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公开(公告)号：US08821870B2
公开(公告)日：2014-09-02
申请号：US12176238
申请日：2008-07-18
IPC分类号： A61K39/395 , A61K9/19 , A61K9/48 , C07K16/22
CPC分类号： A61K9/0048 , A61K9/0051 , A61K9/1635 , A61K9/1647 , A61K9/1652 , A61K31/712 , A61K47/36 , A61K2039/505 , C07K16/22
摘要： Compositions and methods for treating dry age related macular degeneration (dry AMD) by administration to an intraocular location of an anti-neovascular agent (such as bevacizumab) in either a liquid or solid polymeric vehicle (or both), such as a biodegradable hyaluronic acid or PLGA (or PLA).
摘要翻译： 通过向液体或固体聚合物载体（或两者）中的抗新生血管性药物（例如贝伐珠单抗）的眼内部位给药，例如可生物降解的透明质酸（或两者），治疗干性年龄相关性黄斑变性（干性AMD）的组合物和方法 或PLGA（或PLA）。
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公开(公告)号：US08293741B2
公开(公告)日：2012-10-23
申请号：US11119021
申请日：2005-04-29
申请人： James A. Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Glenn Huang , Brittany A. Jackson , Larry A. Wheeler , Rosy S. Donn
发明人： James A. Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Glenn Huang , Brittany A. Jackson , Larry A. Wheeler , Rosy S. Donn
IPC分类号： A61K31/495
CPC分类号： A61L31/148 , A61K9/0051 , A61K9/204 , A61K31/498 , A61K47/34 , A61L27/58 , A61L31/06 , A61L31/16 , A61L2300/436 , A61L2300/604 , C08L67/04 , Y02A50/401
摘要： Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants can be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, among others or to improve vision in a normal eye.
摘要翻译： 生物相容性眼内植入物包括α-2肾上腺素能受体激动剂和与α-2肾上腺素能受体激动剂相关的聚合物，以促进α-2肾上腺素能受体激动剂延长一段时间的眼睛释放。 α-2肾上腺素能受体激动剂可以与可生物降解的聚合物基质例如两种可生物降解的聚合物的基质相关联。 植入物可以放置在眼睛中以治疗一种或多种眼部病症，例如眼睛血管病变或青光眼等，或改善正常眼睛的视力。
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公开(公告)号：US20120142652A1
公开(公告)日：2012-06-07
申请号：US13367070
申请日：2012-02-06
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 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。
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公开(公告)号：US20110182966A1
公开(公告)日：2011-07-28
申请号：US13011467
申请日：2011-01-21
IPC分类号： A61K9/00 , A61K31/216 , A61K31/192 , A61K31/165 , A61P27/06
CPC分类号： A61K9/0051 , A61K9/0024 , A61K9/1647 , A61K31/5575 , A61K47/10 , A61K47/34 , A61L27/18 , A61L27/54 , A61L27/58
摘要： Described herein are intracameral implants including at least one therapeutic agent for treatment of at least one ocular condition. The implants described herein are not anchored to the ocular tissue, but rather are held in place by currents and gravity present in the anterior chamber of an eye. The implants are preferably polymeric, biodegradable and provide sustained release of at least one therapeutic agent to both the trabecular meshwork and associated ocular tissue and the fluids within the anterior chamber of an eye.
摘要翻译： 本文描述的是包括用于治疗至少一种眼部病症的至少一种治疗剂的植入物植入物。 本文所述的植入物不固定在眼组织上，而是通过存在于眼前房中的电流和重力保持在适当位置。 植入物优选是聚合的，可生物降解的并且提供至少一种治疗剂持续释放到小梁网和相关联的眼组织和眼睛前房内的流体。
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公开(公告)号：US20100278898A1
公开(公告)日：2010-11-04
申请号：US12761765
申请日：2010-04-16
IPC分类号： A61F2/00 , A61K31/557
CPC分类号： A61K9/0051 , A61K9/204 , A61K31/165 , A61K31/557 , A61K31/5575 , A61K47/34
摘要： The present invention provides a method of treating an ocular condition in an eye of a patient, comprising the step of placing a biodegradable intraocular implant in an eye of the patient, the implant comprising a prostamide and a biodegradable polymer matrix that releases drug at a rate effective to sustain release of an amount of the prostamide from the implant to provide an amount of the prostamide effective to prevent or reduce a symptom of an ocular condition of the eye, wherein said ocular condition is elevated IOP and said implant is placed in an intracameral location to dilate the outflow channels of the eye emanating from Schlemm's Canal.
摘要翻译： 本发明提供了一种治疗患者眼睛中的眼部病症的方法，包括将可生物降解的眼内植入物放置在患者的眼睛中的步骤，所述植入物包含前列腺酰胺和可以以一定速率释放药物的可生物降解的聚合物基质 有效地维持从植入物中释放一定量的前列腺酰胺以提供一定量的前列腺酰胺，其有效预防或减少眼睛眼部症状，其中所述眼部病症升高IOP，并且所述植入物置于室内 位置，以扩大从施莱姆运河发出的眼睛的流出通道。
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公开(公告)号：US20080292679A1
公开(公告)日：2008-11-27
申请号：US11753419
申请日：2007-05-24
IPC分类号： A61F2/16
CPC分类号： A61K9/0051 , A61F9/0017 , A61F2210/0004 , A61F2250/0067 , A61K31/165 , A61K31/407 , A61K31/4436 , A61K31/498 , A61K31/5377 , A61K31/573 , A61K31/7072 , A61K38/13 , A61K47/34 , A61K2039/505 , C07K16/18
摘要： A drug delivery system (DDS) comprised of segmented biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The segmented implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer, and permit the DDS to have segments that possess individual and different drug release characteristics.
摘要翻译： 由分段生物降解植入物组成的药物递送系统（DDS），其尺寸适于植入眼部或部位，以及用于治疗眼部病症的方法。 分段植入物以治疗有效量提供活性剂在50天至1年或更长时间内的延长释放，并允许DDS具有具有单独和不同药物释放特征的片段。
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公开(公告)号：US20070167527A1
公开(公告)日：2007-07-19
申请号：US11563474
申请日：2006-11-27
申请人： James A. Burke , Kai-Ming Zhang
发明人： James A. Burke , Kai-Ming Zhang
IPC分类号： A61K31/13
CPC分类号： A61K31/13
摘要： A method for the treatment of disturbance of visual function which comprises administering a pharmaceutically effective amount of memantine to a patient in need of treatment of said disturbance.
摘要翻译： 一种用于治疗视功能紊乱的方法，其包括向需要治疗所述干扰的患者施用药学有效量的美金刚。
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8.发明授权Comformationally rigid bicyclic and adamantane derivatives useful as .alpha..sub.2 -adrenergic blocking agents 失效用作α2肾上腺素能阻断剂的组合刚性双环和金刚烷衍生物
公开(公告)号：US6150389A
公开(公告)日：2000-11-21
申请号：US3902
申请日：1998-01-07
IPC分类号： A61P3/04 , A61P3/10 , A61P15/10 , A61P25/24 , A61P27/02 , C07D233/50 , C07D233/54 , C07D263/28 , C07D277/18 , C07D413/12 , A61K31/421 , C07D263/08
CPC分类号： C07D413/12 , C07D233/50 , C07D263/28 , C07D277/18
摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.
摘要翻译： 式I化合物，其中：环A是所示的五种替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或立体异构体或其药学上可接受的盐。 这些化合物具有α2受体阻断活性，因此可用于治疗或缓解眼内压升高，非胰岛素依赖性糖尿病，男性阳ence和肥胖症。
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9.发明授权
公开(公告)号：US5561132A
公开(公告)日：1996-10-01
申请号：US390265
申请日：1995-02-15
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal comprising administering an effective amount of a compound of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, is disclosed wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms wherein the desired therapeutic effect is an alteration in the rate of fluid transport in the gastrointestinal tract.
摘要翻译： 公开了一种治疗哺乳动物的方法，其包括施用有效量的下式化合物及其药学上可接受的酸加成盐及其混合物，其中R 1和R 2各自选自含有1个 至4个碳原子和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以在喹喔啉核中的5-，6-，7-或8-位任何一个，R3，R4 并且R 5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自Cl，Br，H和含有1至3个碳原子的烷基，其中 期望的治疗效果是胃肠道中流体输送速率的改变。
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10.发明授权
公开(公告)号：US5231096A
公开(公告)日：1993-07-27
申请号：US820329
申请日：1992-01-13
IPC分类号： C07D403/12 , A61K31/495 , A61P7/10 , A61P9/08 , A61P9/10 , A61P27/02
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-,6,7或8-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个中，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少周围疼痛，中枢神经系统麻醉，一个或多个血管的收缩，减少或预防至少一种缺血作用，减压 一个或多个鼻通道，以及减少至少一种炎症性疾病的作用。
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