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1. 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。

2. 发明申请

US20050244475A1 Biodegradable intravitreal tyrosine kinase implants 有权
标题翻译：可生物降解的玻璃体内酪氨酸激酶植入物
公开(公告)号：US20050244475A1
公开(公告)日：2005-11-03
申请号：US11119001
申请日：2005-04-29
申请人： Jeffrey Edelman , Patrick Hughes , Thomas Malone , Gerald DeVries , Joan-En Chang-Lin , Jane Shiah , Thierry Nivaggioli , Lon Spada , Wendy Blanda
发明人： Jeffrey Edelman , Patrick Hughes , Thomas Malone , Gerald DeVries , Joan-En Chang-Lin , Jane Shiah , Thierry Nivaggioli , Lon Spada , Wendy Blanda
IPC分类号： A61F2/00 , A61K9/00 , A61K9/20 , A61K31/00
CPC分类号： A61K9/0051 , A61F9/0017 , A61K9/204 , A61K31/404 , A61K31/454 , A61K31/5377 , A61K47/34
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 the vitreous of 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 can be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as posterior 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的眼睛玻璃体。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如眼后病症的发生。

3. 发明申请

US20070059336A1 Anti-angiogenic sustained release intraocular implants and related methods 审中-公开
标题翻译：抗血管生成持续释放眼内植入物及相关方法
公开(公告)号：US20070059336A1
公开(公告)日：2007-03-15
申请号：US11364687
申请日：2006-02-27
申请人： Patrick Hughes , Thomas Malone , Gerald De Vries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Peter Baciu , Scott Whitcup
发明人： Patrick Hughes , Thomas Malone , Gerald De Vries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Peter Baciu , Scott Whitcup
IPC分类号： A61K38/18 , A61K39/395
CPC分类号： A61K48/0041 , A61K9/0051
摘要： Biocompatible intraocular drug delivery systems include a anti-angiogenic therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three dimensional structure but retain its therapeutic activity. The therapeutic agent may be selected from the group consisting of anti-angiogenesis peptides, hormones and nucleic acid agents. 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 among others.
摘要翻译：生物相容性眼内药物递送系统包括抗血管生成治疗剂和植入物，微粒，多种植入物或微粒形式的聚合物组分及其组合。治疗剂以生物活性形式释放，例如，当释放到患者的眼睛中时，治疗剂可以保持其三维结构，或者治疗剂可以具有改变的三维结构，但保持其治疗活性。治疗剂可以选自抗血管生成肽，激素和核酸试剂。植入物可以置于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等。

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

US20060182781A1 Methods for treating ocular conditions with cyclic lipid contraining microparticles 审中-公开
标题翻译：用抑制微粒的环状脂质治疗眼部病症的方法
公开(公告)号：US20060182781A1
公开(公告)日：2006-08-17
申请号：US11368845
申请日：2006-03-06
申请人： Patrick Hughes , Joan-En Chang-Lin , Devin Welty
发明人： Patrick Hughes , Joan-En Chang-Lin , Devin Welty
IPC分类号： A61F2/00
CPC分类号： A61F9/00781 , A61F2210/0004 , A61K9/0051 , A61K9/1647 , A61K31/00
摘要： Biocompatible microparticles include a 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-oil 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，有利于将脂质组分释放到眼睛的前部和后部段中延长的时间。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。本发明的微粒包括油包水乳化微粒。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。

6. 发明申请

US20070066541A1 Compositions and methods for the intraocular transport of therapeutic agents 有权
标题翻译：治疗剂眼内运输的组合物和方法
公开(公告)号：US20070066541A1
公开(公告)日：2007-03-22
申请号：US11521872
申请日：2006-09-15
申请人： Patrick Hughes , Orest Olejnik , Joan-En Chang-Lin
发明人： Patrick Hughes , Orest Olejnik , Joan-En Chang-Lin
IPC分类号： A61K38/04 , A61K31/513 , A61K31/498 , A61K31/557
CPC分类号： A61K31/557 , A61K9/0048 , A61K31/498 , A61K31/513 , A61K47/542 , A61K47/549 , A61K47/55 , A61K47/551 , A61K47/64
摘要： Membrane transporter-targeted therapeutic agents and methods of making and using the same.
摘要翻译：膜转运体靶向治疗剂及其制备和使用方法。

7. 发明申请

US20060257452A1 Ocular therapy using alpha-2 adrenergic receptor anterior compounds having enhanced clearance rates 有权
标题翻译：使用具有增强的清除率的α-2肾上腺素能受体前体化合物进行眼部治疗
公开(公告)号：US20060257452A1
公开(公告)日：2006-11-16
申请号：US11416929
申请日：2006-05-02
申请人： Patrick Hughes , James Burke , Joan-En Chang-Lin
发明人： Patrick Hughes , James Burke , Joan-En Chang-Lin
IPC分类号： A61F2/02
CPC分类号： A61K9/0051 , A61K9/0048 , A61K9/1647
摘要： Ophthalmically therapeutic materials, such as liquid-containing compositions and polymeric drug delivery systems, include a therapeutic component which includes an alpha 2 adrenergic receptor agonist that is cleared from the anterior segment of an individual's eye to which the material is administered. The alpha 2 adrenergic receptor agonist may have a vitreal half-life greater than about three hours. The present materials are effective in treating an ocular condition(s) that affect the anterior segment of an eye, or the anterior and posterior segment of the eye. The materials are suitable for intravitreal or periocular administration and can provide prolonged drug delivery and therapeutic benefits to patients to which the materials have been administered. The alpha 2 adrenergic receptor agonists can be provided in liquid-containing formulations and/or bioerodible and/or non-bioerodible polymeric implants and microparticles. Methods of making and using the present materials are also described.
摘要翻译：眼科治疗材料，例如含液组合物和聚合物药物递送系统，包括治疗成分，其包括α2肾上腺素能受体激动剂，其从施用该物质的个体眼睛的前段清除。 α2肾上腺素能受体激动剂可具有大于约3小时的玻璃体半衰期。本发明的材料可有效治疗影响眼前段或眼部前段和后段的眼睛状况。这些材料适用于玻璃体内或眼周内给药，并且可以为已经施用材料的患者提供延长的药物递送和治疗益处。 α2肾上腺素能受体激动剂可以在含液制剂和/或生物可侵蚀和/或非生物可侵蚀的聚合物植入物和微粒中提供。还描述了制备和使用本发明材料的方法。

8. 发明申请

US20060182783A1 Sustained release intraocular drug delivery systems 审中-公开
标题翻译：持续释放眼内药物递送系统
公开(公告)号：US20060182783A1
公开(公告)日：2006-08-17
申请号：US11370301
申请日：2006-03-08
申请人： Patrick Hughes , Gerald Devries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Robert Lyons
发明人： Patrick Hughes , Gerald Devries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Robert Lyons
IPC分类号： A61K48/00 , A61F2/00
CPC分类号： A61K9/0051 , A61F9/0008 , A61F9/0017 , A61K9/1647 , A61K31/724 , A61K47/34 , A61K47/40 , A61K48/0041
摘要： Biocompatible intraocular drug delivery systems include a anti-angiogenic macromolecular therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three dimensional structure but retain its therapeutic activity. The therapeutic agent contains a component selected from the group consisting of anti-angiogenesis peptides and nucleic acid agents. 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 among others.
摘要翻译：生物相容性眼内药物递送系统包括抗血管生成大分子治疗剂和植入物，微粒，多种植入物或微粒形式的聚合物组分及其组合。治疗剂以生物活性形式释放，例如，当释放到患者的眼睛中时，治疗剂可以保持其三维结构，或者治疗剂可以具有改变的三维结构，但保持其治疗活性。治疗剂含有选自抗血管生成肽和核酸试剂的组分。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等。

9. 发明申请

US20050281861A1 Macromolecule-containing sustained release intraocular implants and related methods 审中-公开
标题翻译：含大分子的持续释放眼内植入物及相关方法
公开(公告)号：US20050281861A1
公开(公告)日：2005-12-22
申请号：US11116698
申请日：2005-04-27
申请人： Patrick Hughes , Tom Malone , Gerald Devries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Peter Baciu , Scott Whitcup
发明人： Patrick Hughes , Tom Malone , Gerald Devries , Jeffrey Edelman , Wendy Blanda , Lon Spada , Peter Baciu , Scott Whitcup
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： Biocompatible intraocular drug delivery systems include a non-neurotoxic macromolecule therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The macromolecule therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three dimensional structure but retain its therapeutic activity. The therapeutic agent may be selected from the group consisting of anti-angiogenesis agents, ocular hemorrhage treatment agents, non-steroidal anti-inflammatory agents, growth factor inhibitors (such as VEGF inhibitors), growth factors, cytokines, antibodies, oligonucleotide aptamers, siRNA molecules and antibiotics. 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 among others.
摘要翻译：生物相容性眼内药物递送系统包括非神经毒性大分子治疗剂和植入物，微粒，多种植入物或微粒形式的聚合物组分及其组合。大分子治疗剂以生物活性形式释放，例如，当释放到患者的眼睛中时，治疗剂可保留其三维结构，或者治疗剂可具有改变的三维结构，但保持其治疗活性。治疗剂可以选自抗血管生成剂，眼出血治疗剂，非甾体抗炎剂，生长因子抑制剂（例如VEGF抑制剂），生长因子，细胞因子，抗体，寡核苷酸适体，siRNA 分子和抗生素。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等。

10. 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。

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