发明名称 NOVEL PRO- AND CODRUG DERIVATIVES FOR NANOPARTICLE DELIVERY OF SELECT ANTICANCER AGENTS FORMED USING RAPIDLY CLEAVABLE PHENOLIC ESTER BRIDGES
摘要 An ester of ArOH according to the formula R-X-CO-OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O-CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R-X-CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R-X- is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety. A dispersion of nanoparticles in an aqueous medium includes nanoparticles including an ester of ArOH according to the formula R-X-CO-OAr wherein ArOH is a pharmaceutically active compound in which Ar is a substituted or unsubstituted aryl or heteroaryl radical, and wherein R is as defined above or R-X-CO-0 is as defined above. The ester or dispersion may be used to treat a diagnosed medical condition in a patient.
申请公布号 WO2013188727(A2) 申请公布日期 2013.12.19
申请号 WO2013US45772 申请日期 2013.06.14
申请人 THE CHILDREN'S HOSPITAL OF PHILADELPHIA 发明人 ALFERIEV, IVAN;CHORNY, MICHAEL;BRODEUR, GARRETT M.;LEVY, ROBERT J.
分类号 A61K31/58 主分类号 A61K31/58
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