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1. 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。

2. 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。

3. 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。

4. 发明申请

WO2007030577A3 PRODRUGS OF T3 AND T4 WITH ENHANCED BIOAVAILABILITY 审中-公开
标题翻译： T3和T4的产品具有增强的生物利用度
公开(公告)号：WO2007030577A3
公开(公告)日：2007-10-25
申请号：PCT/US2006034790
申请日：2006-09-08
申请人： NEW RIVER PHARMACEUTICALS INC , MONCRIEF JAMES SCOTT , MICKLE TRAVIS , OLON LAWRENCE , PICCARIELLO THOMAS
发明人： MONCRIEF JAMES SCOTT , MICKLE TRAVIS , OLON LAWRENCE , PICCARIELLO THOMAS
IPC分类号： C12P13/04 , A01N37/18
CPC分类号： A61K38/06 , A61K31/198 , A61K38/05 , A61K45/06 , A61K47/542 , A61K47/64 , A61K2300/00
摘要： The invention relates to compositions of amino acid and peptide conjugates comprising T3 and/or T4. The T3 or T4 is covalently attached to at least one amino acid via the N-terminus, the C-terminus, a side chain of the peptide carrier, and/or interspersed within the peptide chain. Also discussed are methods for protecting and administering active agents and methods for treating thyroid disorders.
摘要翻译：本发明涉及包含T3和/或T4的氨基酸和肽缀合物的组合物。 T3或T4通过N末端，C末端，肽载体的侧链和/或分散在肽链内共价连接至至少一个氨基酸。还讨论了用于保护和施用活性剂和治疗甲状腺疾病的方法的方法。

5. 发明申请

WO2004062614A3 CARBOHYDRATE CONJUGATES TO PREVENT ABUSE OF CONTROLLED SUBSTANCES 审中-公开
标题翻译：碳氢化合物可以防止受控物质的滥用
公开(公告)号：WO2004062614A3
公开(公告)日：2005-05-06
申请号：PCT/US2004000646
申请日：2004-01-13
申请人： NEW RIVER PHARMACEUTICALS INC , MICKLE TRAVIS , PICCARIELLO THOMAS , MONCRIEF JAMES SCOTT , BOERTH NANCY JOHNSTON , BISHOP BARNEY
发明人： MICKLE TRAVIS , PICCARIELLO THOMAS , MONCRIEF JAMES SCOTT , BOERTH NANCY JOHNSTON , BISHOP BARNEY
IPC分类号： A61K31/485 , A61K31/70 , A61K45/06 , A61K47/48
CPC分类号： A61K31/70 , A61K31/485 , A61K45/06 , A61K47/549 , A61K2300/00
摘要： The invention provides a "street-safe" version of a controlled substance that permits the therapeutically beneficial effects of the substance while reducing or eliminating the euphoric effects that lead to substance abuse. The invention provides pharmaceutical compositions comprising a controlled substance and a carbohydrate covalently bound to said controlled substance in a manner that renders said controlled substance pharmacologically inactive or substantially diminishes its activity and methods of using the same.
摘要翻译：本发明提供了一种“街道安全”的受控物质版本，其允许物质的治疗有益效果，同时减少或消除导致药物滥用的欣快效应。本发明提供药物组合物，其包含受控物质和与所述受控物质共价结合的碳水化合物，使得所述受控物质在药理学上无活性或显着降低其活性及其使用方法。

6. 发明申请

WO2004041208A3 CONTROLLED ABSORPTION OF MIXED THYROYD HORMONE FORMULATIONS 审中-公开
标题翻译：混合三氯呋喃配方的控制吸收
公开(公告)号：WO2004041208A3
公开(公告)日：2005-02-03
申请号：PCT/US0335166
申请日：2003-11-05
申请人： NEW RIVER PHARMACEUTICALS INC , OLON LAWRENCE PETER , PICCARIELLO THOMAS , MONCRIEF JAMES SCOTT , BOERTH NANCY JOHNSTON
发明人： OLON LAWRENCE PETER , PICCARIELLO THOMAS , MONCRIEF JAMES SCOTT , BOERTH NANCY JOHNSTON
IPC分类号： A61K31/198 , A61K31/05 , A61K31/14 , A61K31/195
CPC分类号： A61K31/198 , A61K2300/00
摘要： The invention relates to admixtures of the thyroid hormones and derivatives thereof. These admixtures, particularly L-thyroxine (T4) and liothyronine (T3), produce steady state or near steady state serum levels of (T3). When admixed in the appropriate ratio of (T4) to (T3), blood levels of (T3) hormone are maintained at a steady state for an extended period of time independent of the need for control release excipients. The change in the kinetics of (T3) absorption is controlled by the addition of (T4) to (T3).
摘要翻译：本发明涉及甲状腺激素及其衍生物的混合物。这些混合物，特别是L-甲状腺素（T4）和氨基丝氨酸（T3），产生（T3）的稳态或接近稳态血清水平。当以（T4）至（T3）的适当比例混合时，（T3）激素的血液水平长时间保持在稳定状态，而与对照释放赋形剂的需要无关。通过添加（T4）至（T3）来控制（T3）吸收动力学的变化。

7. 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

8. 发明专利

CA2428971A1 A NOVEL PHARMACEUTICAL COMPOUND CONTAINING ABACAVIA NOVEL PHARMACEUTICAL COMPOUND CONTAINING ABACAVIR SULFATE AND METHODS OF MAKING AND USING SAME R SULFATE AND METHODS OF MAKING AND USING SAME 未知
公开(公告)号：CA2428971A1
公开(公告)日：2003-05-01
申请号：CA2428971
申请日：2001-11-14
申请人： NEW RIVER PHARMACEUTICALS INC , PICCARIELLO THOMAS
发明人： PICCARIELLO THOMAS
IPC分类号： A61K31/506 , A61K31/52 , A61K9/22 , A61K47/42 , A61K47/48
摘要： A composition comprising a polypeptide and benzatropine mesylate covalently attached to the polypeptide. Also provided is a method for delivery of benzatropine mesylate to a patient comprising administering to the patient a composition comprising a polypeptide and benzatropine mesylate covalently attached to the polypeptide. Also provided is a method for protecting benzatropine mesylate from degradation comprising covalently attaching it to a polypeptide. Also provided is a method for controlling release of benzatropine mesylate from a composition comprising covalently attaching it to the polypeptide.

9. 发明专利

CA3127092A1 SOLID MICELLAR COMPOSITIONS OF CANNABINOID ACIDS 未知
公开(公告)号：CA3127092A1
公开(公告)日：2020-07-23
申请号：CA3127092
申请日：2020-01-17
申请人： MULHARE MICHAELA , SYNTHONICS INC , PICCARIELLO THOMAS , PALMER SCOTT
发明人： MULHARE MICHAELA , PICCARIELLO THOMAS , PALMER SCOTT
IPC分类号： A01H6/28 , A61K9/107 , A61K31/352
摘要： Solid, micellar compositions, comprising micelles of one or more cannabinoid acids and a metal, wherein the cannabinoid acids are in a salt form, the salt form has a monovalent counter ion, and the micelles are free of added surfactants, are disclosed. Additionally, processes for preparing solid, micellar compositions, comprising micelles of one or more cannabinoid acids and a metal, wherein the cannabinoid acids are in a salt form, the salt form has monovalent counter ion, and the micelles are free of added surfactants, are disclosed. Finally, methods of treating a number of disorders comprising the step of administering to a patient in need thereof a therapeutically effective amount of a solid, micellar composition comprising micelles of one or more cannabinoid acids and a metal, wherein the cannabinoid acids are in a salt form, the salt form has monovalent counter ion, and the micelles are free of added surfactants, are disclosed.

10. 发明申请

WO2007050181A3 METAL COORDINATED COMPOSITIONS 审中-公开
标题翻译：金属协调组合物
公开(公告)号：WO2007050181A3
公开(公告)日：2007-08-16
申请号：PCT/US2006031757
申请日：2006-08-15
申请人： SYNTHONICS INC , PICCARIELLO THOMAS
发明人： PICCARIELLO THOMAS
IPC分类号： A61K9/50
CPC分类号： C07F3/02 , A61K47/52 , A61K47/547 , A61K47/55 , A61K47/552 , C07F3/003 , C07F3/06 , C07H21/02
摘要： A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.
摘要翻译：公开了生物活性部分和金属的金属配位络合物。复合物赋予生物活性部分改进的性能，其可以包括效力，稳定性，吸收性，靶向递送及其组合。

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