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    Ophthalmic compositions
    1.
    发明授权
    Ophthalmic compositions 有权

    公开(公告)号：US10265375B2

    公开(公告)日：2019-04-23

    申请号：US14627063

    申请日：2015-02-20

    申请人： Aurinia Pharmaceuticals Inc.

    发明人： Ashim K. Mitra ,  Poonam R. Velagaleti ,  Subramanian Natesan

    IPC分类号： A61K9/00 ,  A61K31/56 ,  A61K38/13 ,  A61K47/32 ,  A61K9/107 ,  A61K31/355 ,  A61K31/436

    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.

    CYCLOSPORIN ANALOG FORMULATIONS
    2.
    发明申请
    CYCLOSPORIN ANALOG FORMULATIONS 审中-公开
    环磷酰胺类似物制剂

    公开(公告)号：US20140249092A1

    公开(公告)日：2014-09-04

    申请号：US14201872

    申请日：2014-03-09

    申请人： Aurinia Pharmaceuticals, Inc.

    发明人： Selvaraj A. Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    IPC分类号： A61K9/107 ,  A61K38/13

    CPC分类号： A61K9/1075 ,  A61K9/0095 ,  A61K9/4858 ,  A61K38/13 ,  A61K47/10

    摘要： The present disclosure relates to formulations containing cyclosporin analogs that are structurally similar to cyclosporin A, in particular isomeric mixtures of cyclosporin analogs that are structurally similar to cyclosporin A. The formulations form stable microemulsion preconcentrates and may provide superior drug bioavailability and/or may reduce one or more adverse effects associated with the administration of cyclosporin. Also disclosed are methods for using and preparing the formulations.

    摘要翻译： 本公开内容涉及在结构上类似于环孢菌素A的环孢菌素类似物的制剂，特别是在环孢菌素类似物的结构上类似于环孢菌素A的异构体混合物中。制剂形成稳定的微乳液预浓缩物并且可以提供优异的药物生物利用度和/或可以减少一种 或更多与施用环孢菌素相关的不良反应。 还公开了使用和制备制剂的方法。

    Topical Drug Delivery System for Ophthalmic Use
    6.
    发明申请
    Topical Drug Delivery System for Ophthalmic Use 审中-公开
    眼科用药专用药物输送系统

    公开(公告)号：US20150202150A1

    公开(公告)日：2015-07-23

    申请号：US14676993

    申请日：2015-04-02

    申请人： Aurinia Pharmaceuticals Inc.

    发明人： Ashim K. Mitra ,  Poonam R. Velagaleti ,  Ulrich M. Grau

    IPC分类号： A61K9/107 ,  A61K47/10 ,  A61K47/22 ,  A61K31/573 ,  A61K9/00

    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。

    CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS
    7.
    发明申请
    CYCLOSPORINE ANALOGUE MIXTURES AND THEIR USE AS IMMUNOMODULATING AGENTS 审中-公开
    环孢素类似物混合物及其作为免疫调节剂的使用

    公开(公告)号：US20140370082A1

    公开(公告)日：2014-12-18

    申请号：US14324146

    申请日：2014-07-04

    申请人： Aurinia Pharmaceuticals Inc.

    发明人： Selvaraj A. Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    IPC分类号： C07K7/64

    CPC分类号： C07K7/645 ,  A61K9/0095 ,  A61K9/1075 ,  A61K9/4858 ,  A61K38/00 ,  A61K38/13 ,  B82Y5/00 ,  C07K7/64 ,  Y10S530/806

    摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereo selectivity. The ratio of isomers in a mixture comprises greater than about 80 percent by weight of the E-isomer and less than about 20 percent by weight of the Z-isomer, based on the total weight of the mixture.

    摘要翻译： 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。 本发明的实施方案涉及称为ISATX247的环孢菌素A类似物的顺式和反式异构体及其衍生物。 ISATX247异构体的混合物显示与天然存在的和目前已知的环孢菌素相比，其效力和毒性降低的组合。 ISATX247异构体和烷基化，芳基化和氘代衍生物通过立体选择性途径合成，其中反应的特定条件决定了立体选择性的程度。 基于混合物的总重量，混合物中的异构体的比例包含大于约80重量％的E-异构体和小于约20重量％的Z-异构体。

    Cyclosporine analogue mixtures and their use as immunomodulating agents
    10.
    再颁专利
    Cyclosporine analogue mixtures and their use as immunomodulating agents 有权

    公开(公告)号：USRE48226E1

    公开(公告)日：2020-09-29

    申请号：US14320408

    申请日：2014-06-30

    申请人： Aurinia Pharmaceuticals Inc.

    发明人： Selvaraj A. Naicker ,  Randall W Yatscoff ,  Robert T Foster

    IPC分类号： A61K38/13 ,  C07K7/64 ,  A61K9/00 ,  A61K9/107 ,  A61K9/48 ,  B82Y5/00 ,  A61K38/00

    摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.