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1. 发明授权

US08946200B2 Pharmaceutically active nanosuspensions 有权
标题翻译：药物活性纳米悬浮液
公开(公告)号：US08946200B2
公开(公告)日：2015-02-03
申请号：US11555995
申请日：2006-11-02
申请人： Joseph A McDonough , Hong Dixon
发明人： Joseph A McDonough , Hong Dixon
IPC分类号： A01N43/00 , A61K31/33 , B29B9/00 , A61K31/57 , A61K9/14
CPC分类号： A61K31/57 , A61K9/14
摘要： The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.
摘要翻译：本公开涉及可以是光学透明的药学活性纳米颗粒悬浮液。这种悬浮液可以通过药学活性化合物在第一溶剂中的选择性溶解形成，随后引入第二溶剂如水性介质中，而基本不使用表面活性剂和/或机械剪切。

2. 发明授权

US08722706B2 Two phase bioactive formulations of bis-quaternary pyridinium oxime sulfonate salts 有权
标题翻译：双相吡啶鎓肟磺酸盐的两相生物活性制剂
公开(公告)号：US08722706B2
公开(公告)日：2014-05-13
申请号：US12192400
申请日：2008-08-15
申请人： Hong Dixon , Joseph A McDonough , Larry Allen Cabell , Patricia Underwood
发明人： Hong Dixon , Joseph A McDonough , Larry Allen Cabell , Patricia Underwood
IPC分类号： A61K31/4425 , A61K47/06
CPC分类号： A61K31/4425 , A61K9/0019 , A61K31/44 , A61K47/06 , A61K47/10 , C07D213/53
摘要： The present invention relates to two phase systems of a bioactive ingredient in particle form that has limited or no solubility in a liquid medium, which provides stability to the bioactive ingredient that is similar to the bioactive ingredient when in the solid state. The bioactive ingredient may be capable of therapeutically treating for the presence of a cholinesterase inhibitor. The bio active ingredient comprises 1,1′-methlyenebis[4-[(hydroxyimino)methyl]-pyridinium]dimethanesulfonate.
摘要翻译：本发明涉及在液体介质中具有有限或不溶性的颗粒形式的生物活性成分的两相体系，其在固体状态下对生物活性成分类似于生物活性成分提供稳定性。生物活性成分可能能够治疗治疗胆碱酯酶抑制剂的存在。生物活性成分包括1,1'-亚甲基双[4 - [（肟基）甲基] - 吡啶鎓]二甲磺酸盐。

3. 发明申请

US20120070503A1 Nanoparticle-Based Targeted Drug Delivery For In Vivo Bone Loss Mitigation 审中-公开
标题翻译：基于纳米粒子的靶向药物递送用于体内骨丢失缓解
公开(公告)号：US20120070503A1
公开(公告)日：2012-03-22
申请号：US12886334
申请日：2010-09-20
申请人： Hong DIXON , Qingwen NI , Joseph A. McDONOUGH
发明人： Hong DIXON , Qingwen NI , Joseph A. McDONOUGH
IPC分类号： A61K9/50 , A61P19/08 , A61K31/5415 , B82Y5/00
CPC分类号： A61K31/5415 , A61K9/5153 , B82Y5/00 , Y10T428/2982
摘要： The present invention is directed to nanoparticle-based targeted drug delivery system for treatment of bone-loss. An enantiomeric phenothiazine is formulated into an in-vivo nanoparticle delivery system which may contain bone-targeting functionality. The nanoparticle formulations and their associated influence on whole bone porosity may now also be evaluated utilizing nuclear magnetic resonance (NMR) and relaxation time profiles, and in particular, median T2 relaxation times.
摘要翻译：本发明涉及用于治疗骨丢失的基于纳米颗粒的靶向药物递送系统。将对映体吩噻嗪配制成体内纳米颗粒递送系统，其可以含有骨靶向功能。现在也可以使用核磁共振（NMR）和弛豫时间曲线，特别是中值T2弛豫时间来评估纳米颗粒制剂及其对全骨孔隙度的相关影响。

4. 发明授权

US07758778B2 Methods for preparing biodegradable microparticle formulations containing pharmaceutically active agents 有权
标题翻译：制备含有药物活性剂的可生物降解的微粒制剂的方法
公开(公告)号：US07758778B2
公开(公告)日：2010-07-20
申请号：US11220430
申请日：2005-09-07
申请人： Joseph T. Persyn , Joseph A. McDonough , Neal K. Vail , Darren E. Barlow , Albert M. Zwiener , Eliot M. Slovin
发明人： Joseph T. Persyn , Joseph A. McDonough , Neal K. Vail , Darren E. Barlow , Albert M. Zwiener , Eliot M. Slovin
IPC分类号： B29B9/00 , A61J3/00
CPC分类号： B01J13/04 , A61K9/1682 , A61K9/5089
摘要： This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.
摘要翻译：本发明涉及一种用于生产包含药理活性剂和可生物降解聚合物的微粒的装置和方法。该装置包括在其中心包含储存器的旋转盘和平坦的倾斜表面。该装置可选地包括锯齿状和/或平行于盘的旋转轴线的圆周周围的平坦表面。本发明还涉及使用旋转圆盘装置的含有药理活性剂的微粒的制造方法。提供含有眼科活性剂的制剂。还描述了显示零级释放速率的制剂。

5. 发明授权

US09040080B2 Processing of heat-sensitive active agents 有权
标题翻译：热敏活性剂的加工
公开(公告)号：US09040080B2
公开(公告)日：2015-05-26
申请号：US12255447
申请日：2008-10-21
申请人： Hong Dixon , Joseph A McDonough
发明人： Hong Dixon , Joseph A McDonough
IPC分类号： A61J3/07 , A61K9/48 , A61K9/50 , A61K9/16 , A61K9/70
CPC分类号： A61J3/07 , A61K9/1647 , A61K9/70
摘要： The present disclosure relates to a method of melt processing an active agent. The method may include encapsulating an active agent in a first polymer material exhibiting a first processing temperature T1 and forming capsules including the active agent. The method may also include melt processing the capsules with a second polymer material exhibiting a second processing temperature T2, wherein T1>T2.
摘要翻译：本公开涉及一种熔融加工活性剂的方法。该方法可以包括将活性剂包封在展现第一加工温度T1的第一聚合物材料中，并形成包含活性剂的胶囊。该方法还可以包括用显示第二处理温度T2的第二聚合物材料熔融加工胶囊，其中T1> T2。

6. 发明授权

US09028873B2 Nanoparticles for drug delivery to the central nervous system 有权
标题翻译：用于药物递送至中枢神经系统的纳米颗粒
公开(公告)号：US09028873B2
公开(公告)日：2015-05-12
申请号：US12702095
申请日：2010-02-08
申请人： Joseph A. McDonough , Hong Dixon , Larry A. Cabell
发明人： Joseph A. McDonough , Hong Dixon , Larry A. Cabell
IPC分类号： A61K9/14 , A61K31/444 , A61P25/00 , B32B5/00 , A61K9/50 , A61K9/51
CPC分类号： A61K31/444 , A61K9/5021 , A61K9/5115 , Y10S977/773 , Y10S977/906 , Y10T428/2982
摘要： The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also be of a specific polymorphic structure and which may be formed in either hydrophobic or hydrophilic type liquid media. In addition, the nanoparticle for transport across the blood-brain barrier may comprise a polymeric resin encapsulating a bis-quaternary pyridinium-2-aldoxime salt.
摘要翻译：本公开涉及用于制备纳米颗粒以提供这种颗粒相对更快速地输送穿过血脑屏障的组合物和方法。纳米颗粒可以由双季吡啶鎓 - 醛肟盐形成，其也可以是特定的多晶型结构并且可以在疏水或亲水型液体介质中形成。另外，用于跨血脑屏障传输的纳米颗粒可以包含包封双季吡啶鎓-2-羟基肟盐的聚合物树脂。

7. 发明授权

US5430189A Process for preparing substituted and unsubstituted arylalkylamines 失效
标题翻译：制备取代和未取代的芳基烷基胺的方法
公开(公告)号：US5430189A
公开(公告)日：1995-07-04
申请号：US185098
申请日：1994-01-19
申请人： Joseph A. McDonough , Ahmed M. Tafesh , Olan S. Fruchey
发明人： Joseph A. McDonough , Ahmed M. Tafesh , Olan S. Fruchey
IPC分类号： C07C209/00 , C07C209/40 , C07C215/52 , C07C249/08 , C07C209/38
CPC分类号： C07C215/52 , C07C209/00 , C07C209/40 , C07C249/08
摘要： An arylisonitrosoalkanone is hydrogenated in the presence of a noble metal catalyst and a weak carboxylic acid to form an arylalkanolamine which is then hydrogenated in the presence of a strong mineral acid and the transition metal catalyst to form an arylalkylamine. When the arylisonitrosoalkanone is an isonitrosoacetophenone, the isonitrosoacetophenone is prepared by one of two methods.In the first method, a substituted or an unsubstituted isonitrosoacetophenone is prepared from a corresponding substituted or unsubstituted acetophenone by oxidizing the acetophenone to form a substituted or an unsubstituted phenylglyoxalacetal in a reactor, hydrolyzing the phenylglyoxal acetal in the same reactor to form a corresponding substituted or unsubstituted phenylglyoxal, and condensing the phenylglyoxal with hydroxylamine or a salt thereof in the same reactor to form the substituted or unsubstituted isonitrosoacetophenone. Alternatively, the substituted or unsubstituted isonitrosoacetophenone is prepared from the corresponding substituted or unsubstituted acetophenone by reacting the substituted or unsubstituted acetophenone in water with a source of a nitrosonium ion in the presence of a strong acid to form a corresponding substituted or unsubstituted phenylglyoxal, and condensing the phenylglyoxal with hydroxylamine or a salt thereof to form the substituted or unsubstituted isonitrosoacetophenone. In either method, any strong acid that might be present in the reaction mass following the condensation to the isonitrosoacetophenone shall be removed therefrom prior to initiating the hydrogenation of the isonitrosoacetophenone to the arylalkanolamine.
摘要翻译：芳基亚硝基烷酮在贵金属催化剂和弱羧酸的存在下氢化形成芳基烷醇胺，然后在强无机酸和过渡金属催化剂的存在下氢化形成芳基烷基胺。当芳基亚硝基烷酮是异硝基苯乙酮时，通过两种方法之一制备异硝基苯乙酮。在第一种方法中，通过在反应器中氧化苯乙酮以形成取代或未取代的苯基乙醛缩醛，由相应的取代或未取代的苯乙酮制备取代或未取代的异硝基苯乙酮，在相同的反应器中水解苯乙醛缩醛形成相应的取代或未取代的苯乙酮缩醛，未取代的苯基乙二醛，并将苯乙醛酸与羟胺或其盐在同一反应器中缩合形成取代或未取代的异硝基苯乙酮。或者，取代或未取代的异硝基苯乙酮由相应的取代或未取代的苯乙酮通过在强酸存在下使取代或未取代的苯乙酮在水中与亚硝鎓离子源反应形成相应的取代或未取代的苯基乙二醛，并将苯基乙二醛与羟胺或其盐形成取代或未取代的异硝基苯乙酮。在任一种方法中，在将异亚氨基苯乙酮氢化成芳基烷醇胺之前，任何在与异亚硝基苯乙酮缩合后可能存在于反应物质中的强酸应从其中除去。

8. 发明授权

US5220066A Process for the preparation of arylethylamines and substituted arylethylamines 失效
公开(公告)号：US5220066A
公开(公告)日：1993-06-15
申请号：US859773
申请日：1992-03-30
申请人： Ahmed Tafesh , B. Frank Wood , Joseph A. McDonough , Graham N. Mott
发明人： Ahmed Tafesh , B. Frank Wood , Joseph A. McDonough , Graham N. Mott
IPC分类号： B01J23/42 , B01J23/44 , C07B61/00 , C07C209/40 , C07C211/16 , C07C213/02 , C07C215/46 , C07C215/48
CPC分类号： C07C213/02
摘要： This invention provides a process for directly preparing arylethylamines and their salts from (.alpha.-halo-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst. The process is illustrated by conversion of 4-hydroxy-(.alpha.-chloro-.alpha.-oximino)acetophenone to Tyramine hydrochloride: ##STR1##

9. 发明授权

US09693967B2 Biodegradable microparticle pharmaceutical formulations exhibiting improved released rates 有权
公开(公告)号：US09693967B2
公开(公告)日：2017-07-04
申请号：US11220807
申请日：2005-09-07
申请人： Joseph T. Persyn , Joseph A. McDonough , Neal K. Vail , Darren E. Barlow , Albert M. Zwiener , Eliot M. Slovin
发明人： Joseph T. Persyn , Joseph A. McDonough , Neal K. Vail , Darren E. Barlow , Albert M. Zwiener , Eliot M. Slovin
IPC分类号： A61K9/50 , A61K9/16 , A61K9/00
CPC分类号： A61K9/5089 , A61K9/0048 , A61K9/1694
摘要： This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

10. 发明申请

US20110195125A1 Nanoparticles For Drug Delivery To The Central Nervous System 有权
标题翻译：用于药物输送到中枢神经系统的纳米颗粒
公开(公告)号：US20110195125A1
公开(公告)日：2011-08-11
申请号：US12702095
申请日：2010-02-08
申请人： Joseph A. MCDONOUGH , Hong DIXON , Larry A. CABELL
发明人： Joseph A. MCDONOUGH , Hong DIXON , Larry A. CABELL
IPC分类号： A61K9/14 , A61K31/444 , B32B5/00 , A61P25/00
CPC分类号： A61K31/444 , A61K9/5021 , A61K9/5115 , Y10S977/773 , Y10S977/906 , Y10T428/2982
摘要： The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also be of a specific polymorphic structure and which may be formed in either hydrophobic or hydrophilic type liquid media. In addition, the nanoparticle for transport across the blood-brain barrier may comprise a polymeric resin encapsulating a bis-quaternary pyridinium-2-aldoxime salt of the formula:
摘要翻译：本公开涉及用于制备纳米颗粒以提供这种颗粒相对更快速地输送穿过血脑屏障的组合物和方法。纳米颗粒可以由双季吡啶鎓 - 醛肟盐形成，其也可以是特定的多晶型结构并且可以在疏水或亲水型液体介质中形成。另外，用于跨血脑屏障传输的纳米颗粒可以包含包封下式的双季吡啶鎓-2-醛肟盐的聚合物树脂：

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