公开(公告)号：US20100210686A1

公开(公告)日：2010-08-19

申请号：US12506040

申请日：2009-07-20

申请人： Qun Sun ,  Kate Xin Wen ,  Xiaoming Zhou

发明人： Qun Sun ,  Kate Xin Wen ,  Xiaoming Zhou

IPC分类号： A61K31/4545 ,  C07D401/04 ,  C07D417/14 ,  A61P29/00 ,  C12N5/07

CPC分类号： C07D417/14 ,  C07D401/04

摘要： Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.

摘要翻译： 哌啶化合物; 包含哌啶化合物的组合物; 以及用于治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，受限制 脑功能，亨廷顿舞蹈病，肌萎缩性侧索硬化，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的哌啶化合物。 在一个实施方案中，哌啶化合物具有下式：及其药学上可接受的盐，其中Ar1，Ar2，X，R3，R4和m如本文所公开。

公开(公告)号：US07737148B2

公开(公告)日：2010-06-15

申请号：US11601792

申请日：2006-11-16

申请人： Qun Sun ,  Xiaoming Zhou

发明人： Qun Sun ,  Xiaoming Zhou

IPC分类号： A61K31/44 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61P19/02 ,  A61P25/02 ,  A61P29/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04

摘要： A compound of formula: wherein Ar, Ar1, Ar2, R3-R6, R13, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopiperazine Compound”); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.

摘要翻译： 式中的化合物：其中Ar，Ar1，Ar2，R3-R6，R13，m和t在本文中公开，或其药学上可接受的盐（“羟基亚氨基哌嗪化合物”）; 包含有效量的羟基亚氨基哌嗪化合物的组合物; 以及用于治疗或预防动物中的疼痛和其它病症的方法，包括向有需要的动物施用有效量的羟基亚氨基哌嗪化合物。

公开(公告)号：US07572812B2

公开(公告)日：2009-08-11

申请号：US11337271

申请日：2006-01-20

申请人： Qun Sun ,  Kate Xin Wen ,  Xiaoming Zhou

发明人： Qun Sun ,  Kate Xin Wen ,  Xiaoming Zhou

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  A61K31/444

CPC分类号： C07D417/14 ,  C07D401/04

摘要： Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.

摘要翻译： 哌啶化合物; 包含哌啶化合物的组合物; 以及用于治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，受限制 脑功能，亨廷顿舞蹈病，肌萎缩性侧索硬化，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的哌啶化合物。 在一个实施方案中，哌啶化合物具有下式：及其药学上可接受的盐，其中Ar1，Ar2，X，R3，R4和m如本文所公开。

公开(公告)号：US20090042902A1

公开(公告)日：2009-02-12

申请号：US12240688

申请日：2008-09-29

申请人： Qun Sun ,  Xiaoming Zhou

发明人： Qun Sun ,  Xiaoming Zhou

IPC分类号： A61K31/496 ,  A61P25/00 ,  C07D417/04 ,  C07D401/04

CPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04

摘要： A compound of formula: wherein Ar, Ar1, Ar2, R3, R4, R5, R6, R13, m, t, and x are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Hydroxyiminopiperazine Compound”); compositions comprising an effective amount of a Hydroxyiminopiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Hydroxyiminopiperazine Compound are disclosed.

摘要翻译： 式中的化合物：其中Ar，Ar1，Ar2，R3，R4，R5，R6，R13，m，t和x在本文中公开，或其药学上可接受的盐（“羟基亚氨基哌嗪化合物”）; 包含有效量的羟基亚氨基哌嗪化合物的组合物; 以及用于治疗或预防动物中的疼痛和其它病症的方法，包括向有需要的动物施用有效量的羟基亚氨基哌嗪化合物。

公开(公告)号：US20060199824A1

公开(公告)日：2006-09-07

申请号：US11337271

申请日：2006-01-20

申请人： Qun Sun ,  Kate Wen ,  Xiaoming Zhou

发明人： Qun Sun ,  Kate Wen ,  Xiaoming Zhou

IPC分类号： A61K31/506 ,  A61K31/497 ,  A61K31/501 ,  A61K31/4545 ,  A61K31/454 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D417/14 ,  C07D401/04

摘要： Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.

摘要翻译： 哌啶化合物; 包含哌啶化合物的组合物; 以及用于治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，受限制 脑功能，亨廷顿舞蹈病，肌萎缩性侧索硬化，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的哌啶化合物。 在一个实施方案中，哌啶化合物具有下式：及其药学上可接受的盐，其中Ar 1，Ar 2，X，R 3， R 4，且m如本文所公开。

公开(公告)号：US10118927B2

公开(公告)日：2018-11-06

申请号：US14655882

申请日：2013-12-23

申请人： SHIONOGI & CO., LTD. ,  Kevin Brown ,  Dawit Tadesse ,  Naoki Tsuno ,  Nobuyuki Tanaka ,  Xiaoming Zhou

发明人： Kevin Brown ,  Dawit Tadesse ,  Nobuyuki Tanaka ,  Naoki Tsuno ,  Xiaoming Zhou

IPC分类号： C07D471/08 ,  C07D211/58 ,  C07C235/74

摘要： The disclosure relates to Substituted Piperidin-4-amino-Type Compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, Q1, Q2, E1, E2, A, B, D, W, Z, a, b, n, and x are as defined herein, compositions comprising an effective amount of a Substituted Piperidin-4-amino-Type Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Piperidin-4-amino-Type Compound.

公开(公告)号：US20130216985A1

公开(公告)日：2013-08-22

申请号：US13704922

申请日：2011-06-22

申请人： Etienne de Villers-Sidani ,  Xiaoming Zhou ,  Jyoti Mishra-Ramanathan ,  Michael Merzenich

发明人： Etienne de Villers-Sidani ,  Xiaoming Zhou ,  Jyoti Mishra-Ramanathan ,  Michael Merzenich

IPC分类号： G09B19/00

CPC分类号： G09B19/00 ,  A61B5/04842 ,  A61B5/16 ,  G06F19/3481 ,  Y02A90/26

摘要： The present disclosure relates to methods and tools for enhancing cognition in an individual. The methods involve presenting to the individual multiple sets of stimuli. Each set of the multiple set contains two or more stimuli and at least one set of the multiple sets contains a target stimulus. The method then receives an input from the individual, and informs the individual as to whether the input is a correct response. The methods encompass iterations of stimuli presentation, receiving of the input, and lastly, generation of feedback to the individual until the individual learns and retains what the target stimulus is.

摘要翻译： 本公开涉及用于增强个体认知的方法和工具。 该方法涉及呈现给个体多组刺激。 每组多组包含两个或更多个刺激，并且至少一组多组包含目标刺激。 然后，该方法从个人接收输入，并且通知个人输入是否是正确的响应。 这些方法包括刺激表现的迭代，输入的接收以及最后的反馈的产生，直到个体学习并保留目标刺激为止。

公开(公告)号：US08058292B2

公开(公告)日：2011-11-15

申请号：US12786043

申请日：2010-05-24

申请人： Donald J. Kyle ,  Qun Sun ,  Xiaoming Zhou

发明人： Donald J. Kyle ,  Qun Sun ,  Xiaoming Zhou

IPC分类号： A61K31/4427 ,  C07D401/04 ,  C07D401/12

CPC分类号： C07D401/04 ,  C07D401/12

摘要： The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.

摘要翻译： 本发明提供式（I）化合物：其中R 1，Q，A和R 2在本文中公开）或其药学上可接受的盐（“吡啶 - 炔基化合物”）; 包含有效量的吡啶 - 炔基化合物的药物组合物; 以及用于治疗或预防诸如疼痛，尿失禁，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，癫痫发作，中风，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能 亨廷顿舞蹈病，肌萎缩性侧索硬化症，痴呆症，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的吡啶 - 炔基化合物。

公开(公告)号：US20100256111A1

公开(公告)日：2010-10-07

申请号：US12786043

申请日：2010-05-24

申请人： Donald J. Kyle ,  Qun Sun ,  Xiaoming Zhou

发明人： Donald J. Kyle ,  Qun Sun ,  Xiaoming Zhou

IPC分类号： A61K31/4427 ,  C07D211/98 ,  C07D211/94 ,  A61K31/4545 ,  C07D401/12 ,  A61P13/00 ,  A61P21/00 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D401/04 ,  C07D401/12

摘要： The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.

摘要翻译： 本发明提供式（I）化合物：其中R 1，Q，A和R 2在本文中公开）或其药学上可接受的盐（“吡啶 - 炔基化合物”）; 包含有效量的吡啶 - 炔基化合物的药物组合物; 以及用于治疗或预防诸如疼痛，尿失禁，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，癫痫发作，中风，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能 亨廷顿舞蹈病，肌萎缩性侧索硬化症，痴呆症，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的吡啶 - 炔基化合物。

公开(公告)号：US20100234426A1

公开(公告)日：2010-09-16

申请号：US12447758

申请日：2007-10-31

申请人： Xiaoming Zhou

发明人： Xiaoming Zhou

IPC分类号： A61K31/4468 ,  C07D211/58 ,  C07D401/06 ,  A61K31/454 ,  A61P1/08 ,  A61P1/12 ,  A61P25/08 ,  A61P25/06 ,  A61P29/00 ,  A61P25/04

CPC分类号： C07D211/58 ,  A61K31/4468 ,  A61K31/58 ,  A61K45/06 ,  C07D401/06 ,  A61K2300/00

摘要： The invention relates to phenylpropionamide compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A, B, R1, R2, R3, R4 and R5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the activation of opioid receptors, particularly μ-opioid receptors. Compounds of the present invention are especially useful for treating pain.

摘要翻译： 本发明涉及式（I）的苯基丙酰胺化合物及其药学上可接受的盐，前药和溶剂化物，其中A，B，R 1，R 2，R 3，R 4和R 5如说明书所述定义。 本发明还涉及式（I）化合物用于治疗，预防或改善对阿片受体，特别是μ-阿片样物质受体的活化有反应的病症。 本发明的化合物特别适用于治疗疼痛。