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1. 发明申请

US20120322835A1 PHARMACEUTICAL COMPOSITIONS AND METHODS FOR PRODUCING LOW IMPURITY CONCENTRATIONS OF THE SAME 审中-公开
标题翻译：药物组合物及其生产低劣化浓度的方法
公开(公告)号：US20120322835A1
公开(公告)日：2012-12-20
申请号：US13600056
申请日：2012-08-30
申请人： Rajeshwar Motheram , Gopal Krishna , Min Ding , Keith Flood , Kornepati Ramakrishna
发明人： Rajeshwar Motheram , Gopal Krishna , Min Ding , Keith Flood , Kornepati Ramakrishna
IPC分类号： A61K31/4418 , C07D213/80 , G01N30/00 , A61P9/12
CPC分类号： A61K31/4422 , A61K31/519 , G01N30/02
摘要： A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.
摘要翻译：描述了具有氯维地平作为活性成分的组合物。组合物包括氯维西肽作为活性成分，杂质H168 / 79的量不大于约1.5％，或者氯维地平与H168 / 79之间的比例等于或大于60比1。

2. 发明申请

US20100113534A1 Pharmaceutical Compositions And Methods For Producing Low Impurity Concentrations Of The Same 审中-公开
标题翻译：用于生产低杂质浓度的药物组合物和方法
公开(公告)号：US20100113534A1
公开(公告)日：2010-05-06
申请号：US12511631
申请日：2009-07-29
申请人： Rajeshwar Motheram , Gopal Krishna , Min Ding , Keith Flood , Kornepati Ramakrishna
发明人： Rajeshwar Motheram , Gopal Krishna , Min Ding , Keith Flood , Kornepati Ramakrishna
IPC分类号： A61K31/4418 , G01N30/02
CPC分类号： A61K31/4422 , A61K31/519 , G01N30/02
摘要： A composition having clevidipine as an active ingredient is described. The composition includes clevidipine as an active ingredient and an amount of the impurity H168/79 that is no greater than about 1.5%, or where the ratio between clevidipine and H168/79 is equal or above 60 to 1.
摘要翻译：描述了具有氯维地平作为活性成分的组合物。组合物包括氯维西肽作为活性成分，杂质H168 / 79的量不大于约1.5％，或者氯维地平与H168 / 79之间的比例等于或大于60比1。

3. 发明申请

US20120322836A1 PHARMACEUTICAL COMPOSITIONS AND METHODS FOR STABILIZING THE SAME 审中-公开
标题翻译：药物组合物及其稳定化方法
公开(公告)号：US20120322836A1
公开(公告)日：2012-12-20
申请号：US13600083
申请日：2012-08-30
申请人： Gopal Krishna , Rajeshwar Motheram , Min Ding
发明人： Gopal Krishna , Rajeshwar Motheram , Min Ding
IPC分类号： A61K31/4418 , A61P9/12 , C07D213/80
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/10 , A61K31/435 , A61K31/4418 , A61K2300/00
摘要： Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is described. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324/78 is minimized, such that the total detectable level of H324/78 in a given composition sample does not exceed about 0.2% on a weight-by-weight basis, or the ratio of clevidipine to H324/78 is equal to or greater than about 450 to 1 on a weight-to-weight basis.
摘要翻译：描述了药物组合物和稳定具有氯维地平的药物组合物或其任何药学上可接受的盐作为活性成分的方法。该方法包括减缓或抑制氯维地平的氧化途径。这可以通过在制造和储存过程中减少药物组合物暴露于氧和/或光的量来实现。根据该方法，必须除去或更换氧气，或者必须充分阻挡光，使得光能不能达到组合物的活性成分，或者降低到光诱导的氧化反应将氯维地平转化为H324 / 78 被最小化，使得给定组合物样品中H324 / 78的总可检测水平以重量计不超过约0.2％，或者氯维地平与H324 / 78的比例等于或大于约450 至1，以重量为基准。

4. 发明申请

US20100105743A1 Pharmaceutical compositions and methods for stabilizing the same 审中-公开
标题翻译：药物组合物及其稳定方法
公开(公告)号：US20100105743A1
公开(公告)日：2010-04-29
申请号：US12462147
申请日：2009-07-30
申请人： Gopal Krishna , Rajeshwar Motheram , Min Ding
发明人： Gopal Krishna , Rajeshwar Motheram , Min Ding
IPC分类号： A61K31/44 , A61P9/12
CPC分类号： A61K31/519 , A61K9/0019 , A61K9/10 , A61K31/435 , A61K31/4418 , A61K2300/00
摘要： Pharmaceutical compositions, and a method of stabilizing pharmaceutical compositions having clevidipine, or any pharmaceutically acceptable salt thereof, as the active ingredient is described. The method includes the slowing down or inhibiting of the oxidation pathway of clevidipine. This can be accomplished by reducing the amount the pharmaceutical composition is exposed to oxygen and/or light during the manufacturing and storing processes. According to this method, oxygen must be removed or replaced, or light must be sufficiently blocked such that light energy cannot reach the active ingredient of the composition, or is reduced to a level that the light-induced oxidation reaction converting clevidipine to H324/78 is minimized, such that the total detectable level of H324/78 in a given composition sample does not exceed about 0.2% on a weight-by-weight basis, or the ratio of clevidipine to H324/78 is equal to or greater than about 450 to 1 on a weight-to-weight basis.
摘要翻译：描述了药物组合物和稳定具有氯维地平的药物组合物或其任何药学上可接受的盐作为活性成分的方法。该方法包括减缓或抑制氯维地平的氧化途径。这可以通过在制造和储存过程中减少药物组合物暴露于氧和/或光的量来实现。根据该方法，必须除去或更换氧气，或者必须充分阻挡光，使得光能不能达到组合物的活性成分，或者降低到光诱导的氧化反应将氯维地平转化为H324 / 78 被最小化，使得给定组合物样品中H324 / 78的总可检测水平以重量计不超过约0.2％，或者氯维地平与H324 / 78的比例等于或大于约450 至1，以重量为基准。

5. 发明授权

US07803762B1 Ready-to-use bivalirudin compositions 有权
公开(公告)号：US07803762B1
公开(公告)日：2010-09-28
申请号：US12545036
申请日：2009-08-20
申请人： Nagesh Palepu , Rajeshwar Motheram , Praful Shah , Gopal Krishna
发明人： Nagesh Palepu , Rajeshwar Motheram , Praful Shah , Gopal Krishna
IPC分类号： A61K38/00
CPC分类号： A61K38/58
摘要： Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.

6. 发明授权

US07713928B1 Ready-to-use bivalirudin compositions 有权
标题翻译：即用型比伐卢定组合物
公开(公告)号：US07713928B1
公开(公告)日：2010-05-11
申请号：US12563821
申请日：2009-09-21
申请人： Nagesh Palepu , Rajeshwar Motheram , Praful Shah , Gopal Krishna
发明人： Nagesh Palepu , Rajeshwar Motheram , Praful Shah , Gopal Krishna
IPC分类号： A61K38/00
CPC分类号： A61K38/58
摘要： Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.
摘要翻译：即用比伐卢定组合物，使用即用比伐卢定组合物的方法，以及制备即用型比伐卢定组合物的方法。即用型比伐卢列组合物包含比伐卢定和一种或多种稳定剂。一种或多种稳定剂可以是pKa为约2.5至约6.5的缓冲剂，pH调节剂，聚合物，防腐剂，抗氧化剂，糖或多元醇或其组合。即用型比伐卢定组合物还可以包含[9-10] - 环亚氨基比伐卢定，[11-12] - 环亚氨基比伐卢定或其组合。使用即用比伐卢定组合物的方法包括将即用组合物给予有需要的组合物。此外，制备即用型比伐卢定组合物的方法包括将比伐卢定与一种或多种稳定剂混合。

7. 发明申请

US20120149770A1 Antimicrobial Preservation of Propofol Emulsions 失效
标题翻译：丙泊酚乳液的抗菌保存
公开(公告)号：US20120149770A1
公开(公告)日：2012-06-14
申请号：US13252667
申请日：2011-10-04
申请人： Min Ding , Rajeshwar Motheram , Glenn Sblendorio
发明人： Min Ding , Rajeshwar Motheram , Glenn Sblendorio
IPC分类号： A61K31/235 , A61K31/05
CPC分类号： A61K9/0019 , A61K9/107 , A61K31/045 , A61K31/05 , A61K31/33
摘要： The invention provides intravenous formulations of propofol in an oil-in-water emulsion, having a combination of preservatives.
摘要翻译：本发明提供具有防腐剂组合的水包油乳剂中的异丙酚的静脉内制剂。

8. 发明授权

US08754125B2 Antimicrobial preservation of propofol emulsions 失效
标题翻译：异丙酚乳剂的抗微生物保存
公开(公告)号：US08754125B2
公开(公告)日：2014-06-17
申请号：US13252667
申请日：2011-10-04
申请人： Min Ding , Rajeshwar Motheram , Glenn Sblendorio
发明人： Min Ding , Rajeshwar Motheram , Glenn Sblendorio
IPC分类号： A61K31/235 , A61K31/05
CPC分类号： A61K9/0019 , A61K9/107 , A61K31/045 , A61K31/05 , A61K31/33
摘要： The invention provides intravenous formulations of propofol in an oil-in-water emulsion, having a combination of preservatives.
摘要翻译：本发明提供具有防腐剂组合的水包油乳剂中的异丙酚的静脉内制剂。

9. 发明申请

US20080275009A1 ORAL ADMINISTRATION OF N-(2-CHLORO-6-METHYLPHENYL)-2-[[6-[4-(2-HYDROXYETHYL)-1-PIPERAZINYL]-2-METHYL-4-PYRIMIDINYL]AMINO]-1,3-THIAZOLE-5-CARBOXAMIDE AND SALTS THEREOF 审中-公开
标题翻译： N-（2-氯代-6-甲基苯基）-2 - [[6- [4-（2-羟基乙基）-1-哌嗪基] -2-甲基-4-吡啶基]氨基] 噻唑-5-羧酰胺及其盐
公开(公告)号：US20080275009A1
公开(公告)日：2008-11-06
申请号：US12168366
申请日：2008-07-07
申请人： Ramakrishnan Chidambaram , George M. Derbin , Masaki Endo , Julia ZH Gao , Tu Lee , Rajeshwar Motheram , William Lawrence Parker , Victor W. Rosso , Sailesh A. Varia
发明人： Ramakrishnan Chidambaram , George M. Derbin , Masaki Endo , Julia ZH Gao , Tu Lee , Rajeshwar Motheram , William Lawrence Parker , Victor W. Rosso , Sailesh A. Varia
IPC分类号： A61K31/60 , A61K31/506 , A61P35/00 , C07D403/14
CPC分类号： C07D417/12 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： Disclosed are a method of treating cancer and/or other proliferative diseases comprising orally administering N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof, and pharmaceutical compositions comprising N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof. Also disclosed are N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide salts, as well as crystalline forms thereof.
摘要翻译：公开了一种治疗癌症和/或其它增殖性疾病的方法，其包括口服给予N-（2-氯-6-甲基苯基）-2 - （（6-（4-（2-羟乙基）-1-哌嗪基）-2- 甲基-4-嘧啶基）氨基）-1,3-噻唑-5-甲酰胺或其盐，以及包含N-（2-氯-6-甲基苯基）-2 - （（6-（4-（2 - 羟基乙基）-1-哌嗪基）-2-甲基-4-嘧啶基）氨基）-1,3-噻唑-5-甲酰胺或其盐。还公开了N-（2-氯-6-甲基苯基）-2 - （（6-（4-（2-羟乙基）-1-哌嗪基）-2-甲基-4-嘧啶基）氨基）噻唑-5-甲酰胺盐，以及其结晶形式。

10. 发明授权

US6100302A Propofol formulation with enhanced microbial characteristics 失效
标题翻译：丙泊酚配方具有增强的微生物特性
公开(公告)号：US6100302A
公开(公告)日：2000-08-08
申请号：US286159
申请日：1999-04-05
申请人： Satish K. Pejaver , Rajeshwar Motheram , Barrett E. Rabinow , Josben C. dela Rosa
发明人： Satish K. Pejaver , Rajeshwar Motheram , Barrett E. Rabinow , Josben C. dela Rosa
IPC分类号： A61K9/107 , A61K31/05 , A61K47/10 , A61K47/24 , A61K47/44 , A61K47/46 , A61P23/00
CPC分类号： A61K31/05 , A61K9/1075 , Y10S514/816 , Y10S514/938
摘要： Formulations of intravenous anesthetic propofol emulsions are provided which contain sufficiently low concentrations of soybean oil to produce a stable emulsion and simultaneously provide reduced nutrients, which inhibit microbial growth thereby providing protection against accidental microbial contamination during long-term IV infusions. In addition to the inhibition of microbial growth due to a reduction of nutrients, the formulation exhibits unanticipated additional microbial inhibition due to an increased availability of propofol. The low concentration of soybean oil also provides a formulation that reduces the chances of fat overload when administered over an extended period of time to chronically ill patients.
摘要翻译：提供静脉麻醉丙泊酚乳剂的制剂，其含有足够低浓度的大豆油以产生稳定的乳液，同时提供减少的营养物质，其抑制微生物生长，从而在长期IV输注期间提供防止意外的微生物污染的保护。除了由于营养物质的减少而抑制微生物生长之外，由于异丙酚的可用性的增加，该制剂表现出意外的另外的微生物抑制。低浓度的大豆油也提供了一种配方，可以在延长的时间内长期服用长期患者时，减少脂肪过量的机会。

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