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1. 发明公开

EP2956140A4 NEUROPROTECTIVE MULTIFUNCTIONAL ANTIOXIDANTS AND THEIR MONOFUNCTIONAL ANALOGS 有权
标题翻译：多功能神经保护抗氧化剂
公开(公告)号：EP2956140A4
公开(公告)日：2016-06-29
申请号：EP13875125
申请日：2013-03-18
申请人： KADOR PETER F
发明人： KADOR PETER F
IPC分类号： A61K31/506 , A61P25/00 , A61P39/06 , C07D401/04 , C07D403/04
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，具有以下结构式：其中R 1是CH 2或C 2 H 4; R2是H或-OR4，其中R4是H或芳基; 并且R 3a和R 3b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其独立螯合金属（如Fe，Cu或Zn）和清除由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，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。

2. 发明授权

EP3203993B1 ANTIOXIDANT EYE DROPS 有权
公开(公告)号：EP3203993B1
公开(公告)日：2021-07-21
申请号：EP15849725.5
申请日：2015-10-09
发明人： Kador, Peter F.
IPC分类号： A61K9/06 , A61K9/08 , A61K47/18 , A61K47/26 , A61K47/32 , A61K31/05 , A61K31/122 , A61K31/22 , A61K31/353 , A61K36/82 , A61P27/02 , A61P27/12

3. 发明授权

EP2956140B1 NEUROPROTECTIVE MULTIFUNCTIONAL ANTIOXIDANTS AND THEIR MONOFUNCTIONAL ANALOGS 有权
公开(公告)号：EP2956140B1
公开(公告)日：2018-07-11
申请号：EP13875125.0
申请日：2013-03-18
申请人： Kador, Peter F.
发明人： Kador, Peter F.
IPC分类号： A61K31/506 , C07D403/04 , C07D401/04 , A61P25/00 , A61P39/06
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.

4. 发明公开

EP2956140A1 NEUROPROTECTIVE MULTIFUNCTIONAL ANTIOXIDANTS AND THEIR MONOFUNCTIONAL ANALOGS 有权
标题翻译：多功能神经保护抗氧化剂MONO及其功能类似物
公开(公告)号：EP2956140A1
公开(公告)日：2015-12-23
申请号：EP13875125.0
申请日：2013-03-18
申请人： Kador, Peter F.
发明人： Kador, Peter F.
IPC分类号： A61K31/506 , C07D403/04 , C07D401/04 , A61P25/00 , A61P39/06
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.

5. 发明公开

EP3203993A4 ANTIOXIDANT EYE DROPS 有权
公开(公告)号：EP3203993A4
公开(公告)日：2018-05-23
申请号：EP15849725
申请日：2015-10-09
申请人： KADOR PETER F
发明人： KADOR PETER F
IPC分类号： A61K9/06 , A61K9/08 , A61K31/05 , A61K31/122 , A61K31/19 , A61K31/353 , A61K36/82 , A61K47/18 , A61K47/26 , A61K47/32 , A61P27/02 , A61P27/12
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.

6. 发明公开

EP3203993A1 ANTIOXIDANT EYE DROPS 有权
标题翻译：抗氧化眼药水
公开(公告)号：EP3203993A1
公开(公告)日：2017-08-16
申请号：EP15849725.5
申请日：2015-10-09
申请人： Kador, Peter F.
发明人： Kador, Peter F.
IPC分类号： A61K31/14 , A61K36/82 , A61K31/19 , A61K31/05 , A61K9/08 , A61K47/10
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：抗氧化剂滴眼剂是含有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制品（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。活性成分可通过自由基清除和螯合活性降低氧化应激。该载体由含有约0.4％Carbopol 980NF，5.7％山梨糖醇的去离子水溶液组成。 0.01％西曲溴铵，0.01％EDTA和适量的氯化钠和氢氧化钠调节局部载体的粘度和pH至pH 7.0-7.4。由于活性成分的抗氧化，抗炎和螯合活性，该制剂的使用可以延缓白内障的发展，减少视网膜变性，并维持干眼中的正常眼泪流动。

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