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    • 3. 发明申请
    • MULTI-COMPONENT ANTIOXIDANT COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND THEIR USE FOR REDUCING OR PREVENTING OXIDATIVE STRESS
    • 多组分抗氧化剂,含有它们的药物组合物及其用于减少或预防氧化应激的用途
    • US20110190195A1
    • 2011-08-04
    • US13086429
    • 2011-04-14
    • Daphne ATLAS
    • Daphne ATLAS
    • A61K38/07C07K5/103A61P3/10A61P31/04A61P31/18A61P31/14A61P9/12A61P9/10A61P35/00A61P25/28A61P25/00A61P7/00A61P11/06A61P39/06
    • C07K5/081A61K38/00C07K5/0606C07K5/1013
    • An antioxidant compound is disclosed. The compound is characterized by (a) a peptide including at least three amino acid residues of which at least two are cysteine residues, each having a readily oxidizable sulfhydryl group for effecting antioxidation; and at least two peptide bonds, each being cleavable by at least one intracellular peptidase; and (b) a first hydrophobic or non-charged moiety being attached to an amino terminal of the peptide via a first bond and a second hydrophobic or non-charged moiety being attached to a carboxy terminal of the peptide via a second bond, the first hydrophobic or non-charged moiety and the second hydrophobic or non-charged moiety are selected so as to provide the antioxidant compound with membrane miscibility properties for permitting the antioxidant compound to cross cellular membranes; wherein cleavage of the at least two peptide bonds by the at least one intracellular peptidase results in generation of a plurality of antioxidant species, each including one of the cysteine residues having the readily oxidizable sulfhydryl group and which is also active in effecting antioxidation, thereby providing for a plurality of different antioxidant species acting in synergy in exerting antioxidation.
    • 公开了抗氧化剂化合物。 该化合物的特征在于:(a)包含至少三个氨基酸残基的肽,其中至少两个是半胱氨酸残基,每个氨基酸残基具有用于实现抗氧化的容易氧化的巯基; 和至少两个肽键,各自可被至少一个细胞内肽酶切割; 和(b)通过第一键连接到肽的氨基末端的第一疏水或非带电部分和通过第二键连接到肽的羧基末端的第二疏水或非带电部分,第一 选择疏水或非带电部分,并且选择第二疏水或非带电部分,以使抗氧化剂化合物具有膜混溶性,以允许抗氧化剂化合物跨越细胞膜; 其中由所述至少一种细胞内肽酶切割所述至少两个肽键导致产生多种抗氧化物质,每种抗氧化物质包含其中一个具有易氧化巯基的半胱氨酸残基,并且其还具有有效的抗氧化作用,从而提供 用于多种不同的抗氧化剂物质在协同作用中发挥抗氧化作用。
    • 6. 发明申请
    • Multi-component antioxidant compounds, pharmaceutical compositions containing same and their use for reducing or preventing oxidative stress
    • 多组分抗氧化剂,含有它们的药物组合物及其用于减少或预防氧化应激的用途
    • US20070287662A1
    • 2007-12-13
    • US11797590
    • 2007-05-04
    • Daphne Atlas
    • Daphne Atlas
    • A61K38/02A61P39/06
    • C07K5/081A61K38/00C07K5/0606C07K5/1013
    • An antioxidant compound is disclosed. The compound is characterized by (a) a peptide including at least three amino acid residues of which at least two are cysteine residues, each having a readily oxidizable sulfhydryl group for effecting antioxidation; and at least two peptide bonds, each being cleavable by at least one intracellular peptidase; and (b) a first hydrophobic or non-charged moiety being attached to an amino terminal of the peptide via a first bond and a second hydrophobic or non-charged moiety being attached to a carboxy terminal of the peptide via a second bond, the first hydrophobic or non-charged moiety and the second hydrophobic or non-charged moiety are selected so as to provide the antioxidant compound with membrane miscibility properties for permitting the antioxidant compound to cross cellular membranes; wherein cleavage of the at least two peptide bonds by the at least one intracellular peptidase results in generation of a plurality of antioxidant species, each including one of the cysteine residues having the readily oxidizable sulfhydryl group and which is also active in effecting antioxidation, thereby providing for a plurality of different antioxidant species acting in synergy in exerting antioxidation.
    • 公开了抗氧化剂化合物。 该化合物的特征在于:(a)包含至少三个氨基酸残基的肽,其中至少两个是半胱氨酸残基,每个氨基酸残基具有用于实现抗氧化的容易氧化的巯基; 和至少两个肽键,各自可被至少一个细胞内肽酶切割; 和(b)通过第一键连接到肽的氨基末端的第一疏水或非带电部分和通过第二键连接到肽的羧基末端的第二疏水或非带电部分,第一 选择疏水或非带电部分,并且选择第二疏水或非带电部分,以使抗氧化剂化合物具有膜混溶性,以允许抗氧化剂化合物穿过细胞膜; 其中由所述至少一种细胞内肽酶切割所述至少两个肽键导致产生多种抗氧化物质,每种抗氧化物质包含其中一个具有易氧化巯基的半胱氨酸残基,并且其还具有有效的抗氧化作用,从而提供 用于多种不同的抗氧化剂物质在协同作用中发挥抗氧化作用。
    • 8. 发明授权
    • Multi-component antioxidant compounds, pharmaceutical compositions containing same and their use for reducing or preventing oxidative stress
    • 多组分抗氧化剂,含有它们的药物组合物及其用于减少或预防氧化应激的用途
    • US08530407B2
    • 2013-09-10
    • US13455155
    • 2012-04-25
    • Daphne Atlas
    • Daphne Atlas
    • A61P11/06A61K38/00
    • C07K5/081A61K38/00C07K5/0606C07K5/1013
    • An antioxidant compound is disclosed, along with pharmaceutical compositions and methods of treatment which utilize said compound. The compound is characterized by a peptide including at least three amino acid residues of which at least two are cysteine residues, and a first hydrophobic or non-charged moiety being attached to an amino terminal of the peptide via a first bond and a second hydrophobic or non-charged moiety being attached to a carboxy terminal of the peptide via a second bond, as described herein. Cleavage of the peptide by an intracellular peptidase results in generation of a plurality of antioxidant species, each including one of the cysteine residues, thereby providing for a plurality of different antioxidant species acting in synergy in exerting antioxidation.
    • 公开了一种抗氧化剂化合物,以及利用所述化合物的药物组合物和治疗方法。 该化合物的特征在于包含至少三个氨基酸残基的肽,其中至少两个是半胱氨酸残基,并且第一疏水或非带电部分经由第一键连接到肽的氨基末端,第二疏水或非 - 非电荷部分通过第二键连接到肽的羧基末端,如本文所述。 通过细胞内肽酶切割肽导致产生多种抗氧化物质,每种抗氧化物质各自包含半胱氨酸残基之一,从而提供多种不同的抗氧化剂物质,以协同作用发挥抗氧化作用。