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1. 发明授权

US06864261B2 Therapeutic agents useful for treating pain 有权
标题翻译：用于治疗疼痛的治疗剂
公开(公告)号：US06864261B2
公开(公告)日：2005-03-08
申请号：US10429078
申请日：2003-05-02
申请人： Parviz Gharagozloo , Khondaker Islam , Donald J. Kyle , Qun Sun , Laykea Tafesse , John William Frank Whitehead , Ji Yang , Xiaoming Zhou
发明人： Parviz Gharagozloo , Khondaker Islam , Donald J. Kyle , Qun Sun , Laykea Tafesse , John William Frank Whitehead , Ji Yang , Xiaoming Zhou
IPC分类号： A61P25/00 , A61P29/00 , C07D213/74 , C07D213/80 , C07D213/85 , C07D401/04 , C07D401/14 , C07D405/12 , A61K31/496
CPC分类号： C07D213/74 , C07D213/80 , C07D213/85 , C07D401/04 , C07D401/14 , C07D405/12
摘要： A compound of formula (wherein A, R1, R2, R6, m and n are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Piperazine Compound”); pharmaceutical compositions comprising a Piperazine Compound; and methods for treating pain, urinary incontinence (UI), 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 (ALS), dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia and depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperazine Compound are disclosed.
摘要翻译：式（其中A，R 1，R 2，R 6，m和n在本文中公开）的化合物或其药学上可接受的盐（“哌嗪化合物”）; 包含哌嗪化合物的药物组合物; 和治疗疼痛，尿失禁（UI），成瘾性障碍，帕金森病，帕金森综合征，焦虑症，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，亨廷顿氏舞蹈症，肌萎缩性侧索硬化（ALS），痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍和抑郁症，包括向有需要的动物施用有效量的哌嗪化合物。

2. 发明授权

US07169782B2 Aryl substituted thiazolidinones and the use thereof 有权
标题翻译：芳基取代的噻唑烷酮及其用途
公开(公告)号：US07169782B2
公开(公告)日：2007-01-30
申请号：US10195530
申请日：2002-07-16
申请人： Qun Sun , Donald J. Kyle , Parviz Gharagozloo , Ji Yang
发明人： Qun Sun , Donald J. Kyle , Parviz Gharagozloo , Ji Yang
IPC分类号： C07D277/14 , C07D417/06 , A61K31/426 , A61K31/4439
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/14 , C07D279/06 , C07D417/04 , C07D417/06
摘要： This invention relates aryl substituted thiazolidinones of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein R1 and R2, are defined 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的芳基取代的噻唑烷酮：或其药学上可接受的盐或溶剂合物，其中R 1和R 2 2在本说明书中定义。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。

3. 发明申请

US20110152324A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 有权
标题翻译：治疗药物有用的治疗药物
公开(公告)号：US20110152324A1
公开(公告)日：2011-06-23
申请号：US12706571
申请日：2010-02-16
申请人： Donald J. Kyle , Qun Sun , Laykea Tafesse
发明人： Donald J. Kyle , Qun Sun , Laykea Tafesse
IPC分类号： A61K31/444 , C07D401/14 , C07D211/68 , C07D401/04 , A61P29/00
CPC分类号： C07D211/78 , C07D213/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.
摘要翻译：下式的化合物：其中Ar1，Ar2，V，X，R3，R4和m如本文所公开或其药学上可接受的盐（“环（杂）烯基化合物”）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

4. 发明授权

US07262194B2 Therapeutic agents useful for treating pain 有权
标题翻译：用于治疗疼痛的治疗剂
公开(公告)号：US07262194B2
公开(公告)日：2007-08-28
申请号：US10625708
申请日：2003-07-24
申请人： Donald J. Kyle , Qun Sun
发明人： Donald J. Kyle , Qun Sun
IPC分类号： C07D403/04 , C07D403/14 , A61K31/501
CPC分类号： C07D237/24
摘要： A compound of formula: wherein X is S or O and A, R1-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：式（I）化合物或其药学上可接受的盐（其中X为S或O且A，R 1 -R 4， “哒嗪基哌嗪化合物”），包含哒嗪基哌嗪化合物的组合物，以及在动物中治疗或预防疼痛，UI，溃疡，IBD和IBS的方法，其包括向有需要的动物施用有效量的哒嗪基哌嗪化合物。

5. 发明申请

US20130012541A1 Therapeutic Agents Useful for Treating Pain 有权
标题翻译：用于治疗疼痛的治疗剂
公开(公告)号：US20130012541A1
公开(公告)日：2013-01-10
申请号：US13525950
申请日：2012-06-18
申请人： Donald J. Kyle , Qun Sun , Laykea Tafesse
发明人： Donald J. Kyle , Qun Sun , Laykea Tafesse
IPC分类号： A61K31/444 , A61P25/00 , A61K31/4545 , C07D401/04 , C07D401/14
CPC分类号： C07D211/78 , C07D213/02 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.
摘要翻译：下式化合物：其中Ar1，Ar2，V，X，R3，R4和m如本文所公开或其药学上可接受的盐（环（杂）烯基化合物）; 包含有效量的环（杂）烯基化合物的组合物; 以及用于在动物中治疗或预防例如疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的环（杂）烯基化合物。

6. 发明授权

US08058292B2 Therapeutic agents useful for treating pain 有权
标题翻译：用于治疗疼痛的治疗剂
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。

7. 发明申请

US20100256111A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 有权
标题翻译：治疗药物有用的治疗药物
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。

8. 发明申请

US20100240675A1 THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 有权
标题翻译：治疗药物有用的治疗药物
公开(公告)号：US20100240675A1
公开(公告)日：2010-09-23
申请号：US12715825
申请日：2010-03-02
申请人： Donald J. KYLE , Qun Sun
发明人： Donald J. KYLE , Qun Sun
IPC分类号： A61K31/496 , C07D401/04 , A61P25/04 , A61P13/06 , A61P25/30 , A61P25/16 , A61P25/22 , A61P25/08 , A61P17/04 , A61P25/18 , A61P25/14 , A61P25/06 , A61P25/24 , C12N5/02
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, t, and v 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：其中X为S或O且Ar 2，R 1，R 2，R 3，R 8，n，m，t和v为本文公开的化合物或其药学上可接受的盐（“3-取代的吡啶基化合物”），包含有效量的3-取代的吡啶基化合物的组合物，以及治疗或预防疼痛，尿失禁，溃疡，炎性肠病，肠易激综合征，上瘾性疾病，帕金森病，帕金森综合征，焦虑症，癫痫症，卒中，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，向有需要的动物施用有效量的3-取代的吡啶基化合物。

9. 发明申请

US20080153835A1 Therapeutic agents useful for treating pain 有权
标题翻译：用于治疗疼痛的治疗剂
公开(公告)号：US20080153835A1
公开(公告)日：2008-06-26
申请号：US11899379
申请日：2007-09-04
申请人： Donald J. Kyle , Qun Sun , Laykea Tafesse , Chongwu Zhang , Xiaoming Zhou
发明人： Donald J. Kyle , Qun Sun , Laykea Tafesse , Chongwu Zhang , Xiaoming Zhou
IPC分类号： A61K31/501 , C07D401/04 , A61K31/497 , A61P25/04
CPC分类号： C07D213/74 , C07D213/85 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/06 , C07D333/16
摘要： A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine 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 Cyanoiminopiperazine Compound are disclosed.
摘要翻译：式中的化合物：其中A，Ar，R 3，R 6和m在本文中公开，或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”），包含有效量的氰基亚氨基哌嗪化合物的组合物，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，包括给予一个或多个癫痫发作，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，运动障碍或抑郁症公开了有效量的氰酰亚胺哌嗪化合物的需要动物。

10. 发明授权

US07022714B2 Aryl substituted benzimidazoles and their use as sodium channel blockers 有权
标题翻译：芳基取代的苯并咪唑及其作为钠通道阻断剂的用途
公开(公告)号：US07022714B2
公开(公告)日：2006-04-04
申请号：US10630896
申请日：2003-07-31
申请人： Qun Sun , Xiaoming Zhou , Donald J. Kyle
发明人： Qun Sun , Xiaoming Zhou , Donald J. Kyle
IPC分类号： A61K31/454 , C07D401/06 , C07D401/14
CPC分类号： C07D403/06 , C07D235/08 , C07D235/12
摘要： This invention relates aryl substituted benzimidazoles of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined 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的芳基取代的苯并咪唑或其药学上可接受的盐，前药或溶剂合物，其中R 1，R 2，R 10， >和n在本说明书中定义。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。

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