发明名称 Use of targeted nitroxide agents in mitigating or treating radiation injury
摘要 Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
申请公布号 US8822541(B2) 申请公布日期 2014.09.02
申请号 US201113006640 申请日期 2011.01.14
申请人 University of Pittsburgh—Of the Commonwealth System of Higher Education 发明人 Wipf Peter;Belikova Natalia A.;Jiang Jianfei;Pierce Joshua;Greenberger Joel;Epperly Michael;Kagan Valerian
分类号 A61K31/13 主分类号 A61K31/13
代理机构 Klarquist Sparkman, LLP 代理人 Klarquist Sparkman, LLP
主权项 1. A method of mitigating or treating radiation injury in a subject, or providing radioprotection to a subject, comprising administering to the subject prior to, during or after exposure of the subject to radiation, a composition comprising an amount of a targeted nitroxide compound effective to mitigate or treat radiation injury in the subject, or provide radioprotection to the subject; wherein the targeted nitroxide compound has the structurewherein X is one of R1, and R2 are hydrogen, or a C1-C6 straight or branched-chain alkyl; R4 is hydrogen, C1-C6 straight or branched-chain alkyl, or a C1-C6 straight or branched-chain alkyl further comprising a phenyl (C6H5) group, that is unsubstituted or is methyl-, hydroxyl- or fluoro-substituted; R3 is —NH—R5, —O—R5 or —CH2—R5, and R5 is an —N—O., —N—OH or N═O containing group; R is —C(O)—R6, —C(O)O—R6, or —P(O)—(R6)2, wherein R6 is C1—C6 straight or branched-chain alkyl or C1—C6 straight or branched-chain alkyl further comprising one or more phenyl (—C6H5) groups that are independently unsubstituted, or methyl-, ethyl-, hydroxyl- or fluoro-substituted.
地址 Pittsburgh PA US