双环[3.1.0]己烷：制备和用于治疗神经精神障碍
公开(公告)号：US20090233978A1
公开(公告)日：2009-09-17
申请号：US12334432
申请日：2008-12-12
申请人： Phil Skolnick , Anthony Basile , Zhengming Chen , Joseph W. Epstein
发明人： Phil Skolnick , Anthony Basile , Zhengming Chen , Joseph W. Epstein
IPC分类号： A61K31/40 , C07D209/02 , A61P25/00
CPC分类号： A61K31/403 , C07D209/52
摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
摘要翻译：本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法神经系统（CNS）障碍，包括抑郁和焦虑。

3. 发明申请

US20090069374A1 Novel 1-Heteroaryl-3-Azabicyclo[3.1.0]Hexanes, Methods For Their Preparation And Their Use As Medicaments 审中-公开
标题翻译：新型1-杂芳基-3-氮杂双环[3.1.0]己烷，其制备方法及其作为药物的用途
公开(公告)号：US20090069374A1
公开(公告)日：2009-03-12
申请号：US12135053
申请日：2008-06-06
申请人： Phil Skolnick , Zhengming Chen
发明人： Phil Skolnick , Zhengming Chen
IPC分类号： A61K31/47 , A61K31/403 , A61K31/4439 , A61K31/428
CPC分类号： C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.
摘要翻译：本发明提供新颖的1-杂芳基-3-氮杂双环[3.1.0]己烷，以及制备这些化合物的相关方法和中间体，以及使用这些化合物治疗和/或预防中枢神经系统（CNS）的组合物和方法）疾病，包括但不限于抑郁和焦虑。

4. 发明申请

US20080194696A1 Novel Arylbicyclo[3.1.0]Hexylamines And Methods And Compositions For Their Preparation And Use 审中-公开
公开(公告)号：US20080194696A1
公开(公告)日：2008-08-14
申请号：US11936722
申请日：2007-11-07
申请人： Phil Skolnick , Zhengming Chen , Ji Yang
发明人： Phil Skolnick , Zhengming Chen , Ji Yang
IPC分类号： A61K31/135 , C07C211/41
CPC分类号： C07C211/41 , C07B2200/07 , C07C2602/18
摘要： The invention provides novel arylbicyclo[3.1.0]hexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.

5. 发明申请

US20070082940A1 Novel 1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders 审中-公开
标题翻译：新型1-芳基-3-氮杂双环[3.1.0]己烷：制备和用于治疗神经精神障碍
公开(公告)号：US20070082940A1
公开(公告)日：2007-04-12
申请号：US11493431
申请日：2006-07-25
申请人： Phil Skolnick , Anthony Basile , Zhengming Chen , Joseph Epstein
发明人： Phil Skolnick , Anthony Basile , Zhengming Chen , Joseph Epstein
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , C07D209/52
摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
摘要翻译：本发明提供新的多取代的1-芳基-3-氮杂双环[3.1.0]己烷，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物用于治疗和/或预防中枢的组合物和方法神经系统（CNS）障碍，包括抑郁和焦虑。

6. 发明授权

US5428069A Treating cognition with, aminocyclopropanecarboxylic derivatives 失效
标题翻译：用氨基环丙烷羧酸衍生物治疗认知
公开(公告)号：US5428069A
公开(公告)日：1995-06-27
申请号：US3225
申请日：1993-01-11
申请人： Phil Skolnick , Ramon Trullas , Claudia P. Faiman , Eugenia Viu
发明人： Phil Skolnick , Ramon Trullas , Claudia P. Faiman , Eugenia Viu
IPC分类号： C07D215/48 , A61K31/16 , A61K31/19 , A61K31/195 , A61K31/21 , A61K31/47 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07C229/48 , C07C237/24 , A61K31/215
CPC分类号： A61K31/195 , A61K31/47
摘要： The use of a compound possessing functional antagonist properties at the NMDA receptor complex through a specific action at the associated strychnine-insensitive glycine site to improve cognition in normal humans and to treat cognitive deficits resulting from chronic neuronal degeneration, acute brain injury, hypoxia, or other neurological disorders is provided. The compounds possessing functional antagonist properties comprise 1-aminocyclopropanecarboxylic acid, and its pharmaceutically acceptable esters, salts, and acid addition salts or 7-chlorokynurenic acid, and its pharmaceutically acceptable esters, amides, salts, ethers, and acid addition salts.
摘要翻译：通过在相关的士的宁不敏感甘氨酸位点处的特异性作用在NMDA受体复合物中具有功能性拮抗剂性质的化合物的使用，以改善正常人的认知并治疗由慢性神经元变性，急性脑损伤，缺氧引起的认知缺陷提供其他神经障碍。具有功能性拮抗剂性质的化合物包括1-氨基环丙烷羧酸及其药学上可接受的酯，盐和酸加成盐或7-氯代烟酸，以及其药学上可接受的酯，酰胺，盐，醚和酸加成盐。

7. 发明申请

US20160158197A1 Novel 1-Aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders 有权
公开(公告)号：US20160158197A1
公开(公告)日：2016-06-09
申请号：US14929361
申请日：2015-11-01
申请人： Phil SKOLNICK , Anthony BASILE , Zhengming CHEN , Joseph W. EPSTEIN
发明人： Phil SKOLNICK , Anthony BASILE , Zhengming CHEN , Joseph W. EPSTEIN
IPC分类号： A61K31/403
CPC分类号： A61K31/403 , C07D209/52
摘要： The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

8. 发明申请

US20050245517A1 2-pyridinyl[7-(substituted-pyridin-4-yl) pyrazolo[1,5-a]pyrimidin-3-yl]methanones 审中-公开
标题翻译： 2-吡啶基[7-（取代吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮
公开(公告)号：US20050245517A1
公开(公告)日：2005-11-03
申请号：US11118111
申请日：2005-04-29
申请人： Phil Skolnick , Joseph Epstein
发明人： Phil Skolnick , Joseph Epstein
IPC分类号： A61K31/519 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones with at least one substituent on both the 2- and 4-pyridinyl ring having the chemical structure of formula I: The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula I to modulate GABA and GABAA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and/or GABAA receptors.
摘要翻译：本发明提供了具有至少一个取代基的2-吡啶基[7（吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮，其具有化学式I的结构：本发明还提供了使用式I的新颖2-吡啶基[7-（吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮调节GABA的组合物和方法，以及受体生理学在哺乳动物受试者中引发治疗反应以减轻神经或精神疾病，包括中风，头部创伤，癫痫，疼痛，偏头痛，情绪障碍，焦虑，创伤后应激障碍，强迫症，躁狂症，双相性精神障碍，精神分裂症，惊厥，抽搐，耳鸣，包括阿尔茨海默氏病，肌萎缩性侧索硬化和帕金森病，亨廷顿氏舞蹈病，抑郁症，双相情感障碍，躁狂症，三叉神经痛和其他神经痛，神经性疼痛，高血压，脑部神经退行性疾病局部缺血，心律失常，肌强直，物质滥用，肌阵挛，原发性震颤，运动障碍和其他运动障碍，新生儿脑出血和痉挛状态，以及由GABA和/或GABA介导的其他精神和神经障碍。 SUB>受体。

9. 发明授权

US6017957A Partial agonists of the strychnine insensitive glycine modulatory site of the N-methyl-D-aspartate receptor complex as neuropsychopharmacological agents 失效
标题翻译： N-甲基-D-天冬氨酸受体复合物的士的宁不敏感的甘氨酸调节位点的部分激动剂作为神经精神药理学试剂
公开(公告)号：US6017957A
公开(公告)日：2000-01-25
申请号：US390745
申请日：1989-08-08
申请人： Phil Skolnick , Anita Lewin , Juan-Carlos Marvizon , James Monn , Kenner Rice
发明人： Phil Skolnick , Anita Lewin , Juan-Carlos Marvizon , James Monn , Kenner Rice
IPC分类号： A61K31/195 , A61K31/215 , A61K45/00 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/28
CPC分类号： A61K31/195 , A61K31/215
摘要： A method is disclosed for the treatment of neuropsychopharmacological disorders which are associated with or result from excessive activation of the N-methyl-D-aspartate receptor complex, which method comprises administering an effective neuropsychopharmacological disorder-treating amount of a compound possessing partial agonist properties for the strychnine insensitive glycine modulatory sites of N-methyl-D-aspartate receptors. Exemplary of partial agonists which are useful in the method of the invention are 1-aminocyclopropanecarboxylic acid, and associated derivates thereof. Novel injectable pharmaceutical compositions are also disclosed.
摘要翻译：公开了用于治疗与N-甲基-D-天冬氨酸受体复合物的过量活化相关或由其引起的神经精神药理学障碍的方法，该方法包括给予有效的神经精神药理学障碍治疗量的具有部分激动剂性质的化合物 N-甲基-D-天冬氨酸受体的士的宁不敏感的甘氨酸调节位点。可用于本发明方法的部分激动剂的实例是1-氨基环丙烷羧酸及其相关衍生物。还公开了新的可注射药物组合物。

10. 发明授权

US5280015A 2-substituted adenosines and 2-substituted adenosine 5'-carboxamides 失效
标题翻译： 2-取代腺苷和2-取代腺苷5'-羧酰胺
公开(公告)号：US5280015A
公开(公告)日：1994-01-18
申请号：US577528
申请日：1990-09-05
申请人： Kenneth A. Jacobson , R. Tyler McCabe , Phil Skolnick
发明人： Kenneth A. Jacobson , R. Tyler McCabe , Phil Skolnick
IPC分类号： C07H19/16 , A61K31/70 , C07H19/167
CPC分类号： A61K31/70 , C07H19/16
摘要： The present invention is directed to compounds useful as probes for characterizing and studying the adenosine A.sub.2 receptor. The present invention is also directed to methods of treating central nervous system disorders and cardiovascular disorders which include treating hypertension and thrombosis by administering said compounds.
摘要翻译：本发明涉及可用作表征和研究腺苷A2受体的探针的化合物。本发明还涉及治疗中枢神经系统疾病和心血管疾病的方法，其包括通过施用所述化合物治疗高血压和血栓形成。

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