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1. 发明申请

US20120022032A1 CORTICOSTEROID COMPOSITIONS AND METHODS OF TREATMENTS THEREOF 审中-公开
标题翻译：角质形成组合物及其治疗方法
公开(公告)号：US20120022032A1
公开(公告)日：2012-01-26
申请号：US13123670
申请日：2009-10-08
申请人： Jiansheng Wan , David Monteith , Pranav Gupta , Samir Anupam Shah , Robert L. Berger , Joel Sequeira
发明人： Jiansheng Wan , David Monteith , Pranav Gupta , Samir Anupam Shah , Robert L. Berger , Joel Sequeira
IPC分类号： A61K31/58 , A61P11/06 , A61P11/00
CPC分类号： A61K9/0043 , A61K9/0078 , A61K9/008 , A61K9/1075 , A61K31/58 , A61K47/6951 , B82Y5/00
摘要： This invention relates to steroidal solutions for the preparation of medicaments and drug products useful for treating diseases of the upper and lower airway passages. Various embodiments of the present invention provide compositions, compositions and dosage forms with mometasone furoate in a dissolved state that are suitable for inhalation and can be used for the treatment of diseases of the upper and/or lower airway passages.
摘要翻译：本发明涉及用于制备用于治疗上，下气道通道疾病的药物和药物产品的甾体溶液。本发明的各种实施方案提供了组合物，组合物和剂型，其具有溶解状态的糠酸莫米他松，其适于吸入并且可用于治疗上部和/或下部气道通道的疾病。

2. 发明申请

US20110038925A1 INTRAVENOUS FORMULATIONS OF NEUROKININ-1 ANTAGONISTS 有权
标题翻译：神经营养因子-1拮抗剂的静脉制剂
公开(公告)号：US20110038925A1
公开(公告)日：2011-02-17
申请号：US12855889
申请日：2010-08-13
申请人： Jiansheng WAN , Pranav GUPTA , David MONTEITH , Soumendu BHATTACHARYA
发明人： Jiansheng WAN , Pranav GUPTA , David MONTEITH , Soumendu BHATTACHARYA
IPC分类号： A61K9/127 , A61K31/438 , A61P1/08 , A61P7/06 , A61P25/24 , A61P29/00 , A61P35/00 , C07D471/10 , A61K31/675
CPC分类号： C07D471/10 , A61K9/0019 , A61K9/1075 , A61K31/44 , A61K47/14 , A61K47/24 , A61K47/44
摘要： Pharmaceutical compositions for intravenous administration comprising the compound of Formula I or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
摘要翻译：本文描述了包含式I化合物或其药学上可接受的盐，水合物或前药的用于静脉内给药的药物组合物。本文还描述了制备药物组合物的方法和用药物组合物治疗恶心和/或呕吐的方法。

3. 发明申请

US20100310611A1 Parenteral and oral formulations of benzimidazoles 审中-公开
标题翻译：苯并咪唑的肠胃外和口服制剂
公开(公告)号：US20100310611A1
公开(公告)日：2010-12-09
申请号：US12802621
申请日：2010-06-10
申请人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Dong Liang
发明人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Dong Liang
IPC分类号： A61K31/4184 , A61K9/107 , A61P33/10 , A61P33/12
CPC分类号： A61K9/1075 , A61K9/0019 , A61K9/0095 , A61K31/4184
摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.
摘要翻译：本文提供了药物递送系统，例如适合于向对象的肠胃外或口服递送的自 - 纳米乳化药物递送系统，自乳化药物递送系统和胃肠外微乳剂制剂。药物递送系统可以在微乳液制剂中包含苯并咪唑衍生物，例如甲苯达唑，油，表面活性剂，辅助表面活性剂和偶极非质子溶剂。还提供了通过使用组合特定乳剂液滴直径的组合物和其中表面活性剂：助表面活性剂的比例来改善治疗病理生理状况期间苯并咪唑衍生物的生物利用度的方法，用于增加苯并咪唑衍生物在肺中的浓度和保留通过具有约35nm至小于100nm的液滴尺寸的肠胃外可施用的微乳液，并且在通过具有表面活性剂的肠胃外可施用的微乳液的治疗性治疗期间限定苯并咪唑衍生物的溶血安全微乳液：辅助表面活性剂含量为约6％至48％。

4. 发明申请

US20100081672A1 PH SENSITIVE MATRIX FORMULATION 审中-公开
标题翻译：敏感矩阵公式
公开(公告)号：US20100081672A1
公开(公告)日：2010-04-01
申请号：US12517317
申请日：2007-12-06
申请人： Jiansheng Wan , Xiaoming Chen , Pranav Gupta , David Monteith
发明人： Jiansheng Wan , Xiaoming Chen , Pranav Gupta , David Monteith
IPC分类号： A61K31/403 , A61K31/497 , A61P1/02
CPC分类号： A61K31/155 , A61K9/0065 , A61K9/2027 , A61K9/2054 , A61K9/2077
摘要： The present invention provides formulations of therapeutic agents that benefit from a prolonged time of controlled release in the stomach and upper gastrointestinal (GI) tract, and from an enhanced drug exposure to the upper GI tract. The formulations of the invention comprise a therapeutic agent and one or more pH sensitive polymers that are designed for accelerated hydration, expansion, disintegration and dissolution at the higher pH of the upper GI tract, thereby, ensuring that any therapeutic agent that has not been released in the stomach is released in the upper GI tract, thus maximizing absorption of therapeutic agent that has a window of absorption located at the upper GI tract.
摘要翻译：本发明提供了治疗剂的制剂，其受益于在胃和上消化道（GI）道中的延长的受控释放时间，以及增强的药物暴露于上GI道。本发明的制剂包含治疗剂和一种或多种pH敏感聚合物，其被设计用于在上GI道的较高pH下加速水合，膨胀，崩解和溶解，由此确保任何尚未释放的治疗剂胃部在胃肠道上部被释放，从而最大限度地吸收位于胃肠道上部的具有吸收窗口的治疗剂。

5. 发明申请

US20090048322A1 Parenteral and oral formulations of benzimidazoles 有权
标题翻译：苯并咪唑的肠胃外和口服制剂
公开(公告)号：US20090048322A1
公开(公告)日：2009-02-19
申请号：US12220374
申请日：2008-07-24
申请人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Dong Liang
发明人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Dong Liang
IPC分类号： A61K31/4184
CPC分类号： A61K9/1075 , A61K9/0019 , A61K9/0095 , A61K31/4184
摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.
摘要翻译：本文提供了药物递送系统，例如适合于向对象的肠胃外或口服递送的自 - 纳米乳化药物递送系统，自乳化药物递送系统和胃肠外微乳剂制剂。药物递送系统可以在微乳液制剂中包含苯并咪唑衍生物，例如甲苯达唑，油，表面活性剂，辅助表面活性剂和偶极非质子溶剂。还提供了通过使用组合特定乳剂液滴直径的组合物和其中表面活性剂：助表面活性剂的比例来改善治疗病理生理状况期间苯并咪唑衍生物的生物利用度的方法，用于增加苯并咪唑衍生物在肺中的浓度和保留通过具有约35nm至小于100nm的液滴尺寸的肠胃外可施用的微乳液，并且在通过具有表面活性剂的肠胃外可施用的微乳液的治疗性治疗期间限定苯并咪唑衍生物的溶血安全微乳液：辅助表面活性剂含量为约6％至48％。

6. 发明申请

US20080293796A1 Parenteral and oral formulations of benzimidazoles 审中-公开
标题翻译：苯并咪唑的肠胃外和口服制剂
公开(公告)号：US20080293796A1
公开(公告)日：2008-11-27
申请号：US12220364
申请日：2008-07-24
申请人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Jaymin Shah , Peter Wisniecki
发明人： Diana Shu-Lian Chow , Pranav Gupta , Yulan Qi , Jaymin Shah , Peter Wisniecki
IPC分类号： A61K31/4184 , A61P35/00
CPC分类号： A61K9/0019 , A61K9/0095 , A61K9/1075 , A61K31/4184
摘要： Provided herein are drug delivery systems comprising nanosuspension formulations suitable for parenteral delivery to a subject. The nanosuspension formulations may comprise a benzimidazole derivative, e.g., mebendazole, and surface stabilizers, such as block copolymer(s), e.g., Pluronic F108, and surfactant(s), e.g., Tween 80, and, optionally, water. Provided are methods for defining nanosuspensions of a benzimidazole derivative as having maximum therapeutic efficacy for a treatment regimen by adjusting and/or selecting particles size(s) based on pharmacokinetic parameters of the derivative in the tissue. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition and for treating a cancer by using formulation(s) combining particle diameters whereby the retention of the benzimidazole derivative within the particles increases as the diameter increases such that, upon administration, release of the benzimidazole derivative from the particles into tissue is continuous over a range of time as determined by the particle diameters.
摘要翻译：本文提供的药物递送系统包括适于肠胃外递送给个体的纳米悬浮制剂。纳米悬浮液制剂可以包含苯并咪唑衍生物，例如甲苯咪唑和表面稳定剂，例如嵌段共聚物，例如Pluronic F108和表面活性剂，例如吐温80和任选的水。提供了通过基于组织中衍生物的药代动力学参数调节和/或选择颗粒大小来定义苯并咪唑衍生物的纳米悬浮液对于治疗方案具有最大治疗功效的方法。还提供了用于在治疗病理生理状况期间改善苯并咪唑衍生物的生物利用度和通过使用结合粒径的配方治疗癌症的方法，由此直径增加时，颗粒内苯并咪唑衍生物的保留增加，在施用时，将苯并咪唑衍生物从颗粒中释放到组织中在由颗粒直径确定的时间范围内是连续的。

7. 发明授权

US10577348B2 (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations 有权
公开(公告)号：US10577348B2
公开(公告)日：2020-03-03
申请号：US15536496
申请日：2015-12-14
申请人： Merck Sharp & Dohme Corp. , Pranav Gupta , Jason Wan , Scott T. Trzaska
发明人： Pranav Gupta , Jason Wan , Scott T. Trzaska
IPC分类号： C07D401/14 , A61K9/48 , A61K31/444
摘要： A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.

8. 发明授权

US09101615B2 Intravenous formulations of neurokinin-1 antagonists 有权
标题翻译：神经激肽-1拮抗剂的静脉内制剂
公开(公告)号：US09101615B2
公开(公告)日：2015-08-11
申请号：US12855889
申请日：2010-08-13
申请人： Jiansheng Wan , Pranav Gupta , David Monteith , Soumendu Bhattacharya
发明人： Jiansheng Wan , Pranav Gupta , David Monteith , Soumendu Bhattacharya
IPC分类号： A61K9/48 , A61K31/44 , A61K9/00 , A61K9/107 , A61K47/14 , A61K47/24 , A61K47/44
CPC分类号： C07D471/10 , A61K9/0019 , A61K9/1075 , A61K31/44 , A61K47/14 , A61K47/24 , A61K47/44
摘要： Pharmaceutical compositions for intravenous administration comprising the compound of Formula I or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.
摘要翻译：本文描述了包含式I化合物或其药学上可接受的盐，水合物或前药的用于静脉内给药的药物组合物。本文还描述了制备药物组合物的方法和用药物组合物治疗恶心和/或呕吐的方法。

9. 发明申请

US20120072257A1 Optimizing Facility Utilization For Service Delivery 审中-公开
标题翻译：优化服务提供的设施利用率
公开(公告)号：US20120072257A1
公开(公告)日：2012-03-22
申请号：US12884136
申请日：2010-09-16
申请人： Jayanta Basak , Kashyap Dixit , Pranav Gupta , Julio Heshiki , Gyana R. Parija
发明人： Jayanta Basak , Kashyap Dixit , Pranav Gupta , Julio Heshiki , Gyana R. Parija
IPC分类号： G06Q10/00
CPC分类号： G06Q10/063 , G06Q10/06315
摘要： A processor identifies a first demand type, which includes a first set of demand requirements, and also identifies a second demand type, which includes a second set of demand requirements. Next, the processor retrieves a demand compatibility rule, which specifies a compatibility between the first set of demand requirements and the second set of demand requirements. The processor uses the demand compatibility rule to compute a demand type overlap value between the first demand type and the second demand type. In turn, the processor computes a minimum facility requirement based upon the demand type overlap value and generates a facility report that includes the minimum facility requirement.
摘要翻译：处理器识别包括第一组需求要求的第一需求类型，并且还识别包括第二组需求要求的第二需求类型。接下来，处理器检索需求兼容性规则，其规定了第一组需求需求与第二组需求需求之间的兼容性。处理器使用需求兼容性规则来计算第一需求类型和第二需求类型之间的需求类型重叠值。反过来，处理器根据需求类型重叠值计算最小设施要求，并生成包括最低设施要求的设施报告。

10. 发明申请

US20170362202A1 (S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3-(METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE COMPOSITIONS FOR PHARMACEUTICAL PREPARATIONS 审中-公开
公开(公告)号：US20170362202A1
公开(公告)日：2017-12-21
申请号：US15536496
申请日：2015-12-14
申请人： Pranav GUPTA , Jason WAN , Scott T. TRZASKA , Merck Sharp & Dohme Corp.
发明人： Pranav Gupta , Jason Wan , Scott T. Trzaska
IPC分类号： C07D401/14 , A61K9/48 , A61K31/444
摘要： A composition comprising (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.

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