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    Multifunctional Antioxidants and methods of use thereof
    4.
    发明授权
    Multifunctional Antioxidants and methods of use thereof 有权
    多功能抗氧化剂及其使用方法

    公开(公告)号：US08268849B2

    公开(公告)日：2012-09-18

    申请号：US12237936

    申请日：2008-09-25

    申请人： Peter F. Kador ,  Hongxia Jin

    发明人： Peter F. Kador ,  Hongxia Jin

    IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/02

    CPC分类号： C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/60 ,  C07D403/04

    摘要： Compositions comprising multifunctional agents and methods of use thereof are provided. Particularly, a series of analogs of 1-N, N′-dimethylsulfamoyl-4-(2-pyrimidyl)piperazine are provided which are useful for treating and/or preventing cataract, macular degeneration, neurodegenerative disorders, and/or injury or symptoms associated with radiation exposure.

    摘要翻译： 提供了包含多功能剂的组合物及其使用方法。 特别地，提供了一系列类似的1-N，N'-二甲基氨磺酰基-4-（2-嘧啶基）哌嗪，其可用于治疗和/或预防白内障，黄斑变性，神经变性疾病和/或相关的损伤或症状 与辐射暴露。

    Topical treatment of cataracts in dogs
    5.
    发明申请
    Topical treatment of cataracts in dogs 有权
    狗的白内障的局部治疗

    公开(公告)号：US20090082415A1

    公开(公告)日：2009-03-26

    申请号：US11892307

    申请日：2007-08-21

    申请人： Peter F. Kador ,  Milton Wyman ,  Daniel M. Betts

    发明人： Peter F. Kador ,  Milton Wyman ,  Daniel M. Betts

    IPC分类号： A61K31/4188

    CPC分类号： A61K9/0048 ,  A61K47/10 ,  A61K47/183 ,  A61K47/32 ,  A61K47/36 ,  A61K47/38

    摘要： The topical treatment of cataracts in dogs is a composition having an aldose reductase inhibitor (ARI) in a topical carrier. The ARI is preferably 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4′-imidazolidine]-2′,5′-dione, referred to as 2R-methyl sorbinil, having the structure: The topical carrier is formed from EDTA and deionized water containing about 2.5% carbomer, 1.5% glycerin, 0.02% EDTA and 0.1% benzalkonium chloride mixed to form a uniform emulsion. The concentration of the ARI in the topical carrier is preferably about 5-6%. The treatment includes administering to a dog an effective amount of the composition for preventing the formation of cataracts, reversing the formation of cataracts, and for treating diabetic retinopathy and pathological conditions resulting from diabetes affecting the cornea, iris, ciliary bodies, etc. The composition is preferably administered in the form of about two to four eye drops daily.

    摘要翻译： 在狗中局部治疗白内障是在局部载体中具有醛糖还原酶抑制剂（ARI）的组合物。 ARI优选为具有以下结构的2R，4S-6-氟-2-甲基 - 螺[苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，称为2R-甲基山bin素，其结构为： 载体由含有约2.5％卡波姆，1.5％甘油，0.02％EDTA和0.1％苯扎氯铵的EDTA和去离子水形成，形成均匀的乳液。 局部载体中ARI的浓度优选为约5-6％。 该治疗包括向狗施用有效量的用于防止白内障形成，逆转白内障形成，以及用于治疗糖尿病性视网膜病变的组合物和影响角膜，虹膜，睫状体等的糖尿病引起的病理状况。组合物 优选以每天约2至4滴眼液的形式施用。

    Topical treatment of cataracts in dogs
    6.
    发明授权
    Topical treatment of cataracts in dogs 有权
    狗的白内障的局部治疗

    公开(公告)号：US08158667B2

    公开(公告)日：2012-04-17

    申请号：US11892307

    申请日：2007-08-21

    申请人： Peter F. Kador ,  Milton Wyman ,  Daniel M. Betts

    发明人： Peter F. Kador ,  Milton Wyman ,  Daniel M. Betts

    IPC分类号： A01N43/52

    CPC分类号： A61K9/0048 ,  A61K47/10 ,  A61K47/183 ,  A61K47/32 ,  A61K47/36 ,  A61K47/38

    摘要： The topical treatment of cataracts in dogs is a composition having an aldose reductase inhibitor (ARI) in a topical carrier. The ARI is preferably 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4′-imidazolidine]-2′,5′-dione, referred to as 2R-methyl sorbinil, having the structure: The topical carrier is formed from EDTA and deionized water containing about 2.5% carbomer, 1.5% glycerin, 0.02% EDTA and 0.1% benzalkonium chloride mixed to form a uniform emulsion. The concentration of the ARI in the topical carrier is preferably about 5-6%. The treatment includes administering to a dog an effective amount of the composition for preventing the formation of cataracts, reversing the formation of cataracts, and for treating diabetic retinopathy and pathological conditions resulting from diabetes affecting the cornea, iris, ciliary bodies, etc. The composition is preferably administered in the form of about two to four eye drops daily.

    摘要翻译： 在狗中局部治疗白内障是在局部载体中具有醛糖还原酶抑制剂（ARI）的组合物。 ARI优选为具有以下结构的2R，4S-6-氟-2-甲基 - 螺[苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮，称为2R-甲基山bin素，其结构为： 载体由含有约2.5％卡波姆，1.5％甘油，0.02％EDTA和0.1％苯扎氯铵的EDTA和去离子水形成，形成均匀的乳液。 局部载体中ARI的浓度优选为约5-6％。 该治疗包括向狗施用有效量的用于防止白内障形成，逆转白内障形成，以及用于治疗糖尿病性视网膜病变的组合物和影响角膜，虹膜，睫状体等的糖尿病引起的病理状况。组合物 优选以每天约2至4滴眼液的形式施用。

    Antioxidant eye drops
    8.
    发明授权
    Antioxidant eye drops 有权
    抗氧化眼药水

    公开(公告)号：US09173915B1

    公开(公告)日：2015-11-03

    申请号：US14512365

    申请日：2014-10-10

    申请人： Peter F. Kador

    发明人： Peter F. Kador

    IPC分类号： A01N65/00 ,  A61K36/82 ,  A61K31/122 ,  A61K31/05 ,  A61K31/19 ,  A61K31/353 ,  A61K47/32 ,  A61K47/26 ,  A61K47/18 ,  A61K9/00 ,  A61K36/00

    CPC分类号： A61K36/00 ,  A61K9/0048 ,  A61K9/06 ,  A61K9/08 ,  A61K31/05 ,  A61K31/122 ,  A61K31/19 ,  A61K31/353 ,  A61K36/82 ,  A61K47/183 ,  A61K47/186 ,  A61K47/26 ,  A61K47/32 ,  A61P27/02 ,  A61P27/12 ,  A61K2300/00

    摘要： The antioxidant eye drops is a topical ophthalmic formulation that contains four nutraceuticals (namely, astaxanthin, resveratrol, pyruvate and epigallocatechin gallate (EGCG)) having antioxidant, anti-inflammatory, and chelating activity in a carbomer gel carrier. The active ingredients can reduce oxidative stress through free radical scavenging and chelating activity. The carrier is composed of a solution of deionized water containing about 0.4% Carbopol 980 NF, 5.7% sorbitol. 0.01% cetrimide, 0.01% EDTA, and sodium chloride and sodium hydroxide in adequate amounts to adjust both the viscosity and the pH of the topical carrier to pH 7.0-7.4. Use of the formulation may delay the development of cataracts, reduce retinal degeneration, and maintain normal tear flow in dry eye due to the antioxidant, anti-inflammatory, and chelating activity of the active ingredients.

    摘要翻译： 抗氧化剂滴眼剂是在卡波姆凝胶载体中具有抗氧化，抗炎和螯合活性的四种营养药物（即虾青素，白藜芦醇，丙酮酸和表没食子儿茶素没食子酸酯（EGCG））的局部眼用制剂。 活性成分可以通过自由基清除和螯合活性降低氧化应激。 载体由含有约0.4％Carbopol 980 NF，5.7％山梨糖醇的去离子水溶液组成。 0.01％的四氯化碳，0.01％的EDTA，以及足量的氯化钠和氢氧化钠，以将局部载体的粘度和pH调节至pH 7.0-7.4。 由于活性成分的抗氧化，抗炎和螯合活性，制剂的使用可能会延缓白内障的发展，减少视网膜变性，并维持干眼中正常的泪液流动。

    Neuroprotective multifunctional antioxidants and their monofunctional analogs
    9.
    发明授权
    Neuroprotective multifunctional antioxidants and their monofunctional analogs 有权
    神经保护多功能抗氧化剂及其单功能类似物

    公开(公告)号：US08877766B2

    公开(公告)日：2014-11-04

    申请号：US13769247

    申请日：2013-02-15

    申请人： Peter F. Kador

    发明人： Peter F. Kador

    IPC分类号： C07D401/04 ,  C07D239/60 ,  A61K31/505 ,  C07D239/52 ,  C07D403/04 ,  C07D239/47 ,  C07D239/42

    CPC分类号： C07D403/04 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D239/60 ,  C07D401/04

    摘要： The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.

    摘要翻译： 神经保护性多功能抗氧化剂是含有2-二乙酰氨基-5-羟基嘧啶部分的化合物，其具有以下结构式：其中R1是CH2或C2H4; R2是H或-OR4，其中R4是H或芳基; R3a和R3b独立地选自H和-O-烷基。 抗氧化剂是口服生物可利用的金属减弱多功能抗氧化剂，可以独立减弱过渡金属以及清道夫自由基。 多功能抗氧化剂通过独立地螯合金属（如Fe，Cu或Zn）和清除不同来源产生的自由基的能力是神经保护性的，并且有益于治疗各种神经障碍，例如阿尔茨海默病，帕金森病 ，ALS，创伤性脑损伤，眼部疾病如白内障，青光眼，年龄相关性黄斑变性和其他视网膜变性，以及用于减少糖尿病并发症的进展。

    Periodontitis treatment
    10.
    发明申请
    Periodontitis treatment 审中-公开
    牙周炎治疗

    公开(公告)号：US20100292287A1

    公开(公告)日：2010-11-18

    申请号：US12453557

    申请日：2009-05-14

    申请人： Peter F. Kador

    发明人： Peter F. Kador

    IPC分类号： A61K31/4184 ,  A61K31/352

    CPC分类号： A61K31/352 ,  A61K31/4184

    摘要： The periodontitis treatment is a method for the prevention and treatment of periodontitis in mammals, including humans and dogs. The mammal may be diabetic or non-diabetic. the method includes the step of administering an effective amount of an aldose reductase inhibitor (ARI). The ARI may be (i) a phenolic derivative, such as quercetin, quercitrin (a 3-oxy-glucose analog of quercetin), rutin, and other polyphenols or bioflavonoids exhibiting an ARI effect; (ii) an acetic acid derivative, such as tolrestat, ponalrestat, etc.; (iii) a cyclic imide (or hydantoin), such as sorbinil, 2-methyl sorbinil, imirestat, etc.; and (iv) one of the phenylsulfonyinitromethtane derivatives, such as ZD-5522. In particular embodiments, the method may include, e.g., administering a diet containing about 0.08% quercetin (about 80 mg/kg/day), about 0.0125% imirestat (about 12 mg/kg/day), or about 0.015% tolrestat (about 20 mg/kg/day).

    摘要翻译： 牙周炎治疗是预防和治疗包括人和狗在内的哺乳动物的牙周炎的方法。 哺乳动物可以是糖尿病或非糖尿病。 该方法包括施用有效量的醛糖还原酶抑制剂（ARI）的步骤。 ARI可以是（i）酚衍生物，例如槲皮素，槲皮素（槲皮素的3-氧 - 葡萄糖类似物），芦丁和其它表现出ARI效应的多酚或生物类黄酮; （ii）乙酸衍生物，如托伐他汀，潘那司他等; （iii）环状酰亚胺（或乙内酰脲），例如山bin素，2-甲基苯氧乙脒，灭胺剂等; 和（iv）苯基磺基亚硝基甲烷衍生物之一，例如ZD-5522。 在具体实施方案中，该方法可以包括例如施用含有约0.08％槲皮素（约80mg / kg /天），约0.0125％imirestat（约12mg / kg /天）或约0.015％tolrestat（约 20mg / kg /天）。