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1. 发明授权

US06726919B2 Injectable dispersion of propofol 失效
标题翻译：异丙酚注射分散体
公开(公告)号：US06726919B2
公开(公告)日：2004-04-27
申请号：US09880104
申请日：2001-06-14
申请人： Gary W. Pace , Michael G. Vachon , Awadesh K. Mishra , Robert A. Snow
发明人： Gary W. Pace , Michael G. Vachon , Awadesh K. Mishra , Robert A. Snow
IPC分类号： A61F1300
CPC分类号： A61K31/7016 , A61K9/0019 , A61K9/1075 , A61K31/05 , A61K31/14 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/24 , A61K47/26 , A61K47/44 , Y02A50/473
摘要： A sterile, injectable homogenized dispersion of micromatrices or microdroplets having a mean diameter from about 50 nm to about 1000 nm comprising about 1% to about 7.5% of propofol, about 1% to about 8% of a propofol-soluble diluent, and about 0.67% to about 5% of a surface stabilizing amphiphilic agent suspended in an aqueous medium containing a synergetic quantity of antimicrobial agent and a tonicity modifying amount of a pharmaceutically acceptable water-soluble hydroxyl-group-containing excipient, wherein the ratio of propofol to diluent is in the range of about 0.25 to about 7.5 while the ratio of propofol to amphiphilic agent is in the range from about 0.4 to about 1.5, and wherein the viscosity of the dispersion is in the range of 1.1 to 8 cps, processes for the formation of the dispersion, and methods of use are disclosed.
摘要翻译：平均直径约50nm至约1000nm的微量或微滴的无菌注射匀浆分散体，其包含约1％至约7.5％的异丙酚，约1％至约8％的异丙酚可溶性稀释剂和约0.67 悬浮在含有协同量的抗微生物剂的水性介质中的表面稳定两亲剂的百分比至约5％，以及药学上可接受的水溶性含羟基赋形剂的张力调节量，其中异丙酚与稀释剂的比例为在约0.25至约7.5的范围内，而丙泊酚与两亲剂的比例在约0.4至约1.5的范围内，并且其中分散体的粘度在1.1至8cps的范围内，形成公开了分散体和使用方法。

2. 发明授权

US06696084B2 Spray drying process and compositions of fenofibrate 有权
标题翻译：喷雾干燥工艺和非诺贝特组合物
公开(公告)号：US06696084B2
公开(公告)日：2004-02-24
申请号：US09838593
申请日：2001-04-20
申请人： Gary W. Pace , Awadesh K. Mishra , Robert A. Snow , Indu Parikh , Pol-Henri W. Guivarc'h
发明人： Gary W. Pace , Awadesh K. Mishra , Robert A. Snow , Indu Parikh , Pol-Henri W. Guivarc'h
IPC分类号： A61K914
CPC分类号： A61K31/66 , A61K9/145 , A61K9/1623 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/505 , A61K45/06 , A61K31/215 , A61K2300/00
摘要： The present invention relates to a novel spray drying process for the preparation of pharmaceutical compositions containing small particles of phospholipid-stabilized fenofibrate. This invention also relates to spray dried powdered compositions prepared according to this process, and to dosage forms of fenofibrate (capsules, tablets, powders, granules, and dispersions) prepared from these powdered compositions. The powdered compositions and dosage forms are useful in the treatment of dyslipidemia and dyslipoproteinemia and have the advantage that they provide reduced in vivo variability in the bioavailability of fenofibrate active species among fed and fasted patients when administered orally.
摘要翻译：本发明涉及一种用于制备含有磷脂稳定的非诺贝特的小颗粒的药物组合物的新型喷雾干燥方法。本发明还涉及根据该方法制备的喷雾干燥的粉末组合物，以及由这些粉末状组合物制备的非诺贝特（胶囊，片剂，粉末，颗粒剂和分散体）的剂型。粉末组合物和剂型可用于治疗血脂异常和血脂异常，并且具有这样的优点：当口服给药时，它们在进食和禁食患者中提供非诺贝特活性物质的生物利用度的体内变异性降低。

3. 发明授权

US06604698B2 Media milling 有权
公开(公告)号：US06604698B2
公开(公告)日：2003-08-12
申请号：US09852054
申请日：2001-05-10
申请人： Frank H. Verhoff , Robert A. Snow , Gary W. Pace
发明人： Frank H. Verhoff , Robert A. Snow , Gary W. Pace
IPC分类号： B02C1716
CPC分类号： A61K9/14 , A61K9/145 , B02C17/161 , Y10S977/775 , Y10S977/797 , Y10S977/90
摘要： This invention describes a process for preparing a dispersion of solid particles of a milled substrate in a fluid carrier comprising the steps of (a) providing a plurality of large size milling media to the milling chamber of a media mill and forming a depth filter therefrom on an exit screen or separator in the milling chamber; (b) adding to said milling chamber a plurality of small size milling media optionally containing additional large size milling media, a conglomerate of a solid substance comprising a substrate to be milled and optionally one or more than one surface active substance, and a fluid carrier; (c) milling said conglomerate in said milling chamber to produce very small milled substrate product particles; and (d) separating said milled substrate particles suspended in said fluid carrier from the media through said depth filter; wherein the exit screen comprises openings of size S0; the large size media have a size distribution S1 of which all are larger than S0; the small size media have a size distribution S2 which are smaller than S0; the very small milled substrate particles have a size distribution S3 and are smaller than all of the small media; and the large size media and the small size media are essentially retained in the milling chamber.

4. 发明授权

US06634576B2 Milled particles 有权
公开(公告)号：US06634576B2
公开(公告)日：2003-10-21
申请号：US09940864
申请日：2001-08-29
申请人： Frank Verhoff , Gary W. Pace , Robert A. Snow , Fay Millar
发明人： Frank Verhoff , Gary W. Pace , Robert A. Snow , Fay Millar
IPC分类号： B02C1214
CPC分类号： A61K9/14
摘要： A process for milling a solid substrate in the milling chamber of a dispersion or media mill in the presence of a two or more compositions of milling media bodies is disclosed wherein all milling media bodies contribute to the grinding of the solid substrate and wherein at least one composition of media bodies provides fragments of milling media bodies that are retained with the milled solid substrate particles in the form of a synergetic commixture produced in the milling process. More specifically, a process is disclosed for preparing a synergetic commixture comprising small particles of a solid substrate and small particulates of a first material of a desired size comprising the steps of (a) providing to the milling chamber of a media mill a contents comprising a pre-mix of a solid substrate, a fluid carrier, a plurality of milling bodies of a first material having a fracture toughness Kc1, and a plurality of milling bodies of a second material having a fracture toughness Kc2; (b) operating the media mill to grind the solid substrate and degrade at least a portion of the milling bodies of first material to produce a dispersion in the fluid carrier comprising a synergetic commixture of small particulates of the first material and small particles of the solid substrate having a desired size equal to or less than a size Sp; (c) separating the dispersion from any milling bodies and solid substrate particles having a size larger than Sp; and (d) optionally removing the fluid carrier from the dispersion to form a synergetic commixture free of fluid and comprising the particles and the small particulates, wherein KC2 is greater than KC1.

5. 发明授权

US5559214A Unsymmetrical complexing agents and targeting immunoreagents useful in thearpeutic and diagnostic compositions and methods 失效
标题翻译：非对称络合剂和靶向免疫试剂可用于临床和诊断组合物和方法
公开(公告)号：US5559214A
公开(公告)日：1996-09-24
申请号：US69242
申请日：1993-05-28
申请人： Daniel J. Delecki , Ashis K. Saha , Robert A. Snow
发明人： Daniel J. Delecki , Ashis K. Saha , Robert A. Snow
IPC分类号： A61K47/48 , A61K51/04 , A61K51/10 , C07D213/26 , C07D213/30 , C07D213/48 , C07D213/56 , C07D213/61 , C07D213/74 , C07D213/75 , C07D213/84 , C07F13/00 , C07D213/22 , C07F5/00
CPC分类号： C07D213/84 , A61K47/48707 , A61K51/0478 , A61K51/1093 , C07D213/26 , C07D213/30 , C07D213/48 , C07D213/56 , C07D213/61 , C07D213/74 , C07D213/75 , A61K2121/00 , A61K2123/00
摘要： ##STR1## Unsymmetrical oligo-2,6-pyridine complexing agents, metal chelates and targeting immunoreagents containing such complexing agents are provided, as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.
摘要翻译：提供了非对称寡聚-2,6-吡啶络合剂，金属螯合物和含有这种络合剂的靶向免疫试剂，以及含有这种免疫反应剂的诊断和治疗组合物以及使用免疫反应剂的诊断和治疗方法。

6. 发明授权

US5539117A 2-acetyl-6-cyanopyridines and their use as intermediates in the synthesis of oligo-2,6-pyridines 失效
标题翻译： 2-乙酰基-6-氰基吡啶并且它们用作合成低聚-2,6-吡啶的中间体
公开(公告)号：US5539117A
公开(公告)日：1996-07-23
申请号：US277193
申请日：1994-07-19
申请人： Robert A. Snow , Daniel J. Delecki , Chandra R. Shah , K. Robert Hollister
发明人： Robert A. Snow , Daniel J. Delecki , Chandra R. Shah , K. Robert Hollister
IPC分类号： C07D213/84 , C07D405/06 , C07F7/18 , C07D213/22 , C07F7/02
CPC分类号： C07D213/84 , C07D405/06 , C07F7/1856
摘要： The present invention is directed to 2-acetyl-6-cyanopyridine compounds that are useful as intermediates in the synthesis of oligo-2,6-pyridines. The present invention is also directed to new, simpler, less expensive methods for synthesizing such oligopyridines using the novel 2-acetyl-6-cyanopyridine compounds as intermediates.
摘要翻译：本发明涉及可用作合成低聚-2,6-吡啶的中间体的2-乙酰基-6-氰基吡啶化合物。本发明还涉及使用新颖的2-乙酰基-6-氰基吡啶化合物作为中间体合成这种低聚吡啶的新的，更简单的，更便宜的方法。

7. 发明授权

US5532150A Low diol polyalkylene oxide biologically active proteinaceous substances 失效
标题翻译：低二醇聚环氧烷生物活性蛋白质物质
公开(公告)号：US5532150A
公开(公告)日：1996-07-02
申请号：US245999
申请日：1994-05-19
申请人： Robert A. Snow , David L. Ladd , Denton W. Hoyer
发明人： Robert A. Snow , David L. Ladd , Denton W. Hoyer
IPC分类号： A61K38/00 , A61K38/43 , A61K47/48 , A61P9/00 , A61P9/10 , A61P29/00 , C12N9/96
CPC分类号： A61K47/48215 , Y10S514/886
摘要： Disclosed are pharmaceutical compositions containing low diol polyethylene glycol, covalently attached to superoxide and dismutase process of making the compositions. Also disclosed is a method of treatment of disease processes associated with the adverse effects on tissue of superoxide anions, such as ischemic events, reperfusion injury, trauma and inflammation.
摘要翻译：公开了含有低二醇聚乙二醇的药物组合物，其共价连接到超氧化物上，并且构成组合物的歧化酶过程。还公开了一种治疗与超氧化物阴离子对组织的不良反应（例如缺血事件，再灌注损伤，创伤和炎症）相关的疾病过程的方法。

8. 发明授权

US08703202B2 Coated tablets 有权
标题翻译：涂层片剂
公开(公告)号：US08703202B2
公开(公告)日：2014-04-22
申请号：US11492373
申请日：2006-07-24
申请人： Michael Vachon , Mishra K. Awadhesh , Robert A. Snow , Pol-Henri Guivarc'h
发明人： Michael Vachon , Mishra K. Awadhesh , Robert A. Snow , Pol-Henri Guivarc'h
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K31/19 , A61K31/216 , A61K9/48
CPC分类号： A61K9/14 , A61K9/145 , A61K9/146 , A61K9/148 , A61K9/16 , A61K9/1623 , A61K9/1629 , A61K9/167 , A61K9/1676 , A61K9/19 , A61K9/20 , A61K9/2077 , A61K9/282 , A61K9/284 , A61K9/2866 , A61K9/48 , A61K31/192 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/505 , A61K31/66 , A61K2300/00
摘要： Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.
摘要翻译：公开了包含非诺贝特，磷脂，缓冲盐，选自麦芽糖糊精，甘露糖醇及其组合的水溶性填充剂的药学上可接受的口服剂型，纤维素添加剂，药学上可接受的水溶性赋形剂载体材料的珠粒或晶体，聚乙烯吡咯烷酮或交聚维酮，交联羧甲基纤维素钠，颗粒状甘露醇，十二烷基硫酸钠，二氧化硅和硬脂酸盐，其中非诺贝特为微粒形式，并且其中至少一部分磷脂被涂覆在非诺贝特微粒，将包含磷脂的微粒嵌入包含水溶性填充剂的基质，未涂覆在微粒上的磷脂，缓冲盐和纤维素添加剂，并且将基质涂覆在至多100％的表面上赋形剂载体材料的珠粒或晶体。

9. 发明授权

US06465016B2 Cyclosporiine particles 有权
公开(公告)号：US06465016B2
公开(公告)日：2002-10-15
申请号：US09750218
申请日：2000-12-29
申请人： Indu Parikh , Robert A. Snow
发明人： Indu Parikh , Robert A. Snow
IPC分类号： A61K914
CPC分类号： B82Y5/00 , A61K9/145
摘要： Pharmaceutical compositions containing solid cyclic oligopeptide cyclosporine microparticles are prepared by applying energy input to solid cyclic oligopeptide cyclosporine in the presence of phospholipid and one or more non-ionic, anionic or cationic second surface modifiers. The microparticles consist essentially of a solid cyclic oligopeptide cyclosporine core coated with a combination of phospholipid and at least one second surface modifier. The combination of phospholipid and second surface modifier(s) provide volume-weighted mean particle size values of solid cyclic oligopeptide cyclosporine particles that are about 50% smaller than cyclic oligopeptide cyclosporine particles produced in the presence of the phospholipid and without the presence of the second surface modifier(s) using the same energy input.

10. 发明授权

US5932188A Therapeutic and diagnostic imaging compositions and methods 失效
标题翻译：治疗和诊断成像组合物和方法
公开(公告)号：US5932188A
公开(公告)日：1999-08-03
申请号：US963125
申请日：1997-10-28
申请人： Robert A. Snow , David L. Ladd , John L. Toner
发明人： Robert A. Snow , David L. Ladd , John L. Toner
IPC分类号： A61K47/48 , A61K49/00 , A61K51/00 , A61K51/04 , C08G65/34 , C08G65/48 , C08G69/40 , A61B5/055 , C07F5/00
CPC分类号： A61K47/48215 , A61K47/48192 , A61K47/48207 , A61K51/0497 , A61K2123/00
摘要： This invention provides therapeutic and diagnostic imaging compositions and methods featuring a polymer comprising units containing a poly(alkylene oxide) moiety linked to the residue of a chelating agent, said polymer having a cytotoxic agent associated therewith.
摘要翻译：本发明提供治疗和诊断成像组合物和方法，其特征在于包含含有与螯合剂残基连接的聚（环氧烷）部分的单元的聚合物，所述聚合物具有与其相关的细胞毒性剂。

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