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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

US20130345439A1 Novel 1-Aryl-3-Azabicyclo[3.1.0]Hexanes: Preparation And Use To Treat Neuropsychiatric Disorders 有权
公开(公告)号：US20130345439A1
公开(公告)日：2013-12-26
申请号：US13887367
申请日：2013-05-05
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： C07D209/52
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.

4. 发明授权

US08461196B2 1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders 有权
公开(公告)号：US08461196B2
公开(公告)日：2013-06-11
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 , C07D209/02
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.

5. 发明申请

US20080234354A1 Methods And Compositions For Controlling Body Weight And Appetite 审中-公开
标题翻译：用于控制体重和食欲的方法和组合
公开(公告)号：US20080234354A1
公开(公告)日：2008-09-25
申请号：US11943552
申请日：2007-11-20
申请人： Arnold S. LIPPA , Joseph W. Epstein , Joseph T. Tizzano , Anthony Basile
发明人： Arnold S. LIPPA , Joseph W. Epstein , Joseph T. Tizzano , Anthony Basile
IPC分类号： A61K31/403 , A61P3/04 , A61P3/10
CPC分类号： A61K31/40 , A61K31/403 , A61K45/06 , C07D209/52 , A61K2300/00
摘要： The present invention provides novel compositions and methods for the controlling appetite and weight and/or treating obesity using a (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or related compound. The invention also provides novel compositions and methods for treating or preventing disorders related to or complicated by excessive body weight or obesity, including coronary heart disease, osteoarthritis, osteoporosis, dislipidemias, gout, atherosclerosis, joint pain, sexual and fertility problems, respiratory problems, gall bladder disease, skin conditions, hypertension, diabetes, stroke, pulmonary embolism, sleep apnea, idiopathic intracranial hypertension, lower extremity venous stasis disease, gastro-esophageal reflux, urinary stress incontinence, metabolic syndrome, insulin resistance and cancer. The methods and compositions of the invention may employ a (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or related compound alone, or in combination with a second anti-appetite or anti-obesity agent.
摘要翻译：本发明提供了使用（+）-1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷或相关化合物来控制食欲和体重和/或治疗肥胖症的新型组合物和方法。本发明还提供了用于治疗或预防与体重过重或肥胖相关或复杂的疾病的新型组合物和方法，包括冠心病，骨关节炎，骨质疏松症，血脂异常，痛风，动脉粥样硬化，关节疼痛，性和生殖问题，呼吸问题，胆囊疾病，皮肤病，高血压，糖尿病，中风，肺栓塞，睡眠呼吸暂停，特发性颅内高压，下肢静脉淤滞疾病，胃食管反流，尿失禁，代谢综合征，胰岛素抵抗和癌症。本发明的方法和组合物可以单独使用（+）-1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷或相关化合物，或与第二抗食欲或抗 - 肥胖剂。

6. 发明授权

US5084457A Benzoylaminoquinazolinones 失效
标题翻译：苯甲酰氨基喹唑啉酮
公开(公告)号：US5084457A
公开(公告)日：1992-01-28
申请号：US556228
申请日：1990-07-23
申请人： William J. Fanshawe , Joseph W. Epstein , Jeremy I. Levin
发明人： William J. Fanshawe , Joseph W. Epstein , Jeremy I. Levin
IPC分类号： C07D239/70 , C07D239/94
CPC分类号： C07D239/70 , C07D239/94
摘要： This invention is compounds of the formula: ##STR1## and a method of treating cognitive and related neuronal behavioral problems in mammals using the compounds.
摘要翻译：本发明是下式的化合物：式I和使用该化合物治疗哺乳动物的认知和相关神经元行为问题的方法。

7. 发明授权

US4977189A Substituted guanidinedicarbonyl derivatives 失效
标题翻译：取代的胍基二羰基衍生物
公开(公告)号：US4977189A
公开(公告)日：1990-12-11
申请号：US217518
申请日：1988-07-11
申请人： Andrew S. Tomcufcik , James S. Dixon , Joseph W. Epstein , Gary H. Birnberg , William J. Fanshawe
发明人： Andrew S. Tomcufcik , James S. Dixon , Joseph W. Epstein , Gary H. Birnberg , William J. Fanshawe
IPC分类号： C07C279/22 , C07C335/38 , C07D333/38
CPC分类号： C07D333/38 , C07C279/22 , C07C335/38 , C07C2101/02 , C07C2101/04 , C07C2101/16 , C07C2103/74
摘要： This disclosure describes novel substituted guanidinedicarbonyl derivatives which possess anxiolytic activity and are also useful as agents for the treatment of cognitive and related neural behavioral problems in mammals.
摘要翻译：本公开内容描述了具有抗焦虑活性的新型取代的胍基二羰基衍生物，并且也可用作治疗哺乳动物的认知和相关神经行为问题的药剂。

8. 发明授权

US4131611A Azabicyclohexanes 失效
标题翻译：氮杂双环己烷
公开(公告)号：US4131611A
公开(公告)日：1978-12-26
申请号：US809339
申请日：1977-06-23
申请人： William J. Fanshawe , Joseph W. Epstein , Lantz S. Crawley , Corris M. Hofmann , Sidney R. Safir
发明人： William J. Fanshawe , Joseph W. Epstein , Lantz S. Crawley , Corris M. Hofmann , Sidney R. Safir
IPC分类号： C07C33/36 , C07D209/52
CPC分类号： C07D209/52 , C07C33/36
摘要： Substituted 3-azabicyclo[3.1.0]hexanes, acid addition salts, method of use and method of preparation are described. The compounds have anxiolytic and analgesic activity.
摘要翻译：描述了取代的3-氮杂双环[3.1.0]己烷，酸加成盐，使用方法和制备方法。该化合物具有抗焦虑和止痛活性。

9. 发明授权

US07098229B2 (+)-1-(3,4-Dichlorophenyl)-3-azabicyclo[3.1.0]hexane, compositions and uses thereof 有权
标题翻译：（+） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷，其组成及用途
公开(公告)号：US07098229B2
公开(公告)日：2006-08-29
申请号：US10466457
申请日：2002-01-11
申请人： Arnold S. Lippa , Joseph W. Epstein
发明人： Arnold S. Lippa , Joseph W. Epstein
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D471/08 , A61K31/403 , A61K31/407 , A61K45/06 , C07D209/52 , A61K2300/00
摘要： The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating of or preventing relapse of depression, anxiety disorders, eating disorders, or urinary incontinence in a patient comprising administering (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or pharmaceutically acceptable salt thereof is preferably substantially free of its corresponding (−)-enantiomer.
摘要翻译：本发明涉及（+） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷及其药学上可接受的盐，其包含（+） - 1-（3,4-二氯苯基） 3-氮杂二环[3.1.0]己烷或其药学上可接受的盐，以及用于治疗或预防患者的抑郁症，焦虑障碍，进食障碍或尿失禁的复发的方法，包括给予（+） - 4-二氯苯基）-3-氮杂双环[3.1.0]己烷或其药学上可接受的盐。（+） - 1-（3,4-二氯苯基）-3-氮杂双环[3.1.0]己烷或其药学上可接受的盐优选基本上不含相应的（ - ） - 对映异构体。

10. 发明授权

US5932585A Method of treating or inhibiting neutropenia 失效
标题翻译：治疗或抑制中性粒细胞减少的方法
公开(公告)号：US5932585A
公开(公告)日：1999-08-03
申请号：US991424
申请日：1997-12-16
申请人： Joseph W. Epstein , Jeremy I. Levin , James J. Gibbons , Judy Lucas
发明人： Joseph W. Epstein , Jeremy I. Levin , James J. Gibbons , Judy Lucas
IPC分类号： A61K31/505 , A61K31/55
CPC分类号： A61K31/505
摘要： The invention is a method of treating or inhibiting neutropenia, or accelerating neutrophil recovery in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each, independently selected from the group consisting of hydrogen, alkyl of 1-6 carbon atoms, optionally substituted benzoyl, ##STR2## or R.sub.1 and R.sub.2 are methylene groups which are taken together to form a 4-7 membered saturated heterocyclic ring;R is hydroxy, 4-morpholinyl, 1H-imidazol-1 -yl, --CH(alkoxy of 1-6 carbon atoms).sub.2, .alpha.-hydroxybenzyl, or optionally substituted phenyl;R.sub.3 is hydrogen or alkyl; R.sub.4 is hydrogen, halogen, alkyl, alkoxy, or trifluoromethyl; R.sub.5 is hydrogen or alkyl; and n=1-3, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明是一种在有需要的哺乳动物中治疗或抑制嗜中性白细胞减少或加速嗜中性粒细胞恢复的方法，其包括向所述哺乳动物施用有效量的具有下式的化合物：其中R1和R2各自独立地选自由氢，1-6个碳原子的烷基，任选取代的苯甲酰基组成，或R1和R2是亚甲基，它们一起形成4-7元饱和杂环; R是羟基，4-吗啉基，1H-咪唑-1-基，-CH（1-6个碳原子的烷氧基）2，α-羟基苄基或任选取代的苯基; R3是氢或烷基; R4是氢，卤素，烷基，烷氧基或三氟甲基; R5是氢或烷基; 和n = 1-3，或其药学上可接受的盐。

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