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1. 发明申请

US20050244477A1 Tyrosine kinase microsphers 有权
标题翻译：酪氨酸激酶微球
公开(公告)号：US20050244477A1
公开(公告)日：2005-11-03
申请号：US11119463
申请日：2005-04-29
申请人： Patrick Hughes , Christian Sarrazin , Elisabeth Rossi , Michele Boix
发明人： Patrick Hughes , Christian Sarrazin , Elisabeth Rossi , Michele Boix
IPC分类号： A61K9/00 , A61K9/20 , A61K31/00 , A61K31/404 , A61F2/00
CPC分类号： A61K9/0051 , A61K9/1647 , Y10T428/2985
摘要： Biocompatible intraocular microspheres include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the microspheres can be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The microspheres can be placed into an eye to treat or reduce the occurrence of one or more ocular conditions.
摘要翻译：生物相容性眼内微球包括酪氨酸激酶抑制剂和可生物降解的聚合物，其有效促进酪氨酸激酶抑制剂延长一段时间后进入眼睛玻璃体。微球的治疗剂可以与可生物降解的聚合物基质相结合，例如基本上不含聚乙烯醇的基质。微球可以放置在眼睛中以治疗或减少一种或多种眼睛病症的发生。

2. 发明申请

US20050003007A1 Method of sterilization of polymeric microparticles 审中-公开
标题翻译：聚合物微粒灭菌方法
公开(公告)号：US20050003007A1
公开(公告)日：2005-01-06
申请号：US10614408
申请日：2003-07-02
申请人： Michele Boix , Christian Sarrazin , Patrick Hughes , Marina Do , Isabelle Maroteaux
发明人： Michele Boix , Christian Sarrazin , Patrick Hughes , Marina Do , Isabelle Maroteaux
IPC分类号： A61K9/16 , A61K31/455 , A61K41/00 , A61L2/08 , A61L2/10 , A61L2/12 , A61K9/14
CPC分类号： A61L2/087 , A61K9/1647 , A61K31/455 , A61K41/0019 , A61L2/081 , A61L2/10 , A61L2/12
摘要： This invention relates to the sterilization of polymeric material by irradiation for use in a body of a mammal. We have surprisingly discovered that the sterilization of polymeric materials for use in a mammal by irradiation is improved by reducing the temperature at which the irradiation is carried out. One aspect of this invention relates to a sterilized polymeric material for use in a body of a mammal wherein said polymeric material is sterilized by irradiation at a reduced temperature Another aspect of this invention relates to methods of sustained delivery of a therapeutically active agent to a mammal by using a polymeric material that has been sterilized at a reduced temperature by irradiation.
摘要翻译：本发明涉及通过照射用于哺乳动物体内的聚合材料的灭菌。我们惊奇地发现，通过降低进行照射的温度来改善通过照射对哺乳动物使用的聚合材料的灭菌。本发明的一个方面涉及用于哺乳动物身体的灭菌聚合物材料，其中所述聚合物材料通过在降低的温度下照射而灭菌。本发明的另一方面涉及将治疗活性剂持续递送至哺乳动物的方法通过使用通过照射在降低的温度下灭菌的聚合物材料。

3. 发明申请

US20070224246A1 Oil-in-oil emulsified polymeric implants containing a hypotensive lipid and related methods 有权
标题翻译：油包油乳化聚合物植入物含有低血压脂质和相关方法
公开(公告)号：US20070224246A1
公开(公告)日：2007-09-27
申请号：US11303462
申请日：2005-12-15
申请人： Patrick Hughes , Michele Boix , Christian Sarrazin , Marina Do
发明人： Patrick Hughes , Michele Boix , Christian Sarrazin , Marina Do
IPC分类号： A61K31/557 , A61F2/00
CPC分类号： A61K31/5575 , A61K9/0048 , A61K9/0051 , A61K9/1075 , A61K9/1647 , A61K9/1694 , A61K9/5031 , A61K9/5089 , A61K31/165 , A61K31/216 , A61K47/34 , A61L2/081 , B01J13/02 , B01J13/04 , B01J13/06
摘要： Biocompatible intraocular implants, such as microparticles, include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the prostamide component may be encapsulated by the polymeric component. The present implants include oil-in-oil emulsified implants or microparticles. Methods of producing the present implants are also described. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma.
摘要翻译：生物相容性眼内植入物，例如微粒，包括有助于促进前列腺酰胺组分长时间释放到眼睛中的前列腺酰胺组分和可生物降解的聚合物。前列腺酰胺组分可以与可生物降解的聚合物基质相结合，例如两种可生物降解聚合物的基质。或者，前列腺酰胺组分可以被聚合物组分包封。本植入物包括油包油乳化植入物或微粒。还描述了生产本植入物的方法。植入物可以放置在眼睛中以治疗或减少眼部疾病如青光眼的至少一种症状。

4. 发明申请

US20050271705A1 Retinoid-containing sustained release intraocular drug delivery system and related methods 审中-公开
标题翻译：含维甲酸的持续释放眼内药物递送系统及相关方法
公开(公告)号：US20050271705A1
公开(公告)日：2005-12-08
申请号：US11119024
申请日：2005-04-29
申请人： Patrick Hughes , Orest Olejnik , Glenn Huang , Joan-En Chang-Lin , Thierry Nivaggioli , JaneGuo Shiah , Michele Boix , Christian Sarrazin
发明人： Patrick Hughes , Orest Olejnik , Glenn Huang , Joan-En Chang-Lin , Thierry Nivaggioli , JaneGuo Shiah , Michele Boix , Christian Sarrazin
IPC分类号： A61K9/00 , A61K9/16 , A61K31/07 , A61K31/203 , A61K31/19 , A61K31/20
CPC分类号： A61K31/07 , A61K9/0051 , A61K9/1647 , A61K31/203
摘要： Biocompatible intraocular implants include a retinoid component and a biodegradable polymer that is effective to facilitate release of the retinoid component into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.
摘要翻译：生物相容性眼内植入物包括类视黄醇组分和可生物降解的聚合物，其有效促进类视黄醇组分长时间释放到眼睛中。植入物的治疗剂可以与可生物降解的聚合物基质相关，例如基本上不含聚乙烯醇的基质。植入物可以放置在眼睛中以治疗或减少一种或多种眼部病症的发生，例如视网膜损伤，包括青光眼和增生性玻璃体视网膜病变。

5. 发明申请

US20050244472A1 Intraocular drug delivery systems containing excipients with reduced toxicity and related methods 审中-公开
标题翻译：含有降低毒性的赋形剂和相关方法的眼内药物递送系统
公开(公告)号：US20050244472A1
公开(公告)日：2005-11-03
申请号：US11092122
申请日：2005-03-28
申请人： Patrick Hughes , Laurent Delahaye , Michele Boix
发明人： Patrick Hughes , Laurent Delahaye , Michele Boix
IPC分类号： A61F2/00 , A61F9/00 , A61K9/00 , A61K9/16 , A61K31/724 , A61K39/395 , A61K47/34 , A61K47/40 , A61K47/48 , A61K48/00
CPC分类号： A61K9/0051 , A61F9/0008 , A61F9/0017 , A61K9/1647 , A61K31/724 , A61K47/34 , A61K47/40
摘要： Drug delivery systems suitable for administration into the interior of an eye of a person or animal are described. The present systems include one or more components which are effective in improving a release profile of a drug from the system, improving the stability of the drug, and improving the ocular tolerability of the drug. The present systems include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and an excipient component with reduced toxicity to retinal cells. The excipient component may include a cyclodextrin component that may be complexed with the therapeutic agents to provide advantages over existing intraocular drug delivery systems. The cyclodextrin component of the present systems have a reduced toxicity relative to benzyl alcohol or polysorbate 80. The drug delivery systems include one or more drug delivery elements such as microparticles, bioerodible implants, non-bioerodible implants, and combinations thereof. Methods of using and producing the drug delivery systems are also described.
摘要翻译：描述了适合施用于人或动物的眼睛内部的药物递送系统。本发明的系统包括一种或多种有效改善药物从系统释放曲线，提高药物稳定性和改善药物的眼睛耐受性的成分。本发明的系统包括当放置在眼睛中时有效提供所需治疗效果的量的一种或多种治疗剂和对视网膜细胞毒性降低的赋形剂组分。赋形剂组分可以包括可与治疗剂复合的环糊精组分，以提供优于现有的眼内药物递送系统的优点。本系统的环糊精组分相对于苯甲醇或聚山梨酸酯80具有降低的毒性。药物递送系统包括一种或多种药物递送元件，例如微粒，生物侵蚀性植入物，非生物侵蚀性植入物及其组合。还描述了使用和产生药物递送系统的方法。

6. 发明申请

US20050250737A1 Therapeutic ophthalmic compositions containing retinal friendly excipients and related methods 审中-公开
标题翻译：含有视网膜友好赋形剂的治疗眼用组合物及相关方法
公开(公告)号：US20050250737A1
公开(公告)日：2005-11-10
申请号：US11091977
申请日：2005-03-28
申请人： Patrick Hughes , Laurent Delahaye , Michele Boix , James Chang , Robert Lyons
发明人： Patrick Hughes , Laurent Delahaye , Michele Boix , James Chang , Robert Lyons
IPC分类号： A61K9/00 , A61K31/573 , A61K31/724 , A61K47/36
CPC分类号： A61K9/0048 , A61K31/573 , A61K47/36 , A61K47/40
摘要： Pharmaceutical compositions suitable for administration into the interior of an eye of a person or animal are described. The present compositions include one or more components which are effective in providing a reduced toxicity relative to existing intraocular ophthalmic compositions. The present compositions include one or more therapeutic agents in amounts effective in providing a desired therapeutic effect when placed in an eye, and one or more retinal friendly excipients that have a reduced toxicity relative to benzyl alcohol or polysorbate 80. In certain compositions, the excipient component of the compositions comprises one or more cyclodextrins or cyclodextrin derivatives. Methods of using the compositions to treat ocular conditions are also described.
摘要翻译：描述适于施用于人或动物的眼睛内部的药物组合物。本发明组合物包括一种或多种有效提供相对于现有眼内眼用组合物的毒性降低的成分。本发明的组合物包含一种或多种治疗剂，其用量在置于眼中时可提供所需的治疗效果，以及一种或多种视黄醛友好的赋形剂，其相对于苯甲醇或聚山梨酸酯80具有降低的毒性。在某些组合物中，赋形剂组合物的组分包含一种或多种环糊精或环糊精衍生物。还描述了使用组合物治疗眼睛病症的方法。

7. 发明申请

US20110263611A1 Kinase Inhibitors 有权
标题翻译：激酶抑制剂
公开(公告)号：US20110263611A1
公开(公告)日：2011-10-27
申请号：US13178277
申请日：2011-07-07
申请人： Lon T. Spada , Jane Guo Shiah , Patrick Hughes , Thomas C. Malone , Gerald W. Devries , Jeffrey L. Edelman , Julie A. Wurster
发明人： Lon T. Spada , Jane Guo Shiah , Patrick Hughes , Thomas C. Malone , Gerald W. Devries , Jeffrey L. Edelman , Julie A. Wurster
IPC分类号： A61K31/496 , A61P27/06 , A61K31/5377 , A61P27/02
CPC分类号： C07D213/82 , A61K9/0051 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K47/34 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D413/06 , C07D417/06 , Y02A50/401
摘要： The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.
摘要翻译：本发明涉及药物递送系统，其包括眼部植入物，其包括能够调节酪氨酸激酶信号转导以调节，调节和/或抑制异常细胞增殖的有机分子，所述聚合物用于控制聚合物，改变，调节和/或缓慢释放治疗组分到其中放置所述复合物的眼睛的环境中。

8. 发明申请

US20050244470A1 Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods 有权
标题翻译：含有酪氨酸激酶抑制剂的持续释放眼内植入物及相关方法
公开(公告)号：US20050244470A1
公开(公告)日：2005-11-03
申请号：US10837361
申请日：2004-04-30
申请人： Patrick Hughes , Thomas Malone , Gerald De Vries , Jeffrey Edelman , Joan-En Chang-Lin , Jane Shiah , Thierry Nivaggioli
发明人： Patrick Hughes , Thomas Malone , Gerald De Vries , Jeffrey Edelman , Joan-En Chang-Lin , Jane Shiah , Thierry Nivaggioli
IPC分类号： A61K9/00 , A61K9/20 , A61K31/00 , A61K31/404 , A61F2/00
CPC分类号： A61K9/0051 , A61K9/1647 , Y10T428/2985
摘要： Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.
摘要翻译：生物相容性眼内植入物包括酪氨酸激酶抑制剂和生物可降解聚合物，其有效促进酪氨酸激酶抑制剂长时间释放到眼睛中。植入物的治疗剂可以与可生物降解的聚合物基质相关，例如基本上不含聚乙烯醇的基质。植入物可以放置在眼睛中以治疗或减少一种或多种眼部病症的发生。

9. 发明申请

US20050181017A1 Compositions and methods for localized therapy of the eye 审中-公开
标题翻译：眼睛局部治疗的组成和方法
公开(公告)号：US20050181017A1
公开(公告)日：2005-08-18
申请号：US11039192
申请日：2005-01-19
申请人： Patrick Hughes , Orest Olejnik , Scott Whitcup , James Burke
发明人： Patrick Hughes , Orest Olejnik , Scott Whitcup , James Burke
IPC分类号： A61K9/00 , A61K9/10 , A61K9/14 , A61K31/00 , A61K47/36
CPC分类号： A61K38/13 , A61K9/0048 , A61K9/0051 , A61K9/10 , A61K9/14 , A61K31/00 , A61K47/36 , Y10S514/912
摘要： Compositions, and methods of using such compositions, useful for injection into the posterior segments of human or animal eyes are provided. Such compositions include small particles of a poorly soluble therapeutic agent that facilitates formation of concentrated regions of the therapeutic agent in the retinal pigmented epithelium of an eye. The particles are formed by combining a therapeutic agent with an ophthalmically acceptable polymer component. The particles have sizes less than about 3000 nanometers, and in some cases, less than about 200 nanometers. One example of a composition includes particles of triamcinolone acetonide and hyaluronic acid have a size less than about 3000 nanometers.
摘要翻译：提供了组合物和使用这种组合物的方法，其可用于注射到人或动物眼睛的后段中。这样的组合物包括促进在眼睛的视网膜色素上皮中形成治疗剂的浓缩区域的难溶性治疗剂的小颗粒。通过将治疗剂与眼科可接受的聚合物组分组合来形成颗粒。颗粒具有小于约3000纳米的尺寸，并且在一些情况下小于约200纳米。组合物的一个实例包括曲安奈德的颗粒和透明质酸的尺寸小于约3000纳米。

10. 发明授权

US08722097B2 Oil-in-water method for making polymeric implants containing a hypotensive lipid 有权
标题翻译：用于制造含有低血压脂质的聚合物植入物的水包油法
公开(公告)号：US08722097B2
公开(公告)日：2014-05-13
申请号：US11371118
申请日：2006-03-08
申请人： James Chang , Patrick Hughes , Chin-Ming Chang
发明人： James Chang , Patrick Hughes , Chin-Ming Chang
IPC分类号： A61K9/50 , B01J13/02 , B01J13/04
CPC分类号： A61K31/5575 , A61K9/0048 , A61K9/0051 , A61K9/107 , A61K9/1075 , A61K9/146 , A61K9/1647 , A61K9/1694 , A61K31/165 , A61K47/34 , B01J13/04 , B01J13/06
摘要： Biocompatible microparticles include an ophthalmically active cyclic lipid component and a biodegradable polymer that is effective, when placed into the subconjunctival space, in facilitating release of the cyclic lipid component into the anterior and posterior segments of an eye for an extended period of time. The cyclic lipid component can be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the cyclic lipid component can be encapsulated by the polymeric component. The present microparticles include oil-in-water emulsified microparticles. The subconjunctivally administered microparticles can be used to treat or to reduce at least one symptom of an ocular condition, such as glaucoma or age related macular degeneration.
摘要翻译：生物相容的微粒包括眼科活性的环状脂质组分和可生物降解的聚合物，当放置在结膜下空间中时，有效地促进环状脂质成分延长眼睛部分的时间。环状脂质组分可与可生物降解的聚合物基质相结合，例如两种可生物降解聚合物的基质。或者，环状脂质组分可以被聚合物组分包封。本发明的微粒包括水包油乳化微粒。结膜下施用的微粒可用于治疗或减少眼部疾病如青光眼或年龄相关性黄斑变性的至少一种症状。

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