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1. 发明授权

US5145845A Substituted 2-carboxylindoles having pharmaceutical activity 失效
标题翻译：具有药物活性的取代的2-羧基吲哚
公开(公告)号：US5145845A
公开(公告)日：1992-09-08
申请号：US699875
申请日：1991-05-14
申请人： Graham Johnson , Thomas C. Malone , Po-Wai Yuen
发明人： Graham Johnson , Thomas C. Malone , Po-Wai Yuen
IPC分类号： C07D209/42 , C07D403/04 , C07D403/06
CPC分类号： C07D403/04 , C07D209/42 , C07D403/06
摘要： The present invention relates to novel compounds, which are derivatives of ureas, thioureas, carbamates, sulfonylureas, sulfonamides, amides, and thioamides of 2-carboxyindoles as illustrated by the formula ##STR1## The invention also relates to methods for the preparation of the novel compounds, as well as to pharmaceutical compositions or methods of use for the novel compounds. More specifically, the compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders as well as in the treatment of schizophrenia or epilepsy; and as analgesics and anxiolytics.
摘要翻译：本发明涉及新型化合物，其是如下式所示的2-羧基吲哚的脲，硫脲，氨基甲酸酯，磺酰脲，磺酰胺，酰胺和硫代酰胺的衍生物。本发明还涉及制备该新颖物质的方法化合物，以及用于新化合物的药物组合物或使用方法。更具体地，本发明的化合物可用于治疗神经变性疾病，包括脑血管障碍以及治疗精神分裂症或癫痫; 并作为镇痛药和抗焦虑药。

2. 发明授权

US6124280A Substituted phenols as novel calcium channel blockers 失效
标题翻译：取代酚作为新的钙通道阻滞剂
公开(公告)号：US6124280A
公开(公告)日：2000-09-26
申请号：US983633
申请日：1998-01-23
申请人： Thomas C. Malone , Robert M. Schelkun , Po-Wai Yuen
发明人： Thomas C. Malone , Robert M. Schelkun , Po-Wai Yuen
IPC分类号： C07D295/096 , C07D295/135 , A61K31/55
CPC分类号： C07D295/096 , C07D295/135
摘要： The present invention relates to novel substituted phenols and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also includes.
摘要翻译： PCT No.PCT / US96 / 08064 Sec。 371日期1998年1月23日 102（e）日期1998年1月23日PCT提交1996年7月16日PCT公布。公开号WO97 / 05125 日期：1997年2月13日本发明涉及用于治疗神经障碍的新型取代苯酚及其衍生物。制备化合物的方法，可用于制备的中间体和含有这些化合物的药物组合物还包括。

3. 发明授权

US5284862A Derivatives of 2-carboxyindoles having pharmaceutical activity 失效
标题翻译：具有药物活性的2-羧基吲哚衍生物
公开(公告)号：US5284862A
公开(公告)日：1994-02-08
申请号：US839109
申请日：1992-02-27
申请人： Christopher F. Bigge , Graham Johnson , Po-Wai Yuen
发明人： Christopher F. Bigge , Graham Johnson , Po-Wai Yuen
IPC分类号： C07D209/42 , C07D209/18 , A61K31/38 , A61K31/405 , C07D405/12 , C07D409/12
CPC分类号： C07D209/42
摘要： The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic acids or ester amides, or 2-acylsulfonamides thereof; and including also as 3-substituents unsaturated acids and their further ester and amide derivatives. These 2-carboxyindoles are useful as pharmaceutical agents, therefore, the present invention is also pharmaceutical compositions and pharmaceutical methods of treatment therefor. The compounds of the present invention are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders.
摘要翻译：本发明涉及新的3-取代-2-羧基吲哚; 包括异羟肟酸及其衍生物或脲的3-取代基酰胺和羰基，羧基或膦酸或酯酰胺或其2-酰基磺酰胺; 并且还包括3-取代基不饱和酸及其另外的酯和酰胺衍生物。这些2-羧基吲哚可用作药物，因此，本发明也是药物组合物及其治疗方法。本发明的化合物可用于治疗神经变性疾病，包括脑血管障碍。

4. 发明授权

US07485636B2 Therapeutic pyrazolo[3,4-b]pyridines and indazoles 失效
标题翻译：治疗性吡唑并[3,4-b]吡啶和吲唑
公开(公告)号：US07485636B2
公开(公告)日：2009-02-03
申请号：US11446277
申请日：2006-06-02
申请人： Po-Wai Yuen
发明人： Po-Wai Yuen
IPC分类号： A61K31/535 , C07D413/12
CPC分类号： C07D231/56 , C07D401/04 , C07D403/12 , C07D413/12 , C07D471/04
摘要： The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
摘要翻译：本发明提供式I化合物：其中R2，R3，R4，R5，R6，R7，X和L具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗中枢神经障碍和包括注意力缺陷多动障碍，神经性疼痛，尿失禁，焦虑，抑郁和精神分裂症以及纤维肌痛的病症。还提供了包含一种或多种式I化合物的药物组合物。

5. 发明授权

US06642398B2 Mono-and disubstituted 3-propyl gamma-aminobutyric acids 失效
标题翻译：单取代和二取代的3-丙基γ-氨基丁酸
公开(公告)号：US06642398B2
公开(公告)日：2003-11-04
申请号：US10324929
申请日：2002-12-20
申请人： Thomas Richard Belliotti , Justin Stephen Bryans , Ihoezo Victor Ekhato , Augustine Tobi Osuma , Robert Michael Schelkun , Jacob Bradley Schwarz , Andrew John Thorpe , Lawrence David Wise , David Juergen Wustrow , Po-Wai Yuen
发明人： Thomas Richard Belliotti , Justin Stephen Bryans , Ihoezo Victor Ekhato , Augustine Tobi Osuma , Robert Michael Schelkun , Jacob Bradley Schwarz , Andrew John Thorpe , Lawrence David Wise , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： C07D1000
CPC分类号： C07C229/32 , C07B2200/07 , C07C229/08 , C07C229/20 , C07C229/22 , C07C229/30 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
摘要翻译：本发明是一系列新型的单取代和二取代的3-丙基γ-氨基丁酸，其化合物可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性障碍，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，关节炎，睡眠障碍，IBS和胃损伤。制备化合物和有用的中间体的方法也是本发明的一部分。

6. 发明授权

US6028214A GABA and L-glutamic acid analogs for antiseizure treatment 失效
标题翻译： GABA和L-谷氨酸类似物用于抗发病治疗
公开(公告)号：US6028214A
公开(公告)日：2000-02-22
申请号：US063834
申请日：1998-04-21
申请人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis Martin Sobieray , Lloyd Charles Franklin , Mark Alan Schwindt
发明人： Richard B. Silverman , Ryszard Andruszkiewicz , Po-Wai Yuen , Denis Martin Sobieray , Lloyd Charles Franklin , Mark Alan Schwindt
IPC分类号： A61K31/197 , C07C69/34 , C07C69/675 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07D263/22 , C07D263/26 , G11B20/14 , G11B27/30 , C07C69/66
CPC分类号： A61K31/197 , C07C229/08 , C07C229/24 , C07C229/28 , C07C229/34 , C07C247/12 , C07C309/73 , C07C69/34 , C07C69/675 , C07D263/22 , C07D263/26 , G11B20/1426 , G11B27/3027 , C07C2101/14
摘要： A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are also disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are further disclosed.
摘要翻译：下式化合物其中R 1是具有1至6个碳原子的直链或支链烷基，苯基或具有3至6个碳原子的环烷基; R2是氢或甲基; 并且R 3是氢，甲基或羧基; 其用于治疗癫痫发作。还公开了制备该化合物的方法。进一步公开了在合成化合物期间制备的中间体。

7. 发明授权

US5767129A Substituted quinolines and isoquinolines as calcium channel blockers, their preparation and the use thereof 失效
公开(公告)号：US5767129A
公开(公告)日：1998-06-16
申请号：US698010
申请日：1996-08-13
申请人： Po-Wai Yuen
发明人： Po-Wai Yuen
IPC分类号： C07D217/04 , C07D217/10 , A61K31/47 , C07D215/02 , C07D215/16 , C07D217/22
CPC分类号： C07D217/04 , C07D217/10
摘要： The present invention relates to novel substituted quinolines and isoquinolines and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also included. The compounds are useful in treating pain, cerebral ischemia, and other cerebrovascular disorders.

8. 发明授权

US09458172B2 Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives 有权
标题翻译：吡啶基和嘧啶基亚砜和砜衍生物
公开(公告)号：US09458172B2
公开(公告)日：2016-10-04
申请号：US14382123
申请日：2013-03-01
申请人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
发明人： Kenneth W Bair , Timm R Baumeister , Peter Dragovich , Francis Gosselin , Po-Wai Yuen , Mark Zak , Xiaozhang Zheng
IPC分类号： C07D498/00 , C07D413/00 , C07D487/00 , C07D401/00 , C07D221/02 , C07D471/02 , A61K31/4965 , A61K31/519 , A61K31/44 , A61K31/47 , C07D495/04 , C07D471/04 , C07D491/048 , A61K45/06 , A61K31/455 , A61K31/706 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , C07D487/04
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/706 , A61K45/06 , C07D487/04 , C07D491/048 , C07D495/04 , A61K2300/00
摘要： Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
摘要翻译：公开了某些吡啶基和嘧啶基亚砜和砜化合物，包含这些化合物的药物组合物和使用这些化合物的治疗方法。

9. 发明申请

US20080293715A1 Therapeutic Pyrazolo[3,4-b]Pyridines and Indazoles 审中-公开
标题翻译：治疗性吡唑并[3,4-b]吡啶类和吲唑类
公开(公告)号：US20080293715A1
公开(公告)日：2008-11-27
申请号：US12185419
申请日：2008-08-04
申请人： Robert M. Schelkun , Po-Wai Yuen
发明人： Robert M. Schelkun , Po-Wai Yuen
IPC分类号： A61K31/416 , C07D403/12 , C07D401/12 , C07D413/12 , C07D413/14 , A61K31/5377 , A61K31/454
CPC分类号： C07D231/56 , C07D401/04 , C07D403/12 , C07D413/12 , C07D471/04
摘要： The present invention provides for compounds of Formula I: wherein R2, R3, R4, R5, R6, R7, X, and L have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of central nervous disorders and conditions including attention deficit hyperactivity disorder, neuropathic pain, urinary incontinence, anxiety, depression, and schizophrenia and fibromyalgia. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
摘要翻译：本发明提供式I化合物：其中R2，R3，R4，R5，R6，R7，X和L具有说明书中定义的任何值及其药学上可接受的盐，其可用作治疗中枢神经障碍和包括注意力缺陷多动障碍，神经性疼痛，尿失禁，焦虑，抑郁和精神分裂症以及纤维肌痛的病症。还提供了包含一种或多种式I化合物的药物组合物。

10. 发明授权

US06833385B2 3-heteroarylalkyl substituted GABA analogs 失效
标题翻译： 3-杂芳基烷基取代的GABA类似物
公开(公告)号：US06833385B2
公开(公告)日：2004-12-21
申请号：US10741116
申请日：2003-12-19
申请人： Po-Wai Yuen
发明人： Po-Wai Yuen
IPC分类号： C07D33310
CPC分类号： C07D307/54 , C07D333/24
摘要： The invention is a novel series of compounds which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
摘要翻译：本发明是可用于治疗癫痫，微弱发作，神经退行性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，胃肠道疾病如肠易激综合征（IBS）和炎症，特别是关节炎的新一系列化合物。包括含有本发明化合物的药物组合物以及制备化合物的方法和用于制备最终化合物的新中间体。

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