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1. 发明申请

WO2007120648A2 MONO AND DI-SUBSTITUTED OXYCODONE COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：单和二取代的氧化钴化合物和组合物
公开(公告)号：WO2007120648A2
公开(公告)日：2007-10-25
申请号：PCT/US2007/008821
申请日：2007-04-10
申请人： NEW RIVER PHARMACEUTICALS INC. , MICKLE, Travis , KRISHNAN, Suma , MONCRIEF, James Scott , LAUDERBACK, Christopher , BERA, Sanjib
发明人： MICKLE, Travis , KRISHNAN, Suma , MONCRIEF, James Scott , LAUDERBACK, Christopher , BERA, Sanjib
IPC分类号： A61K38/04
CPC分类号： A61K9/0043 , A61K9/0019 , A61K47/55 , A61K47/64
摘要： The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to oxycodone in a manner that substantially decreases the potential for overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of oxycodone and may also provide sustained release characteristics and/or reduced side-effects. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction of oxycodone.
摘要翻译：本发明涉及药物化合物和组合物，其包含以足够大的降低过量潜力的方式与羟考酮连接的化学部分。当以适当剂量递送时，药物组合物提供类似于羟考酮的治疗活性，并且还可以提供持续释放特征和/或减少的副作用。此外，本发明的化合物和组合物可用于预防成瘾和对羟考酮成瘾的易感性。

2. 发明申请

WO2007126832A3 PHARMACEUTICAL COMPOSITIONS FOR PREVENTION OF OVERDOSE OR ABUSE 审中-公开
标题翻译：用于防止过度或不适用的药物组合物
公开(公告)号：WO2007126832A3
公开(公告)日：2008-10-16
申请号：PCT/US2007007594
申请日：2007-03-29
申请人： SHIRE LLC , MICKLE TRAVIS , KRISHNAN SUMA , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , PICCARIELLO THOMAS , MILLER CHRISTAL
发明人： MICKLE TRAVIS , KRISHNAN SUMA , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , PICCARIELLO THOMAS , MILLER CHRISTAL
IPC分类号： A61K38/00
CPC分类号： A61K31/485 , A61K9/0019 , A61K9/0043 , A61K47/542 , A61K47/64
摘要： The invention relates to pharmaceutical compositions comprised of a chemical moiety attached to an active agent in a manner that substantially decreases the potential of the active agent to cause overdose or to be abused. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.
摘要翻译：本发明涉及药物组合物，其包含以活性剂附着于活性剂的化学部分，其基本上降低了活性剂引起过量或被滥用的潜力。当以适当剂量递送时，药物组合物提供与母体活性剂类似的治疗活性。

3. 发明申请

WO2005000334A1 ABUSE RESISTANT AMPHETAMINE COMPOUNDS 审中-公开
标题翻译：耐药AMPHATAMINE化合物
公开(公告)号：WO2005000334A1
公开(公告)日：2005-01-06
申请号：PCT/US2004/017204
申请日：2004-06-01
申请人： NEW RIVER PHARMACEUTICALS, INC. , MICKLE, Travis , KRISHNAN, Suma , BISHOP, Barney , LAUDERBACK, Christopher , MONCRIEF, James, Scott , OBERLENDER, Rob
发明人： MICKLE, Travis , KRISHNAN, Suma , BISHOP, Barney , LAUDERBACK, Christopher , MONCRIEF, James, Scott , OBERLENDER, Rob
IPC分类号： A61K38/00
CPC分类号： A61K31/165 , A61K47/542 , C07C237/06 , Y02A50/415 , Y10S436/901 , Y10T436/173845
摘要： The invention describes compounds, compositions and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
摘要翻译：本发明描述了使用其的化合物，组合物和方法，其包含与苯丙胺共价连接的化学部分。这些化合物和组合物可用于减少或预防滥用和过量安非他明。这些化合物和组合物特别用于提供某些障碍（例如注意力缺陷多动障碍（ADHD），ADD，发作性睡病和肥胖）的耐药性替代治疗。苯丙胺的口服生物利用度维持在治疗有用的剂量。在较高剂量下，生物利用度显着降低，从而提供减少口服滥用责任的方法。此外，本发明的化合物和组合物通过肠胃外途径（例如静脉内或鼻内给药）降低苯丙胺的生物利用度，进一步限制其滥用责任。

4. 发明申请

WO2007120864A3 COMPOSITIONS AND METHODS FOR ENHANCING ANALGESIC POTENCY OF COVALENTLY BOUND COMPOUNDS, ATTENUATING ITS ADVERSE SIDE EFFECTS, AND PREVENTING THEIR ABUSE 审中-公开
标题翻译：组合物和方法，用于增强共轭化合物的分解性，降低其不利影响，并防止其滥用
公开(公告)号：WO2007120864A3
公开(公告)日：2008-08-28
申请号：PCT/US2007009220
申请日：2007-04-16
申请人： SHIRE LLC , KIRK RANDAL J , KRISHNAN SUMA , MONCRIEF JAMES SCOTT
发明人： KIRK RANDAL J , KRISHNAN SUMA , MONCRIEF JAMES SCOTT
IPC分类号： A61K31/485 , A61K9/20
CPC分类号： A61K31/485 , A61K9/0019 , A61K9/0043 , A61K47/64
摘要： The invention generally relates to compositions and methods with covalently bound compounds, such as controlled substances covalently attached to a chemical moiety, and opioid antagonists or covalently bound opioid antagonists to enhance analgesic potency and/or attenuate one or more adverse effects of covalently bound compounds, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence), physical dependence or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of a covalently bound compound and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of a covalently bound compound. The methods of the invention comprise administering to a subject an analgesic or sub-analgesic amount of a covalently bound compound and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of a covalently bound compound and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of covalently bound compound. The invention also relates to the addition of covalently-bound opioid antagonists to the compositions containing covalently bound compounds such that if the compositions are subjected to manipulation by illicit chemists, the opioid antagonist is released effectively reducing or eliminating the euphoric effect of the covalently bound compounds.
摘要翻译：本发明通常涉及具有共价结合的化合物的组合物和方法，例如共价连接到化学部分的受控物质，以及阿片样物质拮抗剂或共价结合的阿片样物质拮抗剂以增强镇痛效力和/或减弱共价结合的化合物的一种或多种不良作用，包括人体的不良副作用，如恶心，呕吐，头晕，头痛，镇静（嗜睡），身体依赖或瘙痒。本发明涉及用于选择性增强共价结合化合物的止痛效力的组合物和方法，并同时减轻与施用共价结合的化合物相关的抗镇痛，痛觉过敏，过度兴奋性，物理依赖性和/或耐受性作用。本发明的方法包括向受试者施用镇痛或次镇痛量的共价结合的化合物和一定量的兴奋性阿片样物质受体拮抗剂如纳曲酮或纳美芬，以有效提高共价结合的化合物的镇痛效力并减弱抗体 - 辛酸，痛觉过敏，过度兴奋，身体依赖和/或共价结合化合物的耐受性影响。本发明还涉及向包含共价结合的化合物的组合物中加入共价键合的阿片样物质拮抗剂，使得如果组合物被非法化学家操作，则阿片样物质拮抗剂有效地释放降低或消除共价结合化合物的欣快效应。

5. 发明申请

WO2007120864A2 COMPOSITIONS AND METHODS FOR ENHANCING ANALGESIC POTENCY OF COVALENTLY BOUND COMPOUNDS, ATTENUATING ITS ADVERSE SIDE EFFECTS, AND PREVENTING THEIR ABUSE 审中-公开
标题翻译：组合物和方法，用于增强共轭化合物的分解性，降低其不利影响，并防止其滥用
公开(公告)号：WO2007120864A2
公开(公告)日：2007-10-25
申请号：PCT/US2007/009220
申请日：2007-04-16
申请人： NEW RIVER PHARMACEUTICALS INC. , KIRK, Randal J. , KRISHNAN, Suma , MONCRIEF, James Scott
发明人： KIRK, Randal J. , KRISHNAN, Suma , MONCRIEF, James Scott
IPC分类号： A61K31/485
CPC分类号： A61K31/485 , A61K9/0019 , A61K9/0043 , A61K47/64
摘要： The invention generally relates to compositions and methods with covalently bound compounds, such as controlled substances covalently attached to a chemical moiety, and opioid antagonists or covalently bound opioid antagonists to enhance analgesic potency and/or attenuate one or more adverse effects of covalently bound compounds, including adverse side effect(s) in humans such as nausea, vomiting, dizziness, headache, sedation (somnolence), physical dependence or pruritis. This invention relates to compositions and methods for selectively enhancing the analgesic potency of a covalently bound compound and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of a covalently bound compound. The methods of the invention comprise administering to a subject an analgesic or sub-analgesic amount of a covalently bound compound and an amount of excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of a covalently bound compound and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of covalently bound compound. The invention also relates to the addition of covalently-bound opioid antagonists to the compositions containing covalently bound compounds such that if the compositions are subjected to manipulation by illicit chemists, the opioid antagonist is released effectively reducing or eliminating the euphoric effect of the covalently bound compounds.
摘要翻译：本发明通常涉及具有共价结合的化合物的组合物和方法，例如共价连接到化学部分的受控物质，以及阿片样物质拮抗剂或共价结合的阿片样物质拮抗剂以增强镇痛效力和/或减弱共价结合的化合物的一种或多种副作用，包括人体的不良副作用，如恶心，呕吐，头晕，头痛，镇静（嗜睡），身体依赖或瘙痒。本发明涉及用于选择性增强共价结合化合物的镇痛效力的组合物和方法，并同时减轻与施用共价结合的化合物相关的抗镇痛，痛觉过敏，兴奋性过高，物理依赖性和/或耐受性作用。本发明的方法包括向受试者施用镇痛或次镇痛量的共价结合化合物和一定量的兴奋性阿片样物质受体拮抗剂如纳曲酮或纳美芬，其有效提高共价结合化合物的镇痛效力并减弱抗 - 镇痛，痛觉过敏，过度兴奋，身体依赖和/或共价结合化合物的耐受性影响。本发明还涉及向包含共价结合的化合物的组合物中加入共价键合的阿片样物质拮抗剂，使得如果组合物被非法化学家操作，则有效释放阿片样物质拮抗剂以减少或消除共价结合化合物的欣快作用。

6. 发明申请

WO2006121552A9 ABUSE-RESISTANT AMPHETAMINE PRODRUGS 审中-公开
标题翻译：耐药AMPHETAMINE PRODRUGS
公开(公告)号：WO2006121552A9
公开(公告)日：2007-03-08
申请号：PCT/US2006013221
申请日：2006-04-10
申请人： NEW RIVER PHARMACEUTICALS INC , MICKLE TRAVIS , KRISHNAN SUMA , BISHOP BARNEY , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , OBERLENDER ROB , PICCARIELLO THOMAS
发明人： MICKLE TRAVIS , KRISHNAN SUMA , BISHOP BARNEY , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , OBERLENDER ROB , PICCARIELLO THOMAS
IPC分类号： A61K31/4015
CPC分类号： A61K31/4015 , A61K47/542
摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
摘要翻译：本发明描述了使用包含与苯丙胺共价连接的化学部分的化合物，组合物和方法。这些化合物和组合物可用于减少或预防滥用和过量安非他明。这些化合物和组合物特别用于提供某些障碍（例如注意力缺陷多动障碍（ADHD），ADD，发作性睡病和肥胖）的耐药性替代治疗。苯丙胺的口服生物利用度维持在治疗有用的剂量。在较高剂量下，生物利用度显着降低，从而提供减少口服滥用责任的方法。此外，本发明的化合物和组合物通过肠胃外途径（例如静脉内或鼻内给药）降低苯丙胺的生物利用度，进一步限制其滥用责任。

7. 发明申请

WO2007126832A2 PHARMACEUTICAL COMPOSITIONS FOR PREVENTION OF OVERDOSE OR ABUSE 审中-公开
标题翻译：用于防止过度或不适用的药物组合物
公开(公告)号：WO2007126832A2
公开(公告)日：2007-11-08
申请号：PCT/US2007/007594
申请日：2007-03-29
申请人： NEW RIVER PHARMACEUTICALS INC. , MICKLE, Travis , KRISHNAN, Suma , MONCRIEF, James, Scott , LAUDERBACK, Christopher , PICCARIELLO, Thomas , MILLER, Christal
发明人： MICKLE, Travis , KRISHNAN, Suma , MONCRIEF, James, Scott , LAUDERBACK, Christopher , PICCARIELLO, Thomas , MILLER, Christal
IPC分类号： A61K38/17
CPC分类号： A61K31/485 , A61K9/0019 , A61K9/0043 , A61K47/542 , A61K47/64
摘要： The invention relates to pharmaceutical compositions comprised of a chemical moiety attached to an active agent in a manner that substantially decreases the potential of the active agent to cause overdose or to be abused. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.
摘要翻译：本发明涉及药物组合物，其包含以活性剂附着于活性剂的化学部分，以显着降低活性剂引起过量或被滥用的潜力的方式。当以适当剂量递送时，药物组合物提供类似于母体活性剂的治疗活性。

8. 发明申请

WO2006121552A2 ABUSE-RESISTANT AMPHETAMINE PRODRUGS 审中-公开
标题翻译：耐药AMPHETAMINE PRODRUGS
公开(公告)号：WO2006121552A2
公开(公告)日：2006-11-16
申请号：PCT/US2006/013221
申请日：2006-04-10
申请人： NEW RIVER PHARMACEUTICALS INC. , MICKLE, Travis , KRISHNAN, Suma , BISHOP, Barney , MONCRIEF, James Scott , LAUDERBACK, Christopher , OBERLENDER, Rob , PICCARIELLO, Thomas
发明人： MICKLE, Travis , KRISHNAN, Suma , BISHOP, Barney , MONCRIEF, James Scott , LAUDERBACK, Christopher , OBERLENDER, Rob , PICCARIELLO, Thomas
IPC分类号： A61K31/4015
CPC分类号： A61K31/4015 , A61K47/542
摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
摘要翻译：本发明描述了使用包含与苯丙胺共价连接的化学部分的化合物，组合物和方法。这些化合物和组合物可用于减少或预防滥用和过量安非他明。这些化合物和组合物特别用于提供某些障碍（例如注意力缺陷多动障碍（ADHD），ADD，发作性睡病和肥胖）的耐药性替代治疗。苯丙胺的口服生物利用度维持在治疗有用的剂量。在较高剂量下，生物利用度显着降低，从而提供减少口服滥用责任的方法。此外，本发明的化合物和组合物通过肠胃外途径（例如静脉内或鼻内给药）降低苯丙胺的生物利用度，进一步限制其滥用责任。

9. 发明申请

WO2007120648A3 MONO AND DI-SUBSTITUTED OXYCODONE COMPOUNDS AND COMPOSITIONS 审中-公开
标题翻译：单和二取代的氧化剂化合物和组合物
公开(公告)号：WO2007120648A3
公开(公告)日：2008-07-17
申请号：PCT/US2007008821
申请日：2007-04-10
申请人： SHIRE LLC , MICKLE TRAVIS , KRISHNAN SUMA , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , BERA SANJIB
发明人： MICKLE TRAVIS , KRISHNAN SUMA , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , BERA SANJIB
IPC分类号： C07D471/00 , C07D489/00 , C07D491/00
CPC分类号： A61K9/0043 , A61K9/0019 , A61K47/55 , A61K47/64
摘要： The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to oxycodone in a manner that substantially decreases the potential for overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of oxycodone and may also provide sustained release characteristics and/or reduced side-effects. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction of oxycodone.
摘要翻译：本发明涉及药物化合物和组合物，其包含与羟考酮连接的化学部分，其基本上降低过量的潜力。当以适当的剂量递送时，药物组合物提供类似于羟考酮的治疗活性，并且还可以提供持续释放特征和/或减少的副作用。此外，本发明的化合物和组合物可用于预防成瘾和对羟考酮成瘾的易感性。

10. 发明申请

WO2006121552A3 ABUSE-RESISTANT AMPHETAMINE PRODRUGS 审中-公开
标题翻译：滥用抗药性苯丙胺前药
公开(公告)号：WO2006121552A3
公开(公告)日：2007-07-05
申请号：PCT/US2006013221
申请日：2006-04-10
申请人： NEW RIVER PHARMACEUTICALS INC , MICKLE TRAVIS , KRISHNAN SUMA , BISHOP BARNEY , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , OBERLENDER ROB , PICCARIELLO THOMAS
发明人： MICKLE TRAVIS , KRISHNAN SUMA , BISHOP BARNEY , MONCRIEF JAMES SCOTT , LAUDERBACK CHRISTOPHER , OBERLENDER ROB , PICCARIELLO THOMAS
IPC分类号： A61K38/16
CPC分类号： A61K31/4015 , A61K47/542
摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.
摘要翻译：本发明描述了包含与苯丙胺共价连接的化学部分的化合物，组合物和使用其的化合物的使用方法。这些化合物和组合物可用于减少或防止苯丙胺的滥用和过量使用。这些化合物和组合物特别用于为某些疾病如注意力缺陷多动障碍（ADHD），ADD，嗜睡症和肥胖症提供抗滥用的替代治疗。苯丙胺的口服生物利用度维持在治疗有效剂量。在较高剂量下，生物利用度显着降低，从而提供了减少口服滥用责任的方法。此外，本发明的化合物和组合物通过肠胃外途径如静脉内或鼻内给药降低苯丙胺的生物利用度，从而进一步限制其滥用可能性。

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