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1.发明申请ADJUNCTS AND COMPLEXES FOR IMPROVING HMG-CoA REDUCTASE INHIBITOR (STATIN) AND SELECTIVE PHOSPHODIESTERASE 5 INHIBITOR THERAPY 审中-公开用于改善HMG-CoA还原酶抑制剂（STATIN）和选择性磷酸二酯酶5抑制剂治疗的结合物和复合物公开(公告)号：US20110104137A1
公开(公告)日：2011-05-05
申请号：US12762639
申请日：2010-04-19
IPC分类号： A61K31/122 , C07C279/14 , C07D475/04 , C07C49/753 , C07D339/04 , C07C215/40 , A61K31/385 , A61K31/519 , A61K31/205 , A61K31/40 , A61K31/496 , A61P15/10 , A61P3/00
CPC分类号： A61K9/2059 , A61K31/122 , A61K31/205 , A61K31/385 , A61K31/40 , A61K31/496 , A61K31/519 , A61K2300/00
摘要： Dosage forms and methods of use are disclosed for a) adjuncts administered individually or simultaneously with HMg-CoA reductase inhibitors (statins) and/or selective phosphodiesterase 5 inhibitors or, b) the administration of a conjugate consisting of the adjuncts and an HMG-CoA reductase inhibitor and/or a selective phosphodiesterase 5 inhibitor. The invention is useful in the amelioration of side effects associated with HMG-CoA reductase inhibitors and will improve their effectiveness in diseases for which these are useful. The invention will also improve the effectiveness in the of selective phosphodiesterase 5 inhibitors in patients using these medications alone or in conjunction with statins, for the treatment of erectile dysfunction.
摘要翻译： 公开了剂量形式和使用方法：a）与HMg-CoA还原酶抑制剂（他汀类）和/或选择性磷酸二酯酶5抑制剂单独或同时施用的辅助剂，或b）施用由辅助物和HMG-CoA组成的缀合物 还原酶抑制剂和/或选择性磷酸二酯酶5抑制剂。 本发明可用于改善与HMG-CoA还原酶抑制剂相关的副作用，并且将提高它们在有用的疾病中的有效性。 本发明还将改善使用这些药物单独使用或与他汀类药物联合用于治疗勃起功能障碍的患者中选择性磷酸二酯酶5抑制剂的有效性。
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2.发明授权公开(公告)号：US06693094B2
公开(公告)日：2004-02-17
申请号：US10093476
申请日：2002-03-07
IPC分类号： A61K31555
CPC分类号： A61K31/375 , A61K31/16 , A61K31/185 , A61K31/198 , A61K31/525 , A61K2300/00
摘要： The invention describes formulations that include either metformin, sulfonylurea or a biguanide-sulfonylurea combination as one active ingredient in addition to specific, other active ingredients. The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of the included biguanide (metformin) and/or sulfonylurea in the prevention and treatment of insulin resistance and diabetes mellitus. The carefully chosen additional active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and those adverse incidences associated with the concurrent use of metformin and/or the sulfonylureas. When clinically administered, the invention will provide therapeutic levels of metformin and of a sulfonylurea, alone or in combination, and broaden their usefulness. The invention will retard the progression of insulin resistance to type 2 diabetes, and reduce the serious microvascular and macrovascular complications commonly associated with insulin resistance syndrome and diabetes mellitus.
摘要翻译： 本发明描述除了特定的其它活性成分之外，还包括二甲双胍，磺酰脲或双胍磺酰脲组合作为一种活性成分的制剂。 本发明的组合物和剂型在临床上可用作增加包含的双胍（二甲双胍）和/或磺酰脲在预防和治疗胰岛素抵抗和糖尿病中的有效性，有效性和安全性的方法。 精心选择的本发明的另外的活性成分以模块化方式设计，以防止和纠正与胰岛素抵抗综合征和糖尿病相关的不良事件，以及与同时使用二甲双胍和/或磺酰脲相关的那些不良事件。 当临床施用时，本发明将提供单独或组合的二甲双胍和磺酰脲的治疗水平，并且扩大其用途。 本发明将阻止胰岛素抵抗2型糖尿病的进展，并减少通常与胰岛素抵抗综合征和糖尿病相关的严重微血管和大血管并发症。
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公开(公告)号：US06632445B2
公开(公告)日：2003-10-14
申请号：US10209432
申请日：2002-07-30
IPC分类号： A61E1300
CPC分类号： A61K31/7004 , A61K9/0034 , A61K9/0048 , A61K9/06 , A61K9/209 , A61K33/34 , A61K45/06 , Y10S514/944 , A61K33/30 , A61K33/04 , A61K31/375 , A61K31/19 , A61K31/195 , A61K2300/00
摘要： The components of this invention are chosen because of their complementarity for the prevention or treatment of diseases caused by the herpes simplex virus. L-Lysine favorably increases the physiologic immunomodulation necessary for defense against this virus. Zinc improves and maintains a normal immune response. 2-Deoxy-2-D-glucose and heparin sodium alter the surface interaction between the herpes virus and the cell, preventing fusion and infectivity. N-Acetyl-L-cysteine increases glutathione levels thereby creating a thiol redox barrier to the virus at the cell membrane. Quercetin reduces intracellular replication of the herpes virus and viral infectivity. Ascorbate, in concert with copper and D-&agr;-tocopherol, provides an antioxidant defense against the herpes virus, which tends to lose latency during period of oxidative, free radical excess. Selenium and quercetin also participate in reducing various oxidative stresses. Together the components of this invention provide the potential for improved resistance to, improved recovery from, and a decreased frequency of recurrence of herpes simplex virus infection.
摘要翻译： 选择本发明的组分是因为它们与预防或治疗由单纯疱疹病毒引起的疾病相互补充。 L-赖氨酸有利地增加防御这种病毒所必需的生理免疫调节。 锌改善并保持正常的免疫反应。 2-脱氧-2-D-葡萄糖和肝素钠改变疱疹病毒与细胞之间的表面相互作用，防止融合和感染。 N-乙酰基-L-半胱氨酸增加谷胱甘肽水平，从而在细胞膜上产生对病毒的硫醇氧化还原屏障。 槲皮素减少疱疹病毒的细胞内复制和病毒感染。 抗坏血酸盐与铜和D-α-生育酚一起提供抗疱疹病毒的抗氧化防御，这在氧化，自由基过量期间往往会失去潜伏期。 硒和槲皮素也参与减少各种氧化应激。 一起，本发明的组分提供改善抗单纯疱疹病毒感染复发的抗性，改善的恢复和降低的复发的潜力。
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4.发明授权Various thiol complexes, processes for their synthesis and clinical applications 失效各种硫醇复合物，其合成方法和临床应用公开(公告)号：US06531608B2
公开(公告)日：2003-03-11
申请号：US10167630
申请日：2002-06-11
IPC分类号： C07D27702
CPC分类号： A61K31/28 , A61K31/30 , A61K31/315 , A61K31/555
摘要： This invention relates to the synthesis of certain complexes of cysteine, N-acetylcysteine, N-(2-mercaptopropionyl)glycine, and L-2-oxothiazolidine-4-carboxylate and to the nutritional use of these and other related individual or complexed thiol-contributing glutathione predecessors. Clinical uses for these molecules and complexes in the beneficial modification of various physiological conditions and functions associated with aging, chronic glaucoma, diabetes mellitus, insulin resistance, macular degeneration, neurodegenerative diseases and vasoconstriction are described in particular.
摘要翻译： 本发明涉及半胱氨酸，N-乙酰半胱氨酸，N-（2-巯基丙酰基）甘氨酸和L-2-氧代噻唑烷-4-羧酸盐的某些复合物的合成，以及这些和其它相关的单独或络合的硫醇 - 贡献谷胱甘肽前身。 具体地描述了这些分子和复合物在与老化，慢性青光眼，糖尿病，胰岛素抵抗，黄斑变性，神经变性疾病和血管收缩相关的各种生理条件和功能的有益修饰中的临床应用。
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5.发明授权公开(公告)号：US06288106B1
公开(公告)日：2001-09-11
申请号：US09564074
申请日：2000-05-03
IPC分类号： A61K31385
CPC分类号： C07D307/62 , A61K31/385 , C07D339/04
摘要： This invention is in the fields of pharmacology and biochemistry. It relates to processes for the synthesis of certain complexes of &agr;-lipoic acid and the nutritional or therapeutic use of these and other related individual or complexed antioxidant, proglutathione molecules. Therapeutic uses for these molecules and complexes in the clinical management of conditions and functions associated with chronic glaucoma, insulin resistance, macular degeneration, lenticular cataract, neurodegenerative diseases, essential hypertension, atherosclerosis and vasoconstriction are described in particular.
摘要翻译： 本发明属于药理学和生物化学领域。 它涉及合成α-硫辛酸的某些复合物的方法以及这些和其它相关的个体或复合抗氧化剂，原始谷胱甘肽分子的营养或治疗用途。 具体地描述了在与慢性青光眼，胰岛素抵抗，黄斑变性，透镜状白内障，神经变性疾病，原发性高血压，动脉粥样硬化和血管收缩相关的条件和功能的临床管理中这些分子和复合物的治疗用途。
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公开(公告)号：US06231889B1
公开(公告)日：2001-05-15
申请号：US09396019
申请日：1999-09-15
IPC分类号： A61K600
CPC分类号： A61K31/7004 , A61K9/0034 , A61K9/0048 , A61K9/06 , A61K9/209 , A61K33/34 , A61K45/06 , Y10S514/944 , A61K33/30 , A61K33/04 , A61K31/375 , A61K31/19 , A61K31/195 , A61K2300/00
摘要： The components of this invention are chosen because of their complementarity for the prevention or treatment of diseases caused by the herpes simplex virus. L-Lysine favorably increases the physiologic immunomodulation necessary for defense against this virus. Zinc improves and maintains a normal immune response. 2-Deoxy-2-D-glucose and heparin sodium alter the surface interaction between the herpes virus and the cell, preventing fusion and infectivity. N-Acetyl-L-cysteine increases glutathione levels thereby creating a thiol redox barrier to the virus at the cell membrane. Quercetin reduces intracellular replication of the herpes virus and viral infectivity. Ascorbate, in concert with copper and D-&agr;-tocopherol, provides an antioxidant defense against the herpes virus, which tends to lose latency during period of oxidative, free radical excess. Selenium and quercetin also participate in reducing various oxidative stresses. Together the components of this invention provide the potential for improved resistance to, improved recovery from, and a decreased frequency of recurrence of herpes simplex virus infection.
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公开(公告)号：US06207190B1
公开(公告)日：2001-03-27
申请号：US09372362
申请日：1999-08-11
IPC分类号： A61K924
CPC分类号： A61K33/06 , A61K9/2059 , A61K33/04 , A61K31/505 , A61K31/455 , A61K31/385 , A61K31/375 , A61K31/355 , A61K31/195 , A61K31/185 , A61K2300/00
摘要： Four interdependent functional groups of biofactors and biomolecules are identified and formulations are defined which are comprised of their members. The active agents are demonstrated to be complementary in their physiological functions especially as these relate to endothelial biochemistry and physiology, hyperinsulinemia and, ultimately, to vascular health. The active components of the invention are selected for inclusion in precise combinations that reduce a variety of risks of vasculopathy in addition to reducing intraocular pressure. Widespread systemic improvement associated with local, optic nerve betterment of vascular health, reduces the risk of optic nerve atrophy with its accompanying visual field loss and potential blindness. The reduction of this maximizes the potential clinical therapeutic success of current medical, IOP-lowering, anti-glaucoma mediations.
摘要翻译： 确定生物因子和生物分子的四个相互依赖的官能团，并且定义由其成员组成的制剂。 活性剂被证明在其生理功能上是互补的，特别是因为这些涉及内皮生物化学和生理学，高胰岛素血症，最终涉及血管健康。 选择本发明的活性组分以包含在减少眼压以外的血管病变的各种风险的精确组合中。 与局部，视神经改善血管健康相关的广泛系统改善降低视神经萎缩的风险及伴随的视野丧失和潜在的失明。 减少这种现象可以最大限度地提高当前医学，眼压降低，抗青光眼中介的临床治疗成功。
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8.发明授权
公开(公告)号：US06042849A
公开(公告)日：2000-03-28
申请号：US111055
申请日：1998-07-07
IPC分类号： A61K33/06 , A61K33/24 , A61K31/355 , A61K31/34 , A61K31/40 , A61K31/495 , A61K31/50 , A61K33/04
CPC分类号： A61K33/06 , A61K33/24 , Y10S514/929
摘要： Magnesium is formulated in combination with vitamin E, vitamin C, folate, selenium, and optionally melatonin a unit dosage form for oral administration, for the treatment of vasoconstriction and the physiological and pathological conditions giving rise to vasoconstriction. These active agents complement each other in suppressing these conditions, using a variety of mechanisms operating in conjunction with one another. The inclusion of magnesium in a plurality of forms provides additional advantages in terms of controlling and sustaining the release of magnesium in locations along the digestive tract where the magnesium will have its greatest effectiveness as a therapeutic agent, thus improving control over the clinical bioavailability of magnesium and in improving the selection of appropriate therapeutic ranges.
摘要翻译： 镁与维生素E，维生素C，叶酸，硒和任选的褪黑激素一起配制成口服给药的单位剂型，用于治疗血管收缩和引起血管收缩的生理和病理状况。 这些活性剂通过使用彼此结合操作的各种机制来抑制这些条件相互补充。 以多种形式包含镁在控制和维持镁沿着消化道的位置的释放方面提供了额外的优点，其中镁将作为治疗剂具有最大的有效性，从而改善对镁的临床生物利用度的控制 并改善适当治疗范围的选择。
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公开(公告)号：US4255022A
公开(公告)日：1981-03-10
申请号：US948115
申请日：1978-10-02
申请人： Christian L. Kuether , Robert E. Williams , Thomas A. Decker , Charles Kurtzman , Kenneth T. Richardson , Richard A. Harrison
发明人： Christian L. Kuether , Robert E. Williams , Thomas A. Decker , Charles Kurtzman , Kenneth T. Richardson , Richard A. Harrison
CPC分类号： A61B3/024
摘要： A microprocessor based instrument designed to retrofit into existing perimeters utilizing the mechanics and stimulus control aspects of the existing perimeter. The device includes an array board positioned adjacent the perimeter mechanical arm and includes a multiplicity of visual indicators spatially arranged in a composite pattern of testing locations required for one or more ophthalmic testing procedures. A processor is connected to the array board for sequentially actuating the visual indicators in accordance with the testing procedure whereby the operator guides a cursor attached to the perimeter mechanical arm to align with the actuated indicators and control the location of the perimeter test stimulus. The processor includes means for sensing the position of the cursor, silently presenting a light flash to the patient, and a memory which records the patient's responses. When the program test sequence has been completed, the missed locations on the array board actuate allowing the examiner to manually record the data on a printed form. Switching means are provided whereby manual presentation of test stimuli may be provided, the patient's response overridden, and previous trials retested.
摘要翻译： 基于微处理器的仪器设计用于利用现有周边的力学和刺激控制方面来改造现有的周边。 该装置包括邻近周边机械臂定位的阵列板，并且包括空间上以一个或多个眼科测试程序所需的测试位置的复合图案空间布置的多个视觉指示器。 处理器连接到阵列板，用于根据测试程序顺序地启动视觉指示器，由此操作者引导附接到周边机械臂的光标以与致动指示器对准以及控制周边测试刺激的位置。 处理器包括用于感测光标的位置，静默地向患者呈现闪光的装置以及记录患者的响应的存储器。 当程序测试顺序完成时，阵列板上的错过的位置启动，允许检查者手动将数据记录在打印的表格上。 提供了切换手段，其中可以提供测试刺激的手动呈现，覆盖患者的反应以及先前的试验重新测试。
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公开(公告)号：US07351715B2
公开(公告)日：2008-04-01
申请号：US10627439
申请日：2003-07-25
CPC分类号： A61K31/7004 , A61K9/0034 , A61K9/0048 , A61K9/06 , A61K9/209 , A61K33/34 , A61K45/06 , Y10S514/944 , A61K33/30 , A61K33/04 , A61K31/375 , A61K31/19 , A61K31/195 , A61K2300/00
摘要： The components of this invention are chosen because of their complementarity for the prevention or treatment of diseases caused by the herpes simplex virus. L-Lysine favorably increases the physiologic immunomodulation necessary for defense against this virus. Zinc improves and maintains a normal immune response. 2-Deoxy-2-D-glucose and heparin sodium alter the surface interaction between the herpes virus and the cell, preventing fusion and infectivity. N-Acetyl-L-cysteine increases glutathione levels thereby creating a thiol redox barrier to the virus at the cell membrane. Quercetin reduces intraoellular replication of the herpes virus and viral infectivity. Ascorbate, in concert with copper and D-α-tocopherol, provides an antioxidant defense against the herpes virus, which tends to lose latency during period of oxidative, free radical excess. Selenium and quercetin also participate in reducing various oxidative stresses. Together the components of this invention provide the potential for improved resistance to, improved recovery from, and a decreased frequency of recurrence of herpes simplex virus infection.
摘要翻译： 选择本发明的组分是因为它们与预防或治疗由单纯疱疹病毒引起的疾病相互补充。 L-赖氨酸有利地增加防御这种病毒所必需的生理免疫调节。 锌改善并保持正常的免疫反应。 2-脱氧-2-D-葡萄糖和肝素钠改变疱疹病毒与细胞之间的表面相互作用，防止融合和感染。 N-乙酰基-L-半胱氨酸增加谷胱甘肽水平，从而在细胞膜上产生对病毒的硫醇氧化还原屏障。 槲皮素减少疱疹病毒的细胞内复制和病毒感染。 抗坏血酸盐与铜和D-α-生育酚一起提供抗疱疹病毒的抗氧化防御，这在氧化，自由基过量期间往往会失去潜伏期。 硒和槲皮素也参与减少各种氧化应激。 本发明的组分一起提供改善单纯疱疹病毒感染复发的抗性，改善的恢复和降低的复发频率的潜力。
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