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1. 发明申请

WO2004021972A3 PHARMACEUTICALS FORMULATIONS AND METHODS FOR MODIFIED RELEASE OF STATIN DRUGS 审中-公开
标题翻译：药物制剂及其改性释放方法
公开(公告)号：WO2004021972A3
公开(公告)日：2004-08-12
申请号：PCT/IB0304361
申请日：2003-09-03
申请人： BIOVAIL LAB INC , BUTLER JACKIE , DEVANE JOHN , STARK PAUL
发明人： BUTLER JACKIE , DEVANE JOHN , STARK PAUL
IPC分类号： A61K9/20 , A61K9/28 , A61K31/225 , A61K31/35 , A61K31/366 , A61K31/401 , A61K45/06
CPC分类号： A61K31/401 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/284 , A61K9/2846 , A61K31/225 , A61K31/366 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to compositions and methods of their use in treating, preventing, and/or managing one or more cardiovascular diseases using at least one poorly water-soluble statin, such as, for example, simvastatin and/or lovastatin. One method of the invention involves delaying release of the poorly water-soluble statin for a time sufficient to avoid metabolism of the statin at or near the gastrointestinal tract wall by the cytochrome P450 3A metabolic system, and releasing said statin in the ileum, colon, or both, with subsequent uptake into the hepatic portal vein and distribution to hepatocytes, wherein HMG-CoA reductase activity may be inhibited with minimal adverse drug interactions.
摘要翻译：本发明涉及其用于治疗，预防和/或控制使用至少一种难溶于水的他汀类药物（例如辛伐他汀和/或洛伐他汀）的一种或多种心血管疾病的组合物和方法。本发明的一种方法包括延迟释放水溶性差的他汀类药物足够的时间，以避免细胞色素P450 3A代谢系统在胃肠道壁上或其附近抑制他汀类药物的代谢，并在回肠，结肠，或两者，随后摄入肝门静脉并分布到肝细胞，其中HMG-CoA还原酶活性可以以最小的不良药物相互作用被抑制。

2. 发明申请

WO2004014849A2 ISOSORBIDE MONONITRATE COMPOSITIONS AND METHODS OF THEIR USE 审中-公开
标题翻译：异硫氰酸酯单体化合物及其使用方法
公开(公告)号：WO2004014849A2
公开(公告)日：2004-02-19
申请号：PCT/IB0304245
申请日：2003-08-08
申请人： BIOVAIL LAB INC , DEVANE JOHN , STARK PAUL , KELLY JOHN , BUTLER JACKIE
发明人： DEVANE JOHN , STARK PAUL , KELLY JOHN , BUTLER JACKIE
IPC分类号： C07D493/04 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/32 , A61K9/50 , A61K9/58 , A61K31/34 , A61K47/12 , A61K47/20 , A61K47/32 , A61K47/34 , A61K47/38 , A61P9/04 , A61P9/10 , C07D
CPC分类号： A61K9/5078 , A61K9/2054 , A61K9/2846 , A61K9/5026 , A61K9/5047 , A61K31/34
摘要： The present invention relates to delayed onset, extended release formulations of isosorbide mononitrates (ISMNs), and methods of their use in treating, preventing, reducing, reversing, and/or managing nitrate tolerance and/or cardiovascular conditions. In particular, the present invention is directed to once-daily delayed onset, extended release formulations that (1) provide a subject with a therapeutically effective amount of ISMNs during the early morning hours prior to and after awakening, (2) continue to provide therapeutically effective amounts of ISMN throughout the waking hours of the day, and (3) provide a reduction, or washout, of ISMN plasma levels to treat, prevent, reduce, reverse, and/or manage nitrate tolerance.
摘要翻译：本发明涉及异山梨醇单硝酸盐（ISMN）的延迟开始，延长释放制剂及其用于治疗，预防，减少，逆转和/或控制硝酸盐耐受性和/或心血管疾病的方法。特别地，本发明涉及每日一次延迟发作的延长释放制剂，其（1）在醒来之前和之后的清晨时间向受试者提供治疗有效量的ISMNs，（2）继续提供治疗在一天的醒来时间内有效量的ISMN，以及（3）提供ISMN血浆水平的减少或清除以治疗，预防，减少，逆转和/或控制硝酸盐耐受性。

3. 发明申请

WO2004021973A3 PRAVASTATIN PHARMACEUTICAL FORMULATIONS AND METHODS OF THEIR USE 审中-公开
标题翻译： PRAVASTATIN药物制剂及其使用方法
公开(公告)号：WO2004021973A3
公开(公告)日：2004-05-21
申请号：PCT/IB0304523
申请日：2003-09-03
申请人： BIOVAIL LAB INC , DEVANE JOHN , BUTLER JACKIE , STARK PAUL
发明人： DEVANE JOHN , BUTLER JACKIE , STARK PAUL
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K31/22 , A61K31/225 , A61P3/10 , A61P9/00
CPC分类号： A61K9/2846 , A61K9/2018 , A61K9/2054 , A61K9/284 , A61K9/2886 , A61K31/22 , A61K31/225
摘要： The present invention relates to formulations comprising a therapeutically effective amount of pravastatin, or a pharmaceutically acceptable salt thereof. The present formulations are designed to prevent inactivation of pravastatin in the stomach, limit systemic exposure of the body to pravastatin, and maximize hepatic-. specific absorption of the drug. The formulations of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.
摘要翻译：本发明涉及包含治疗有效量的普伐他汀或其药学上可接受的盐的制剂。本发明的制剂设计用于防止普伐他汀在胃中失活，限制身体全身暴露于普伐他汀，并使肝脏最大化。药物的特定吸收。本发明的制剂特别适用于治疗和/或预防由于体内脂质和/或胆固醇水平降低而受益的病症。

4. 发明申请

WO2005020954A2 PROTON PUMP INHIBITOR FORMULATIONS, AND METHODS OF PREPARING AND USING SUCH FORMULATIONS 审中-公开
标题翻译：质子泵抑制剂制剂，以及制备和使用这种制剂的方法
公开(公告)号：WO2005020954A2
公开(公告)日：2005-03-10
申请号：PCT/EP2004009806
申请日：2004-09-02
申请人： AGI THERAPEUTICS LTD , DEVANE JOHN , BUTLER JACKIE , STARK PAUL
发明人： DEVANE JOHN , BUTLER JACKIE , STARK PAUL
IPC分类号： A61K9/16 , A61K9/20 , A61K9/22 , A61K9/28 , A61K9/50 , A61K9/54 , A61K31/4439 , A61K9/00
CPC分类号： A61K9/2886 , A61K9/1676 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/2077 , A61K9/284 , A61K9/2866 , A61K9/5078
摘要： Pharmaceutical formulation comprising at least one proton pump inhibitor structured and arranged to provide an initial pH independent time-based delayed-release, and a subsequent extended-release of the at least one proton pump inhibitor.
摘要翻译：包含至少一种质子泵抑制剂的药物制剂，所述质子泵抑制剂被构造和布置成提供初始pH独立的基于时间的延迟释放和随后的所述至少一种质子泵抑制剂的延长释放。

5. 发明申请

WO2005021009A2 FORMULATIONS AND METHODS OF TREATING INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译：治疗炎症性皮肤病的制剂和方法
公开(公告)号：WO2005021009A2
公开(公告)日：2005-03-10
申请号：PCT/IB2004003059
申请日：2004-09-02
申请人： AGI THERAPEUTICS LTD , DEVANE JOHN , BUTLER JACKIE
发明人： DEVANE JOHN , BUTLER JACKIE
IPC分类号： A61K9/20 , A61K9/28 , A61K9/50 , A61K31/606 , A61K31/655 , A61P1/06 , C07C245/08
CPC分类号： A61K9/2059 , A61K9/2054 , A61K9/284 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/5078 , A61K31/606 , A61K31/655 , C07C245/08
摘要： Methods and formulations for treating inflammatory bowel disease are disclosed. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of 4aminosalicylic acid and/or 5-aminosalicylic acid to affected areas of the intestine. The methods and formulations comprise modified-release elements, providing for drug delivery to the affected or desired area. Diseases and conditions treatable with the present invention include Crohn's disease and ulcerative colitis.
摘要翻译：公开了治疗炎症性肠病的方法和制剂。所述方法和制剂包括但不限于用于将有效浓度的四氨基水杨酸和/或5-氨基水杨酸递送至肠的受影响区域的方法和制剂。方法和制剂包含修饰释放元件，提供药物递送到受影响的或期望的区域。可用本发明治疗的疾病和病症包括克罗恩病和溃疡性结肠炎。

6. 发明申请

WO2007119177A3 MODIFIED RELEASE FORMULATIONS AND METHODS OF TREATING INFLAMMATORY BOWEL DISEASE 审中-公开
标题翻译：改良释放配方及治疗炎症性皮肤病的方法
公开(公告)号：WO2007119177A3
公开(公告)日：2008-06-26
申请号：PCT/IB2007002029
申请日：2007-03-07
申请人： AGI THERAPEUTICS RES LTD , DEVANE JOHN , BUTLER JACKIE
发明人： DEVANE JOHN , BUTLER JACKIE
IPC分类号： A61K9/20 , A61K31/606 , A61K31/655 , C07C245/08
CPC分类号： A61K9/2054 , A61K9/2031 , A61K31/60 , A61K31/606 , A61K31/655 , C07C245/08 , C07C251/84
摘要： Methods and formulations for treating inflammatory bowel disease are disclosed. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of 4-aminosalicylic acid and/or 5-aminosalicylic acid, and pharmaceutically acceptable salts and pro-drugs thereof, to affected areas of the intestine, i.e., distal gut. The methods and formulations comprise modified-release elements, providing for drug delivery to the affected or desired area. Diseases and conditions treatable with the present invention include Crohn's disease and ulcerative colitis.
摘要翻译：公开了治疗炎症性肠病的方法和制剂。方法和制剂包括但不限于用于将有效浓度的4-氨基水杨酸和/或5-氨基水杨酸及其药学上可接受的盐和前药递送到受影响的肠的区域的方法和制剂，即，远端肠道方法和制剂包含修饰释放元件，提供药物递送到受影响的或期望的区域。可用本发明治疗的疾病和病症包括克罗恩病和溃疡性结肠炎。

7. 发明申请

WO2004034959A3 MULTIPARTICULATE MODIFIED RELEASE COMPOSITION COMPRISING BERAPROST 审中-公开
标题翻译：包含BERAPROST的多重改性释放组合物
公开(公告)号：WO2004034959A3
公开(公告)日：2004-07-29
申请号：PCT/IB0306415
申请日：2003-09-18
申请人： ELAN CORP PLC , STARK PAUL , JEARY THERESA , PALMER FIONA , BUTLER JACKIE , CODD JANET
发明人： STARK PAUL , JEARY THERESA , PALMER FIONA , BUTLER JACKIE , CODD JANET
IPC分类号： A61K9/16 , A61K9/20 , A61K9/26 , A61K9/28 , A61K9/48 , A61K9/50 , A61K9/54 , A61K31/343 , A61P9/00
CPC分类号： A61K31/343 , A61K9/1676 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/2846 , A61K9/4808 , A61K9/5026 , A61K9/5078 , A61K9/5084
摘要： A formulation which is capable of being taken orally for the delivery of beraprost sodium and which comprises the following components, each of which includes the beraprost sodium: (A) an instant-release (IR) component which releases substantially all of the beraprost sodium thereof in the stomach within about 15 minutes after ingestion; (B) a sustained-release (SR) component which has associated therewith a material that is effective in controlling the release of beraprost sodium in the body over a period of time of about 6 hours after ingestion; and (C) a delayedrelease (DR) component which includes: (i) a sub-component which has associated therewith a material that is effective in controlling the release of beraprost sodium in the body in a period of time of about 6 to about 12 hours after ingestion; and (ii) another sub-component which has associated therewith a material that is effective in controlling the release of beraprost sodium in the body in a period of time of about 12 to about 18 hours after ingestion, and the use of the formulation in therapeutically effective amounts to treat various types of conditions, for example, peripheral vascular disease, thrombosis, pulmonary ischemia, pulmonary hypertension, diabetes, and neuropathy.
摘要翻译：能够口服用于输送贝前列素钠的制剂，其包含以下组分，每种组分包括贝前列素钠：（A）释放基本上所有的贝前列素钠的即释型（IR）组分摄入后约15分钟内胃; （B）持续释放（SR）成分，其具有与摄入后约6小时的时间段内有效控制体内贝前列素钠释放的材料; （C）延迟释放（DR）组分，其包括：（i）具有与其相关联的材料的子组分，所述材料在约6至约12的时间段内有效控制贝前列素钠在体内的释放摄入后几小时; 和（ii）与摄入后约12至约18小时的时间相关联的具有有效控制贝前列素钠在体内释放的材料的另一子组分，以及该制剂在治疗上的用途有效量治疗各种类型的病症，例如外周血管疾病，血栓形成，肺部缺血，肺动脉高压，糖尿病和神经病变。

8. 发明专利

NO20050933A 未知
公开(公告)号：NO20050933A
公开(公告)日：2005-04-18
申请号：NO20050933
申请日：2005-02-21
申请人： BIOVAIL LAB INC
发明人： DEVANE JOHN G , BUTLER JACKIE , STARK PAUL
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K31/22 , A61K31/225 , A61P3/10 , A61P9/00
CPC分类号： A61K9/2846 , A61K9/2018 , A61K9/2054 , A61K9/284 , A61K9/2886 , A61K31/22 , A61K31/225

9. 发明专利

CA2497896A1 PRAVASTATIN PHARMACEUTICAL FORMULATIONS AND METHODS OF THEIRUSE 未知
公开(公告)号：CA2497896A1
公开(公告)日：2004-03-18
申请号：CA2497896
申请日：2003-09-03
申请人： BIOVAIL LAB INC
发明人： DEVANE JOHN , STARK PAUL , BUTLER JACKIE
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K31/22 , A61K31/225 , A61P3/10 , A61P9/00
摘要： The present invention relates to formulations comprising a therapeutically effective amount of pravastatin, or a pharmaceutically acceptable salt thereof. The present formulations are designed to prevent inactivation of pravastatin in the stomach, limit systemic exposure of the body to pravastatin, and maximize hepatic-. specific absorption of the drug. The formulations of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipi ds and/or cholesterol in the body.

10. 发明专利

PL375712A1 PRAVASTATIN PHARMACEUTICAL FORMULATIONS AND METHODS OF THEIR USE 未知
公开(公告)号：PL375712A1
公开(公告)日：2005-12-12
申请号：PL37571203
申请日：2003-09-03
申请人： BIOVAIL LAB INC
发明人： DEVANE JOHN , BUTLER JACKIE , STARK PAUL
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K31/22 , A61K31/225 , A61P3/10 , A61P9/00
摘要： The present invention relates to formulations comprising a therapeutically effective amount of pravastatin, or a pharmaceutially acceptable salt thereof The present formulations are designed to prevent inactivation of pravastatin in the stomach, limit systemic exposure of the body to pravastatin, and maximize hepatic-specific absorption of the drug. The formulations of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.

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