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1. 发明专利

JP2010229140A Active agent delivery system and method for protecting and administering active agent 审中-公开
标题翻译：活性剂递送系统和保护和管理活性剂的方法
公开(公告)号：JP2010229140A
公开(公告)日：2010-10-14
申请号：JP2010114223
申请日：2010-05-18
申请人： Shire Llc , シャイアエルエルシー
发明人： PICCARIELLO THOMAS , KIRK RANDAL J , OLON LAWRENCE P
IPC分类号： A61K47/48 , A61K47/12 , A61K47/18 , A61K47/34 , A61K47/40 , A61K47/42 , C07K5/06 , C07K5/08 , C07K7/00
摘要： PROBLEM TO BE SOLVED: To provide drug delivery systems and the like, enabling use of new molecular compositions improving active agent performance associated with absorption parameter and stability and decreasing risk of technological aspect, controlling aspect and financial aspect accompanied with the active agent. SOLUTION: There are provided active agent delivery systems, and more specifically, compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents, and conjugated active agent compositions. More specifically, a composition comprising a carrier peptide that comprises at least one active agent covalently attached to the carrier peptide at the C-terminus, interspersed, side-chain attached, or combination thereof, wherein the carrier peptide further comprises fewer than 50 amino acids, and wherein the composition is in a form suitable for release of the active agent into the bloodstream. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供药物递送系统等，使得能够使用改善与吸收参数和稳定性相关的活性剂性能的新分子组合物，降低技术方面的风险，伴随活性剂的控制方面和财务方面。提供了活性剂递送系统，更具体地，包含与活性剂共价连接的氨基酸，单个氨基酸或肽共轭活性剂组合物的组合物。更具体地，包含载体肽的组合物，其包含至少一种在C-末端共价连接到载体肽的活性剂，散在，侧链连接或其组合，其中所述载体肽还包含少于50个氨基酸，并且其中所述组合物是适于将活性剂释放到血流中的形式。版权所有（C）2011，JPO＆INPIT

2. 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。

3. 发明专利

AU2003219863B2 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances 未知
公开(公告)号：AU2003219863B2
公开(公告)日：2008-07-31
申请号：AU2003219863
申请日：2003-02-24
申请人： SHIRE LLC
发明人： PICCARIELLO THOMAS , KIRK RANDAL J
IPC分类号： A61K47/48 , A61K31/135 , A61K31/137 , A61K31/222 , A61K31/4458 , A61K31/4468 , A61K31/4535 , A61K31/485 , A61P25/04 , A61P25/36 , A61P43/00
摘要： The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time-dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time-dependent manner (sustained release) by way of serum enzymes.

4. 发明专利

CA2648659A1 COMPOSITIONS AND METHODS FOR ENHANCING ANALGESIC POTENCY OF COVALENTLY BOUND COMPOUNDS, ATTENUATING ITS ADVERSE SIDE EFFECTS, AND PREVENTING THEIR ABUSE 未知
公开(公告)号：CA2648659A1
公开(公告)日：2007-10-25
申请号：CA2648659
申请日：2007-04-16
申请人： SHIRE LLC
发明人： KIRK RANDAL J , MONCRIEF JAMES SCOTT , KRISHNAN SUMA
IPC分类号： A61K31/485 , A61K9/20
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.

5. 发明专利

AU2008229978A1 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances 未知
公开(公告)号：AU2008229978A1
公开(公告)日：2008-11-06
申请号：AU2008229978
申请日：2008-10-16
申请人： SHIRE LLC
发明人： PICCARIELLO THOMAS , KIRK RANDAL J
IPC分类号： A61K47/48 , A61K31/135 , A61K31/137 , A61K31/222 , A61K31/4458 , A61K31/4468 , A61K31/4535 , A61K31/485 , A61P25/04 , A61P25/36 , A61P43/00
摘要： The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time-dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time-dependent manner (sustained release) by way of serum enzymes.

6. 发明专利

AU2005304751A1 Synergistic effects of combined administration of mirtazapine and a stimulant compound 未知
公开(公告)号：AU2005304751A1
公开(公告)日：2006-05-18
申请号：AU2005304751
申请日：2005-11-07
申请人： SHIRE LLC
发明人： KIRK RANDAL J
IPC分类号： A61K38/16 , A61K31/137 , A61K31/445 , A61K31/551
摘要： The invention discloses combination therapies and formulations of a stimulant (e.g., amphetamine) and mirtazapine and their methods of use.

7. 发明专利

CA2740256A1 NOVEL SUSTAINED RELEASE PHARMACEUTICAL COMPOUNDS TO PREVENT ABUSE OF CONTROLLED SUBSTANCES 未知
公开(公告)号：CA2740256A1
公开(公告)日：2003-09-04
申请号：CA2740256
申请日：2003-02-24
申请人： SHIRE LLC
发明人： PICCARIELLO THOMAS , KIRK RANDAL J
IPC分类号： A61K47/48

8. 发明公开

EP1812040A4 SYNERGISTIC EFFECTS OF COMBINED ADMINISTRATION OF MIRTAZAPINE AND A STIMULANT COMPOUND 审中-公开
标题翻译：协同效应米氮平联合用药和兴奋剂的连接
公开(公告)号：EP1812040A4
公开(公告)日：2010-05-05
申请号：EP05848555
申请日：2005-11-07
申请人： SHIRE LLC
发明人： KIRK RANDAL J
IPC分类号： A61K31/55 , A01N25/34 , A01N43/00 , A61K9/20 , A61K9/48 , A61K31/137 , A61K31/4458 , A61K45/06 , A61K47/48 , A61P3/04 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/30
CPC分类号： A61K31/55 , A61K31/137 , A61K31/445 , A61K31/4458 , A61K31/551 , A61K45/06 , A61K47/55 , A61K2300/00

9. 发明专利

AU2003219863C1 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances 未知
公开(公告)号：AU2003219863C1
公开(公告)日：2009-03-05
申请号：AU2003219863
申请日：2003-02-24
申请人： SHIRE LLC
发明人： PICCARIELLO THOMAS , KIRK RANDAL J
IPC分类号： A61K47/48 , A61K31/135 , A61K31/137 , A61K31/222 , A61K31/4458 , A61K31/4468 , A61K31/4535 , A61K31/485 , A61P25/04 , A61P25/36 , A61P43/00
摘要： The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time-dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time-dependent manner (sustained release) by way of serum enzymes.

10. 发明专利

AU2003213259B2 Use of peptide-drug conjugation to reduce inter-subject variability of drug serum levels 未知
公开(公告)号：AU2003213259B2
公开(公告)日：2009-01-08
申请号：AU2003213259
申请日：2003-02-24
申请人： SHIRE LLC
发明人： PICCARIELLO THOMAS , KIRK RANDAL J
IPC分类号： A61K38/22 , A61K45/00 , A61K47/48 , A61P5/14 , C07K5/06
摘要： The present invention provides compositions and methods to decrease inter-patient variability particularly with respect to the systemic concentration of a drug. More particularly the invention relates to oral drugs which are conjugated to peptides or related carriers which alter release characteristics as compared to the analogous free drug.

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