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1. 发明专利

HRP970715A2 SUSTAINED RELEASE CISAPRIDE MINI-TABLET FORMULATION 未知
公开(公告)号：HRP970715A2
公开(公告)日：1998-10-31
申请号：HRP970715
申请日：1997-12-30
申请人： KENNETH IAIN CUMMING
发明人： CUMMING KENNETH IAIN
IPC分类号： A61K9/20 , A61K9/22 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/445 , A61K31/4468 , A61P1/00 , A61K9/00
摘要： A sustained release cisapride oral dosage formulation suitable for once-daily administration comprises a plurality of mini-tablets containing cisapride or a salt thereof with an organic acid and capable of releasing cisapride at different sites along the gastrointestinal tract. The mini-tablets include a proportion of immediate release tablets and a proportion of tablets which release cisapride in response to the pH environment at a given site in the distal regions of the gastrointestinal tract and which include cisapride or a salt thereof embedded in a matrix of hydrophilic polymer, said matrix being coated with a pH dependent polymer, the formulation having a Cmax/Cmin ratio under steady state conditions of 2:1 or less as evidenced by a substantially flat plasma profile in vivo.

2. 发明申请

US20100119611A1 Delivery of a Bioactive Material 失效
标题翻译：生物活性物质的交付
公开(公告)号：US20100119611A1
公开(公告)日：2010-05-13
申请号：US12691927
申请日：2010-01-22
申请人： Maurice Joseph Anthony Clancy , K. Iain Cumming , Conor B. Mc Crystal
发明人： Maurice Joseph Anthony Clancy , K. Iain Cumming , Conor B. Mc Crystal
IPC分类号： A61K9/14 , A61K33/42
CPC分类号： A61K9/141 , A61K9/145 , A61K9/146 , A61K9/4833 , A61K9/4858 , A61K9/4866
摘要： A solid pharmaceutical composition comprising a water-soluble bioactive material and an encapsulating material which is present in the composition in the form of continuous solid phase, and in which solid particles of the bioactive material are dispersed and encapsulated in the continuous solid phase of the encapsulating material, wherein each of the bioactive material and the encapsulating material is normally a solid at room temperature and the melting point of the encapsulating material is lower than the melting point of the bioactive material, the bioactive material being preferably a bisphosphonate, most preferably alendronate, and the encapsulating material includes an enhancer, preferably a mono- or di-glyceride, or an encapsulating surfactant, preferably a polyoxyethylene/polyoxypropylene block copolymer having surface active properties, and a process for preparing the composition in which solid particles of the bioactive material are mixed with and dispersed in the encapsulating material which is in molten (liquid) form; and cooling the molten form of the encapsulating material to form a solid pharmaceutical composition having the solid particles of the bioactive material dispersed and encapsulated in a continuous solid phase of the encapsulating material.
摘要翻译：一种固体药物组合物，其包含以连续固相形式存在于组合物中的水溶性生物活性材料和封装材料，其中生物活性材料的固体颗粒分散并包封在包封的连续固相中材料，其中每个生物活性材料和包封材料在室温下通常为固体，并且包封材料的熔点低于生物活性材料的熔点，生物活性材料优选为双膦酸盐，最优选阿仑膦酸盐，并且包封材料包括增强剂，优选单甘油酯或甘油二酯或包封表面活性剂，优选具有表面活性的聚氧乙烯/聚氧丙烯嵌段共聚物，以及制备其中生物活性物质的固体颗粒为混合并分散在胶囊中处于熔融（液体）形式的材料; 并且冷却包封材料的熔融形式以形成固体药物组合物，其具有将生物活性材料的固体颗粒分散并包封在封装材料的连续固相中。

3. 发明授权

US07687515B2 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives 失效
标题翻译： 6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物
公开(公告)号：US07687515B2
公开(公告)日：2010-03-30
申请号：US11653600
申请日：2007-01-16
申请人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Iain Cumming , Jonathan Gillespie
发明人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Iain Cumming , Jonathan Gillespie
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途，如神经性疼痛。

4. 发明申请

US20090297619A1 NANOPARTICULATE ANTICONVULSANT AND IMMUNOSUPPRESSIVE COMPOSITIONS 审中-公开
标题翻译：纳米抗性和免疫抑制组合物
公开(公告)号：US20090297619A1
公开(公告)日：2009-12-03
申请号：US12483188
申请日：2009-06-11
申请人： Jon Swanson , Rajeev A. Jain , Robert Hontz , John G. Devane , Kenneth Iain Cumming , Maurice Joseph Anthony Clancy , Janet Elizabeth Codd , Gary G. Liversidge
发明人： Jon Swanson , Rajeev A. Jain , Robert Hontz , John G. Devane , Kenneth Iain Cumming , Maurice Joseph Anthony Clancy , Janet Elizabeth Codd , Gary G. Liversidge
IPC分类号： A61K9/14 , A61P37/02 , A61K31/55 , A61K31/5513 , A61K31/5517 , A61K31/53 , A61K31/519 , A61K31/135 , A61K31/437 , A61K31/4164 , A61K38/13 , A61K31/52 , A61K31/573
CPC分类号： A61K9/2077 , A61K9/146 , A61K9/2054
摘要： Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.
摘要翻译：描述了包含要施用的纳米颗粒剂的控释纳米颗粒制剂和用于在施用后延长试剂释放的速率控制聚合物。该新型组合物在施用后释放约2至约24小时或更长时间的时间。

5. 发明申请

US20070179138A1 6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives 失效
标题翻译： 6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物
公开(公告)号：US20070179138A1
公开(公告)日：2007-08-02
申请号：US11653600
申请日：2007-01-16
申请人： Jiaqiang Cai , Zoran Rankovic , Philip Jones , David Bennett , Iain Cumming , Jonathan Gillespie
发明人： Jiaqiang Cai , Zoran Rankovic , Philip Jones , David Bennett , Iain Cumming , Jonathan Gillespie
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途，如神经性疼痛。

6. 发明授权

US6153220A Taste-masked formulations 失效
标题翻译：口味掩饰的配方
公开(公告)号：US6153220A
公开(公告)日：2000-11-28
申请号：US163731
申请日：1998-09-30
申请人： Kenneth Iain Cumming , Elaine Harris
发明人： Kenneth Iain Cumming , Elaine Harris
IPC分类号： A61K9/10 , A61K9/14 , A61K9/16 , A61K9/20 , A61K9/44 , A61K9/46 , A61K31/426 , A61K31/4453 , A61K31/557 , A61K38/00 , A61K38/22 , A61K45/00 , A61K47/32 , A61P1/08 , A61P7/02 , A61P7/10 , A61P9/00 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/20 , A61P31/04 , A61P35/00 , A61P43/00 , A61K9/22
CPC分类号： A61K9/1652 , A61K9/1635 , A61K9/2081 , Y10S514/937 , Y10S514/974
摘要： A taste-masked micromatrix powder in which the ratio of a cationic copolymer synthesized form dimethylaminoethyl methacrylate and neutral methacrylic acid esters compared to a drug having poor organoleptic properties is greater than 2 to 1, preferably 4 to 1, most preferably 6 to 1 (wt/wt). Taste masked immediate release micromatrix powders can be formed by spray drying the drug and cationic copolymer whereas sustained release micromatrix powders can be formed by granulating controlled release powders, which can be made by spray drying the drug with a retarding polymer, with the cationic copolymer. The immediate release or sustained release taste-masked powders of this invention can be incorporated into conventional oral dosage forms such as sprinkles, suspension, fast melt tablets, chewable tablets or effervescent tablets.
摘要翻译：合成的甲基丙烯酸二甲基氨基乙酯和中性甲基丙烯酸酯的阳离子共聚物与具有不良感官特性的药物相比的比例大于2比1，优选4比1，最优选6比1（重量比）的掩味微米矩阵粉末 / wt）。可以通过喷雾干燥药物和阳离子共聚物来形成口味掩蔽的立即释放微阵列粉末，而通过使用阳离子共聚物通过用延迟聚合物喷雾干燥药物来制备控释粉末，可以形成持续释放微阵列粉末。本发明的立即释放或持续释放的掩味粉末可以掺入常规的口服剂型如洒剂，悬浮液，快速熔融片剂，咀嚼片剂或泡腾片剂中。

7. 发明申请

US20130011447A1 CONTROLLED RELEASE NANOPARTICULATE COMPOSITIONS 审中-公开
标题翻译：控制释放纳米颗粒组合物
公开(公告)号：US20130011447A1
公开(公告)日：2013-01-10
申请号：US13620570
申请日：2012-09-14
申请人： Jon Swanson , Rajeev A. Jain , Robert Hontz , John G. Devane , Kenneth Iain Cumming , Maurice Joseph Anthony Clancy , Janet Elizabeth Codd , Gary G. Liversidge
发明人： Jon Swanson , Rajeev A. Jain , Robert Hontz , John G. Devane , Kenneth Iain Cumming , Maurice Joseph Anthony Clancy , Janet Elizabeth Codd , Gary G. Liversidge
IPC分类号： A61K9/14 , B82Y5/00
CPC分类号： A61K9/146 , A61K9/2054 , A61K9/2077
摘要： Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.
摘要翻译：描述了包含要施用的纳米颗粒剂的控释纳米颗粒制剂和用于在施用后延长试剂释放的速率控制聚合物。该新型组合物在施用后释放约2至约24小时或更长时间的时间。

8. 发明申请

US20120114754A1 RAPIDLY DISINTEGRATING SOLID ORAL DOSAGE FORM 审中-公开
标题翻译：快速消毒固体口服剂型
公开(公告)号：US20120114754A1
公开(公告)日：2012-05-10
申请号：US13291873
申请日：2011-11-08
申请人： Rajeev A. Jain , Stephen B. RUDDY , Kenneth Iain CUMMING , Maurice Joseph Anthony CLANCY , Janet Elizabeth CODD
发明人： Rajeev A. Jain , Stephen B. RUDDY , Kenneth Iain CUMMING , Maurice Joseph Anthony CLANCY , Janet Elizabeth CODD
IPC分类号： A61K9/14 , A61K31/4422 , A61P29/00 , A61K31/192 , A61K31/4965 , B82Y40/00 , B82Y5/00
CPC分类号： A61K9/5161 , A61K9/0056 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K9/2081 , A61K9/5192
摘要： Disclosed is a rapidly disintegrating solid oral dosage form of a poorly soluble active ingredient and at least one pharmaceutically acceptable water-soluble or water-dispersible excipient, wherein the poorly soluble active ingredient particles have an average diameter, prior to inclusion in the dosage form, of less than about 2000 nm. The dosage form of the invention has the advantage of combining rapid presentation and rapid dissolution of the active ingredient in the oral cavity.
摘要翻译：公开了一种快速崩解的难溶性活性成分和至少一种药学上可接受的水溶性或水分散性赋形剂的固体口服剂型，其中所述难溶性活性成分颗粒在包含在剂型之前具有平均直径，小于约2000nm。本发明的剂型具有将活性成分快速呈现和快速溶解在口腔中的优点。

9. 发明授权

US08119159B2 Solid oral dosage form containing an enhancer 有权
标题翻译：含有增强剂的固体口服剂型
公开(公告)号：US08119159B2
公开(公告)日：2012-02-21
申请号：US11400689
申请日：2006-04-07
申请人： Kenneth Iain Cumming , Zebunissa Ramtoola , Thomas Waymond Leonard
发明人： Kenneth Iain Cumming , Zebunissa Ramtoola , Thomas Waymond Leonard
IPC分类号： A61K9/20
CPC分类号： A61K9/1617 , A61K9/2013 , A61K9/2054 , A61K9/2846 , A61K47/12
摘要： The invention relates to a pharmaceutical composition and oral dosage forms comprising a bisphosphonate in combination with an enhancer to promote absorption of the bisphosphonate at the GIT cell lining. The enhancer is a medium chain fatty acid or a medium chain fatty acid derivative having a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is a controlled release dosage form such as a delayed release dosage form.
摘要翻译：本发明涉及药物组合物和口服剂型，其包含与增强剂组合的双膦酸盐以促进GIT细胞内衬上双膦酸盐的吸收。增强剂是碳链长为6〜20个碳原子的中链脂肪酸或中链脂肪酸衍生物。优选地，固体口服剂型是控释剂型，例如延迟释放剂型。

10. 发明授权

US06399100B1 Controlled release pharmaceutical compositions containing tiagabine 失效
标题翻译：包含噻加滨的控释药物组合物
公开(公告)号：US06399100B1
公开(公告)日：2002-06-04
申请号：US09127210
申请日：1998-07-31
申请人： Maurice Joseph Anthony Clancy , Kenneth Iain Cumming , Michelle Caulfield
发明人： Maurice Joseph Anthony Clancy , Kenneth Iain Cumming , Michelle Caulfield
IPC分类号： A61K922
CPC分类号： A61K9/2031 , A61K9/2054 , A61K31/4535
摘要： Controlled release oral pharmaceutical preparations are provided which comprise a therapeutically effective amount of tiagabine or a pharmaceutically acceptable salt thereof dispersed in a rate controlling polymeric matrix comprising at least one rate controlling polymer. The preparation can be formulated into oral dosage forms such as tablets or multiparticulates which provide therapeutically effective plasma levels of tiagabine for a period of at least 12 hours, preferably 24 hours or more. The preparation can provide tiagabine mean plasma concentrations equal to or greater than 50% of the maximum plasma concentration for at least 10 hours, preferably 14 hours, most preferably 16 hours or more.
摘要翻译：提供了控制释放的口服药物制剂，其包含分散在包含至少一种速率控制聚合物的速率控制聚合物基质中的治疗有效量的噻加滨或其药学上可接受的盐。该制剂可以配制成口服剂型，例如片剂或多颗粒，其提供治疗有效的噻加滨的血浆水平至少12小时，优选24小时或更长时间。该制剂可以提供等于或大于最大血浆浓度的50％的替加滨平均血浆浓度至少10小时，优选14小时，最优选16小时或更长。

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