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公开(公告)号：US20110105417A1
公开(公告)日：2011-05-05
申请号：US12999149
申请日：2009-06-26
IPC分类号： A61K38/05 , C07D473/18 , C07D475/04 , C07H21/02 , A61K31/522 , A61K31/519 , A61K31/713
CPC分类号： A61K47/64 , A61K47/545 , A61K47/551 , A61K47/557
摘要： Conjugated compounds comprising a therapeutic or diagnostic agent linked to a substrate for a cell membrane transporter or receptor by lipophilic linker are provided.
摘要翻译： 提供了包含通过亲脂性接头与细胞膜转运蛋白或受体的底物连接的治疗剂或诊断剂的共轭化合物。
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2.发明授权Stereochemically defined dipeptide esters of antiviral agents for enhanced ocular treatment 有权用于增强眼部治疗的抗病毒剂的立体定义二肽酯公开(公告)号：US07951774B2
公开(公告)日：2011-05-31
申请号：US12277442
申请日：2008-11-25
CPC分类号： C07K5/06026 , C07K5/06052 , C07K5/06078
摘要： Stereochemically defined dipeptide esters of nucleoside-analogous antiviral agents including acyclovir and ganciclovir are provided. Certain of these stereochemically defined dipeptide esters are found to have unexpectedly enhanced delivery to and uptake by ocular tissues, crossing the blood-ocular barrier more effectively than other stereochemically defined dipeptide esters. For example, (L-Val)-(D-Val)-acyclovir was found to be taken up more effectively into corneal tissue than were underivatized acyclovir, monoesters (L-Val)-acyclovir or (D-Val)-acyclovir, or diester (L-Val)-(L-Val)-acyclovir.
摘要翻译： 提供了包括阿昔洛韦和更昔洛韦的核苷类似抗病毒剂的立体定义的二肽酯。 发现这些立体定义的二肽酯中的某些具有意想不到的增强对眼组织的摄取和摄取，与其它立体定义的二肽酯相比更有效地穿过血球屏障。 例如，发现（L-Val） - （D-Val） - 环孢菌素比未发病的阿昔洛韦，单酯（L-Val） - 环己烷或（D-Val） - 环孢菌素更有效地吸收在角膜组织中，或 二酯（L-Val） - （L-Val） - 环孢菌素。
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公开(公告)号：US07910553B2
公开(公告)日：2011-03-22
申请号：US11677947
申请日：2007-02-22
申请人： Ashim K. Mitra , Soumyajit Majumdar , Ritesh Jain , Yasser Nashed
发明人： Ashim K. Mitra , Soumyajit Majumdar , Ritesh Jain , Yasser Nashed
IPC分类号： C07K5/06
CPC分类号： A61K38/04 , C07K5/06026 , C07K5/06052 , Y02P20/55
摘要： A method of treating a patient for a condition wherein the bioactive agent of choice is DRUG, wherein DRUG is a substrate that is effluxed by the P-gp transporter, is provided, the method comprising administering to the patient an effective amount of a compound of formula (I): DRUG-X—Y(n)—Z(n′)—Z′(n″)—R (I) wherein each X, Y, Z, and Z′ is independently Met, Val, Thr, Tyr, Trp, Ser, Ala, or Gly; R is H or an amino-protecting group; n is 1, and each n′, or n″ is independently 0 or 1; or a pharmaceutically acceptable salt thereof, with the proviso that DRUG is not acyclovir or ganciclovir and that DRUG is non-peptidyl.
摘要翻译： 一种治疗患者的方法，其中选择的生物活性剂是DRUG，其中DRUG是由P-gp转运蛋白排出的底物，所述方法包括向患者施用有效量的化合物 式（I）：其中X，Y，Z和Z'各自独立地为Met，Val，Thr， Tyr，Trp，Ser，Ala或Gly; R是H或氨基保护基; n为1，每个n'或n“独立地为0或1; 或其药学上可接受的盐，条件是DRUG不是阿昔洛韦或更昔洛韦，并且该DRUG是非肽基。
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公开(公告)号：US20080177220A1
公开(公告)日：2008-07-24
申请号：US11620990
申请日：2007-01-08
申请人： Daniel Lindgren , Ashim K. Mitra
发明人： Daniel Lindgren , Ashim K. Mitra
CPC分类号： A61F9/0008 , A61M37/0092
摘要： The present invention relates to processes, systems, and apparatuses for transcieral delivery of pharmaceutical formulations to the eye using ultrasound. In one embodiment, a transducer is placed in contact with a coupling media contained in a coupling well in contact with the sclera. When the transducer is placed at a desired standoff distance, ultrasonic waves are emitted to increase tissue porosity and transport a pharmaceutical formulation through the scleral tissue and into the eye. In another embodiment, a function generator is coupled to an amplifier, a matching network, and a transducer configured to maximize the cavitation effect of ultrasonic waves for drug delivery across a sclera.
摘要翻译： 本发明涉及使用超声波将药物制剂向眼睛进行电导传递的方法，系统和装置。 在一个实施例中，换能器放置成与包含在与巩膜接触的联接井中的耦合介质接触。 当换能器放置在所需的间隔距离时，发射超声波以增加组织孔隙率并将药物制剂输送通过巩膜组织并进入眼睛。 在另一个实施例中，功能发生器耦合到放大器，匹配网络和被配置为使超声波的空化效应最大化以用于穿过巩膜的药物递送的换能器。
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公开(公告)号：US09017725B2
公开(公告)日：2015-04-28
申请号：US12774600
申请日：2010-05-05
IPC分类号： A61K9/14 , A61K31/56 , A61K31/573 , A61K9/00 , A61K9/107 , A61K31/14 , A61K31/436 , A61K47/10 , A61K47/22
CPC分类号： A61K9/1075 , A61K9/0048 , A61K9/107 , A61K31/14 , A61K31/436 , A61K31/573 , A61K47/10 , A61K47/22 , Y10S514/912
摘要： Topical drug delivery systems for ophthalmic use including mixed nanomicellar formulations of water-insoluble drugs and methods of treating diseases affecting the posterior ocular segments are disclosed. In an embodiment, an aqueous ophthalmic solution includes nanomicelles in a physiologically acceptable buffer, having a pH of 5.0 to 8.0, wherein a corticosteroid at a concentration from about 0.01% w/v to about 1.00% w/v is solubilized through entrapment in a mixed micellar hydrophobic core with a corona composed of hydrophilic chains extending from the hydrophobic core, wherein the nanomicelles comprise vitamin E TPGS at a concentration ranging from about 3.0% w/v to about 5.0% w/v stabilized with octoxynol-40 at a concentration ranging from about 1.0% w/v to about 3.0% w/v.
摘要翻译： 公开了用于眼用的局部药物递送系统，包括水不溶性药物的混合纳米胶囊制剂和治疗影响后眼部疾病的疾病的方法。 在一个实施方案中，眼用水溶液包括生理学上可接受的缓冲液中的纳米胶囊，pH为5.0-8.0，其中浓度为约0.01％w / v至约1.00％w / v的皮质类固醇通过包埋在 混合的胶束疏水核心，其具有由疏水核心延伸的亲水链组成的电晕，其中所述纳米胶束包含浓度范围为约3.0％w / v至约5.0％w / v的维生素E TPGS，其浓度为辛烯苯醇-40 范围为约1.0％w / v至约3.0％w / v。
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6.发明申请OPHTHALMIC COMPOSITIONS COMPRISING CALCINEURIN INHIBITORS OR mTOR INHIBITORS 有权包含CALCINEURIN抑制剂或mTOR抑制剂的眼科组合物公开(公告)号：US20090092665A1
公开(公告)日：2009-04-09
申请号：US12247701
申请日：2008-10-08
IPC分类号： A61K9/127 , A61K38/13 , A61K31/436 , A61K31/355 , A61P27/02 , A61P27/04
CPC分类号： A61K38/13 , A61K9/0048 , A61K9/1075 , A61K31/355 , A61K31/436 , A61K31/56 , A61K47/32
摘要： The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.
摘要翻译： 本文公开的实施方案涉及包含钙调神经磷酸酶抑制剂或mTOR抑制剂的眼用组合物，更具体地涉及使用所公开的组合物治疗眼部疾病和/或病症的方法。 根据本文所述的方面，提供了包含钙调神经磷酸酶抑制剂或mTOR抑制剂的药物组合物; HLB指数大于约10的第一表面活性剂; 和HLB指数大于约13的第二表面活性剂，其中第一表面活性剂的HLB指数与第二表面活性剂的HLB指数之间的绝对差大于约3，并且其中所述组合物形成混合胶束。
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公开(公告)号：US08980839B2
公开(公告)日：2015-03-17
申请号：US13975175
申请日：2013-08-23
申请人： Ashim K. Mitra , Sidney L. Weiss
发明人： Ashim K. Mitra , Sidney L. Weiss
CPC分类号： A61K38/13 , A61K9/0048 , A61K9/1075 , A61K31/202 , A61K47/10 , A61K47/44
摘要： Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.
摘要翻译： 本文提供了用于局部给药的制剂，例如眼用制剂，以及使用这些制剂的方法。 在一些方面和实施方案中，制剂可以包括聚氧脂质或脂肪酸，和/或聚烷氧基化的醇，并且可以包括纳米胶束。 还包括治疗或预防诸如眼部疾病或病症的疾病或病症的方法。
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8.发明申请Ophthalmic Compositions Comprising Calcineurin Inhibitors or mTOR Inhibitors 有权包含钙调神经磷酸酶抑制剂或mTOR抑制剂的眼科组合物公开(公告)号：US20110300195A1
公开(公告)日：2011-12-08
申请号：US13213451
申请日：2011-08-19
IPC分类号： A61K9/00 , A61P29/00 , A61P27/02 , A61K38/13 , A61K31/436
CPC分类号： A61K38/13 , A61K9/0048 , A61K9/1075 , A61K31/355 , A61K31/436 , A61K31/56 , A61K47/32
摘要： The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.
摘要翻译： 本文公开的实施方案涉及包含钙调神经磷酸酶抑制剂或mTOR抑制剂的眼用组合物，更具体地涉及使用所公开的组合物治疗眼部疾病和/或病症的方法。 根据本文所述的方面，提供了包含钙调神经磷酸酶抑制剂或mTOR抑制剂的药物组合物; HLB指数大于约10的第一表面活性剂; 和HLB指数大于约13的第二表面活性剂，其中第一表面活性剂的HLB指数与第二表面活性剂的HLB指数之间的绝对差大于约3，并且其中所述组合物形成混合胶束。
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公开(公告)号：US20110250283A1
公开(公告)日：2011-10-13
申请号：US12758541
申请日：2010-04-12
CPC分类号： A61K9/5031 , A61K9/0019 , A61K9/5026 , A61K9/5138 , A61K31/573 , A61K49/0093 , C08G63/664
摘要： Novel pentablock polymers comprising PGA-PCL-PEG-PCL-PGA or PEG-PCL-PLA-PCL-PEG, wherein PEG is polyethylene glycol, PCL is poly(ε-caprolactone), PGA is poly(glycolic acid), and PLA is poly(lactic acid).
摘要翻译： 包括PGA-PCL-PEG-PCL-PGA或PEG-PCL-PLA-PCL-PEG的新型五嵌段聚合物，其中PEG是聚乙二醇，PCL是聚（ε-己内酯），PGA是聚（乙醇酸），PLA 是聚（乳酸）。
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公开(公告)号：US07214664B2
公开(公告)日：2007-05-08
申请号：US11285754
申请日：2005-11-22
申请人： Ashim K. Mitra , Soumyajit Majumdar , Ritesh Jain , Yasser Nashed
发明人： Ashim K. Mitra , Soumyajit Majumdar , Ritesh Jain , Yasser Nashed
IPC分类号： A61K31/00
CPC分类号： A61K38/04 , C07K5/06026 , C07K5/06052 , Y02P20/55
摘要： Dipeptide, and tripeptide and tetrapeptide ester derivatives of bioactive agents are provided wherein the parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactive agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery by nutrient or peptide transporters comprising linking the agent to one or more groups of the formula —X—Y(n)-Z(n′)-Z′(n″)-R; wherein each X, Y, Z, and Z′ is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; R is independently H or an amino-protecting group; n=1, and each, n′, or n″ is independently 0 or 1.
摘要翻译： 提供二肽和生物活性剂的三肽和四肽酯衍生物，其中母体试剂是由P-gp转运蛋白排出的底物。 衍生物可用于治疗与生物活性剂相同的条件。 还公开了一种通过营养或肽转运蛋白制备用于靶向递送的生物活性剂的方法，包括将该试剂与一种或多种式-XY（n）-Z（n'） ） -Z'（n“） -R; 其中每个X，Y，Z和Z'独立地为Met，Val，Thr，Tyr，Trp，Ser，Ala或Gly; R独立地为H或氨基保护基; n = 1，并且每个，n'或n“独立地为0或1。
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