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公开(公告)号：US20170101377A1
公开(公告)日：2017-04-13
申请号：US15365566
申请日：2016-11-30
发明人： Martin HANBAUER , Zarghun NAZIR , Peter HILDEBRAND , Attilia FIGINI , Likan LIANG , Tiziano FUMAGALLI
IPC分类号： C07D209/08 , C07D295/13
CPC分类号： C07D209/08 , C07D295/13
摘要： The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
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公开(公告)号：US09555004B2
公开(公告)日：2017-01-31
申请号：US14630099
申请日：2015-02-24
发明人： Likan Liang , Hua Wang , Padmanabh P. Bhatt , Michael L. Vieira
IPC分类号： A61K9/16 , A61K9/50 , A61K9/24 , A61K31/357 , A61K47/48 , B82Y5/00 , A61K31/7048
CPC分类号： A61K9/5042 , A61K9/1652 , A61K9/1676 , A61K9/209 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/357 , A61K31/7048 , A61K45/06 , A61K47/48969 , A61K47/6951 , B82Y5/00 , Y02A50/465
摘要： Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.
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公开(公告)号：US20160304475A1
公开(公告)日：2016-10-20
申请号：US15192098
申请日：2016-06-24
发明人： Likan LIANG , Padmanabh P. BHATT , David DAIN , Jean-Philippe TAQUET , Aleksandr PECHENOV , Alexei TCHESNOKOV , Reynold MARIAUX
IPC分类号： C07D265/30
CPC分类号： C07D265/30 , C07C215/08 , C07C217/34 , C07D265/32
摘要： Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
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公开(公告)号：US09393203B2
公开(公告)日：2016-07-19
申请号：US14881374
申请日：2015-10-13
发明人： Argaw Kidane , Padmanabh P Bhatt
IPC分类号： A61K9/24 , A61K9/20 , A61K9/00 , A61K9/16 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61K9/28 , A61K31/192
CPC分类号： A61K9/282 , A61K9/0004 , A61K9/1623 , A61K9/1652 , A61K9/2013 , A61K9/2077 , A61K9/28 , A61K9/2826 , A61K9/286 , A61K31/192 , A61K31/557 , A61K31/5575 , A61K31/5585
摘要： An oral osmotic pharmaceutical delivery system comprises a highly water-soluble drug exhibiting an erratic or an incomplete release profile when formulated in an elementary osmotic pump delivery system and at least one release enhancing agent.
摘要翻译： 口服渗透药物递送系统包含当配制在基本渗透泵递送系统和至少一种释放增强剂中时表现出不稳定或不完全释放特征的高度水溶性药物。
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公开(公告)号：US09370525B2
公开(公告)日：2016-06-21
申请号：US14807165
申请日：2015-07-23
发明人： Padmanabh P. Bhatt , Argaw Kidane , Kevin Edwards
CPC分类号： A61K31/55 , A61K9/0073 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K2800/56
摘要： Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
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公开(公告)号：US20160022596A1
公开(公告)日：2016-01-28
申请号：US14630099
申请日：2015-02-24
发明人： Likan Liang , Hua WANG , Padmanabh P. BHATT , Michael L. VIEIRA
IPC分类号： A61K9/50 , A61K31/7048
CPC分类号： A61K9/5042 , A61K9/1652 , A61K9/1676 , A61K9/209 , A61K9/5047 , A61K9/5078 , A61K9/5084 , A61K31/357 , A61K31/7048 , A61K45/06 , A61K47/48969 , A61K47/6951 , B82Y5/00 , Y02A50/465
摘要： Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.
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公开(公告)号：US09144551B2
公开(公告)日：2015-09-29
申请号：US14563089
申请日：2014-12-08
IPC分类号： A61K9/14 , A61K9/20 , A61K9/28 , A61K9/50 , A61K9/70 , A61K31/00 , A61K31/137 , A61K31/485 , A61K31/5513 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/34 , A61K47/38
CPC分类号： A61K9/2886 , A61K9/14 , A61K9/2013 , A61K9/2018 , A61K9/205 , A61K9/2846 , A61K9/2853 , A61K9/5078 , A61K9/5084 , A61K9/7061 , A61K9/7069 , A61K31/00 , A61K31/137 , A61K31/485 , A61K31/5513 , A61K47/186 , A61K47/22 , A61K47/26 , A61K47/34 , A61K47/38
摘要： Drug formulations having reduced abuse potential which contain one or more of (1) a bittering agent, (2) a bright deterrent/indicator dye and (3) fine insoluble particulate matter. The bittering agent and dye are in a form which does not affect proper administration of the drug, but the bittering agent creates a bitter side effect when the dosage form is crushed or chemically extracted and nasally, orally, buccally or sublingually administered and the dye produces a bright color when crushed and contacted. The fine insoluble particulate matter hinders extraction of the drug from the dosage form and, when crushed, can deter intravenous injection because of the presence of the insoluble particles or hinder injection by blocking an intravenous needle. The bright color of the dye, when extracted, also has a psychologically deterrent effect on intravenous abusers.
摘要翻译： 药物制剂具有降低的滥用潜力，其含有（1）苦味剂，（2）明亮的威慑/指示剂染料和（3）细小的不溶性颗粒物质中的一种或多种。 苦味剂和染料是不影响药物正确给药的形式，但当剂型粉碎或化学提取并经鼻，口服，口腔或舌下给药时，苦味剂会产生苦味副作用，染料产生 粉碎并接触时，颜色鲜艳。 细小的不溶性颗粒物质妨碍药物从剂型中的提取，当被粉碎时，由于存在不溶性颗粒或通过阻塞静脉内针阻止注射，可以阻止静脉内注射。 染色剂的鲜艳色彩在提取时也对静脉滥用药物有心理上的威慑作用。
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公开(公告)号：US20150086629A1
公开(公告)日：2015-03-26
申请号：US14261709
申请日：2014-04-25
发明人： Rong-Kun Chang , Michael L. Vieira , Likan LIANG , Padmanabh P. BHATT , Austin B. HUANG , Sachin V. PATEL
IPC分类号： A61K31/5377 , A61K9/16
CPC分类号： A61K31/5377 , A61K9/0004 , A61K9/16 , A61K9/1623 , A61K9/1635 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2072 , A61K9/209 , A61K9/2866 , A61K9/2886 , A61K9/4808 , A61K9/4858 , A61K9/4866
摘要： Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.
摘要翻译： 提供了具有优异稳定性的摩霉素制剂及其施用方法。 制剂可以是莫立多内的即时，改性或其它延迟释放制剂。
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公开(公告)号：US20140303252A1
公开(公告)日：2014-10-09
申请号：US14265630
申请日：2014-04-30
发明人： Argaw Kidane , Padmanabh P. Bhatt
IPC分类号： A61K9/20 , A61K31/557
CPC分类号： A61K9/282 , A61K9/0004 , A61K9/1623 , A61K9/1652 , A61K9/2013 , A61K9/2077 , A61K9/28 , A61K9/2826 , A61K9/286 , A61K31/192 , A61K31/557 , A61K31/5575 , A61K31/5585
摘要： An oral osmotic pharmaceutical delivery system comprises a highly water-soluble drug exhibiting an erratic or an incomplete release profile when formulated in a elementary osmotic pump delivery system and at least one release enhancing agent.
摘要翻译： 口服渗透药物递送系统包含当配制在基本渗透泵输送系统和至少一种释放增强剂中时表现出不稳定或不完全释放特征的高度水溶性药物。
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20.发明授权公开(公告)号：US08821930B2
公开(公告)日：2014-09-02
申请号：US14103103
申请日：2013-12-11
发明人： Padmanabh P. Bhatt , Argaw Kidane , Kevin Edwards
CPC分类号： A61K31/55 , A61K9/0073 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/205 , A61K9/2054 , A61K2800/56
摘要： Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
摘要翻译： 公开了奥卡西平及其衍生物的一日一次给药的控制释放制剂。 本发明的组合物包含溶解度和/或释放增强剂，以提供定制的药物释放曲线，优选S形释放曲线。 还公开了包含本发明组合物的治疗方法。
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