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公开(公告)号：US08551998B2
公开(公告)日：2013-10-08
申请号：US13439948
申请日：2012-04-05
申请人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, Jr. , William Pendergast , Shy-Tai Jan
发明人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, Jr. , William Pendergast , Shy-Tai Jan
IPC分类号： A61K31/497
CPC分类号： C07D241/04 , A61K31/00 , A61K31/445 , A61K31/495 , A61K31/519 , A61K38/33 , A61K2300/00
摘要： Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.
摘要翻译： 用于治疗性功能障碍的组合物和方法，其通过向受试者施用包含δ阿片受体激动剂的药物组合物，所述药物组合物有效地延迟性刺激期间受试者的射精发作。
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公开(公告)号：US08575169B2
公开(公告)日：2013-11-05
申请号：US10335764
申请日：2003-01-02
申请人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, Jr. , William Pendergast , Shyi-Tai Jan
发明人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, Jr. , William Pendergast , Shyi-Tai Jan
IPC分类号： A61K31/497
CPC分类号： C07D241/04 , A61K31/00 , A61K31/445 , A61K31/495 , A61K31/519 , A61K38/33 , A61K2300/00
摘要： Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.
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公开(公告)号：US20130053326A9
公开(公告)日：2013-02-28
申请号：US10335764
申请日：2003-01-02
申请人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, JR. , William Pendergast , Shyi-Tai Jan
发明人： Kwen-Jen Chang , Klim King , Kestutis P. Biciunas , Robert W. McNutt, JR. , William Pendergast , Shyi-Tai Jan
IPC分类号： A61K38/33 , A61K31/519
CPC分类号： C07D241/04 , A61K31/00 , A61K31/445 , A61K31/495 , A61K31/519 , A61K38/33 , A61K2300/00
摘要： Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.
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4.发明授权Compositions and methods for combating lower urinary tract dysfunctions with delta opioid receptor agonists 有权用Δ阿片受体激动剂对抗下尿路功能障碍的组合物和方法公开(公告)号：US08476280B2
公开(公告)日：2013-07-02
申请号：US10434004
申请日：2003-05-08
申请人： Kwen-Jen Chang , Peter J. Gengo , Kestutis P. Biciunas , Xin Ma , William Pendergast , Shyi-Tai Jan
发明人： Kwen-Jen Chang , Peter J. Gengo , Kestutis P. Biciunas , Xin Ma , William Pendergast , Shyi-Tai Jan
IPC分类号： A61K31/4965 , A61K31/497
CPC分类号： A61K31/496 , A61K31/495 , A61K45/06
摘要： Compositions and methods for treatment of a urinary tract dysfunction by administering to a subject in need of such treatment a pharmaceutical composition including a delta opioid receptor agonist in an amount effective to reduce the effects of the urinary tract dysfunction. The compositions may further include an additional active agent that is used to treat urinary tract dysfunctions, e.g., alpha-adrenergic agonists, anticholinergics, alpha-adrenergic antagonists and tricyclic antidepressants.
摘要翻译： 用于治疗尿道功能障碍的组合物和方法，其通过向需要这种治疗的受试者施用包含δ阿片受体激动剂的药物组合物，其量有效降低尿路功能障碍的作用。 组合物还可以包括用于治疗尿道功能障碍的另外的活性剂，例如α-肾上腺素能激动剂，抗胆碱能药，α-肾上腺素能拮抗剂和三环抗抑郁药。
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公开(公告)号：US20070173515A1
公开(公告)日：2007-07-26
申请号：US11696806
申请日：2007-04-05
申请人： Kwen-Jen Chang , Klim King , Kestutis Biciunas , Robert McNutt , William Pendergast , Shyi-Tai Jan
发明人： Kwen-Jen Chang , Klim King , Kestutis Biciunas , Robert McNutt , William Pendergast , Shyi-Tai Jan
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D241/04 , A61K31/00 , A61K31/445 , A61K31/495 , A61K31/519 , A61K38/33 , A61K2300/00
摘要： Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.
摘要翻译： 用于治疗性功能障碍的组合物和方法，其通过向受试者施用包含δ阿片受体激动剂的药物组合物，所述药物组合物有效地延迟性刺激期间受试者的射精发作。
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公开(公告)号：US07683168B2
公开(公告)日：2010-03-23
申请号：US11404632
申请日：2006-04-14
申请人： Shyi-Tai Jan , Kwen-Jen Chang , Kestutis P. Biciunas , Xin Ma
发明人： Shyi-Tai Jan , Kwen-Jen Chang , Kestutis P. Biciunas , Xin Ma
IPC分类号： C07D245/02
CPC分类号： C07D405/12 , C07D241/04 , C07D401/10 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D491/10
摘要： Diarylmethylpiperazine compounds are described, which are useful as mu and/or delta receptor opioid compounds, without central side effects. Pharmaceutical compositions containing such compounds are variously useful for peripheral or non-centrally mediated indications, including peripherally mediated and neuropathic pain, urogenital tract disorders, overactive bladder, urinary incontinence, sexual disorders, premature ejaculation, cough, lung edema, cardiac disorders, cardioprotection, gastro-intestinal disorders, diarrhea, irritable bowl syndrome, functional distention, immuno-modulation and anti-tumor activity.
摘要翻译： 描述了二芳基甲基哌嗪化合物，其可用作mu和/或δ受体阿片样物质，没有中枢副作用。 包含这些化合物的药物组合物可用于外周或非中枢介导的适应症，包括周围介导的和神经性疼痛，泌尿生殖道疾病，膀胱过度活动症，尿失禁，性功能障碍，早泄，咳嗽，肺水肿，心脏病，心脏保护， 胃肠道疾病，腹泻，肠易激综合征，功能扩张，免疫调节和抗肿瘤活性。
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公开(公告)号：US06919350B2
公开(公告)日：2005-07-19
申请号：US09974004
申请日：2001-10-09
IPC分类号： A61K45/00 , A61K9/70 , A61K31/00 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/55 , A61K45/06 , A61P11/00 , A61P11/16 , A61P43/00 , C07D295/096 , C07D295/155 , A61K31/44 , A61K31/4965 , A61K38/00
CPC分类号： A61K31/495 , A61K31/00 , A61K31/40 , A61K31/445 , A61K31/485 , A61K31/496 , A61K31/55 , A61K45/06 , C07D295/096 , C07D295/155 , A61K2300/00
摘要： A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.
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公开(公告)号：US5552404A
公开(公告)日：1996-09-03
申请号：US431377
申请日：1995-04-28
IPC分类号： C07D295/14 , A61K31/495 , A61P1/00 , A61P11/00 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P25/30 , A61P43/00 , C07D213/75 , C07D295/155 , A61K31/445
CPC分类号： C07D213/75 , C07D295/155 , C07C2101/02
摘要： Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.
摘要翻译： 公开了作为用于与诸如δ，mu，σ和/或kappa受体的受体结合的外源受体组合物质的二芳基甲基哌嗪化合物。 本发明的化合物可用作激动剂/拮抗剂对中的缀合物用于传导监测和神经递质功能的测定，并且还各种表现出治疗效用，包括介导镇痛，并具有用于治疗腹泻，尿失禁，精神疾病，药物 酒精成瘾/过量，肺水肿，抑郁症，哮喘，肺气肿，咳嗽和呼吸暂停，呼吸抑制，认知障碍，呕吐和胃肠道疾病。
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公开(公告)号：US5574159A
公开(公告)日：1996-11-12
申请号：US430677
申请日：1995-04-28
IPC分类号： C07D211/70 , C07D213/38 , C07D213/75 , C07D213/82 , C07D277/28 , C07D295/02 , C07D295/03 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/192 , C07D333/20 , C07D333/28 , C07D333/38 , C07K5/06 , C07K5/065 , C07D403/10
CPC分类号： C07D213/75 , C07D211/70 , C07D213/38 , C07D213/82 , C07D277/28 , C07D295/03 , C07D295/096 , C07D295/135 , C07D295/155 , C07D295/192 , C07D333/20 , C07D333/28 , C07D333/38 , C07K5/06026 , C07K5/06078 , C07C2101/02
摘要： Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.
摘要翻译： 公开了作为用于与诸如δ，mu，σ和/或kappa受体的受体结合的外源受体组合物质的二芳基甲基哌嗪化合物。 本发明的化合物可用作激动剂/拮抗剂对中的缀合物用于传导监测和神经递质功能的测定，并且还各种表现出治疗效用，包括介导镇痛，并具有用于治疗腹泻，尿失禁，精神疾病，药物 酒精成瘾/过量，肺水肿，抑郁症，哮喘，肺气肿，咳嗽和呼吸暂停，呼吸抑制，认知障碍，呕吐和胃肠道疾病。
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公开(公告)号：US5807858A
公开(公告)日：1998-09-15
申请号：US658726
申请日：1996-06-05
IPC分类号： A61K31/00 , A61K31/495 , A61K31/496 , C07D295/096 , C07D295/155 , C07D241/04
CPC分类号： C07D295/096 , A61K31/00 , A61K31/495 , A61K31/496 , C07D295/155
摘要： The present invention relates to, inter alia, methods and compositions for reducing, treating or preventing respiratory depression in an animal, using a compound of the formula: ##STR1## wherein: Ar, G, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in specification, or a pharmaceutically acceptable ester or salt thereof.
摘要翻译： 本发明特别涉及用下列化合物降低，治疗或预防动物呼吸抑制的方法和组合物：其中：Ar，G，Z，R 2，R 3，R 4 ，R5，R6和R7如说明书中所定义，或其药学上可接受的酯或其盐。
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