公开(公告)号：US08178560B2

公开(公告)日：2012-05-15

申请号：US12817773

申请日：2010-06-17

申请人： Qun Sun ,  Xin Wen

发明人： Qun Sun ,  Xin Wen

IPC分类号： A61K31/44 ,  A01N43/40 ,  C07D401/00 ,  C07D417/00

CPC分类号： A61K31/444 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

摘要： A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl 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 Cycloheteroalkenyl Compound are disclosed herein.

摘要翻译： 式中的化合物：其中Ar1，Ar2，X，R3和m如本文所公开或其药学上可接受的盐（“环烯基烯基化合物”）; 包含有效量的环烯基烯基化合物的组合物; 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环烯基烯基化合物。

公开(公告)号：US08129388B2

公开(公告)日：2012-03-06

申请号：US13158267

申请日：2011-06-10

申请人： Qun Sun

发明人： Qun Sun

IPC分类号： C07D403/12 ,  A61K31/497

CPC分类号： C07D417/12 ,  C07D213/56

摘要： The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.

摘要翻译： 本发明公开了下式的化合物：其中Ar1，Ar2，X，R3和m如本文所公开或其药学上可接受的盐（“亚苯基化合物”）; 包含有效量的苯亚甲基化合物的组合物; 以及用于治疗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苯撑化合物。

公开(公告)号：US20110245357A1

公开(公告)日：2011-10-06

申请号：US13160586

申请日：2011-06-15

申请人： Qun Sun

发明人： Qun Sun

IPC分类号： C08K5/1535

CPC分类号： C08J5/20 ,  C08J3/095 ,  H01M4/8668 ,  H01M8/1023 ,  H01M8/1039 ,  H01M8/1081 ,  H01M2300/0082 ,  Y02P70/56

摘要： Highly fluorinated ion-exchange polymers achieve dissolution in aqueous tetrahydrofuran at lower pressures and temperatures than in other solvents, with few or no side products being formed.

摘要翻译： 高度氟化的离子交换聚合物在比其他溶剂更低的压力和温度下实现在四氢呋喃水溶液中溶解，几乎没有或没有形成副产物。

公开(公告)号：US08008300B2

公开(公告)日：2011-08-30

申请号：US12499480

申请日：2009-07-08

申请人： Qun Sun ,  Laykea Tafesse ,  Sam Victory

发明人： Qun Sun ,  Laykea Tafesse ,  Sam Victory

IPC分类号： A61K31/50 ,  A61K31/497 ,  C07D403/04 ,  C07D241/02

CPC分类号： C07D417/12 ,  A61K31/495 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine 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 Benzoazolylpiperazine Compound are disclosed.

摘要翻译： 下式的化合物：其中Ar1，A，R3，x和m如本文所公开，Ar 2是苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并恶唑基哌嗪化合物”），包含苯并恶唑基哌嗪化合物 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， 限制性脑功能，亨廷顿氏舞蹈病，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，其中包括向有需要的动物施用有效量的苯并恶唑基哌嗪化合物。

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：US07696208B2

公开(公告)日：2010-04-13

申请号：US11344937

申请日：2006-01-31

申请人： Donald J. Kyle ,  Qun Sun

发明人： Donald J. Kyle ,  Qun Sun

IPC分类号： C07D213/75 ,  A61K31/44 ,  A61K31/496

CPC分类号： C07D401/04 ,  C07D213/74 ,  C07D213/85

摘要： Compounds of formulae: where X is S or O and Ar2, R1, R2, R3, R8, n, m, and t are disclosed herein, or a pharmaceutically acceptable salt thereof (a “3-substituted Pyridyl Compound”), compositions comprising an effective amount of a 3-substituted Pyridyl Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, 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 3-substituted Pyridyl Compound are disclosed herein.

摘要翻译： 式中的化合物：其中X为S或O且Ar 2，R 1，R 2，R 3，R 8，n，m和t在本文中公开，或其药学上可接受的盐（“3-取代的吡啶基化合物”）， 有效量的3-取代的吡啶基化合物，以及治疗或预防疼痛，尿失禁，溃疡，炎性肠病，肠易激综合征，成瘾性疾病，帕金森病，帕金森综合征，焦虑症，癫痫，中风， 包括施用于癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷，限制性脑功能，亨廷顿氏舞蹈病，肌萎缩性侧索硬化症，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症 有需要的动物本文公开了有效量的3-取代的吡啶基化合物。

公开(公告)号：US07696207B2

公开(公告)日：2010-04-13

申请号：US11893916

申请日：2007-08-17

申请人： Donald J. Kyle ,  Qun Sun

发明人： Donald J. Kyle ,  Qun Sun

IPC分类号： C07D403/04 ,  C07D403/14

CPC分类号： C07D237/24

摘要： A compound of formula: wherein X is S or O and A, R1, R2, R3, R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.

摘要翻译： 下式的化合物：其中X为S或O且A，R 1，R 2，R 3，R 4，n和m在本文中公开，或其药学上可接受的盐（“哒嗪基哌嗪化合物”），包含哒嗪基哌嗪化合物， 以及用于在动物中治疗或预防疼痛，UI，溃疡，IBD和IBS的方法，包括向有需要的动物施用有效量的哒嗪基哌嗪化合物。

公开(公告)号：US20100048626A1

公开(公告)日：2010-02-25

申请号：US12546572

申请日：2009-08-24

申请人： Bin SHAO ,  R. Richard Goehring ,  Samuel F. Victory ,  Qun Sun

发明人： Bin SHAO ,  R. Richard Goehring ,  Samuel F. Victory ,  Qun Sun

IPC分类号： A61K31/4545 ,  C07D401/12 ,  C07D213/56 ,  A61K31/4418 ,  A61P25/00 ,  G01N33/00

CPC分类号： C07D213/81 ,  C07D213/82 ,  Y10T436/145555

摘要： This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

摘要翻译： 本发明涉及式I的芳基取代的吡啶：或其药学上可接受的盐，前药或溶剂化物，其中Ar和R 1 -R 4被置于说明书中。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

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。