发明名称 GLYCOSYLATED VALPROIC ACID ANALOGS AND USES THEREOF
摘要 Glycosylated valproic acid and its analogs are provided. In some embodiments, the glycosylated valproic acid and its analogs have improved solubility and are ideal for drug delivery to treat a variety of diseases.
申请公布号 US2015119346(A1) 申请公布日期 2015.04.30
申请号 US201414584571 申请日期 2014.12.29
申请人 Chromatin Technologies 发明人 HEYMAN Norman S.;SHULL Brian K.
分类号 C07H15/04 主分类号 C07H15/04
代理机构 代理人
主权项 1. A compound of formula I, II, III, IV, V, or VI: wherein R1 is saccharide; R2 is C1-10 alkyl or alkene having one carbon substituted by 1-3 of halogen atoms, amino, hydroxy, carboxylic acid group, ester, amide, or cyano wherein one or more of the hydroxy, carboxylic acid or amide group is optionally glycosylated with a saccharide group; R3 is H, halo or loweralkyl; each R4 and R5 is independently amine, cyano, hydroxyl, or carboxylic acid each of which may be glycosylated; Rx is oxo or hydroxy; each of R6 and R7 is independently a linear or branched, saturated or partially unsaturated aliphatic C2-C20 hydrocarbon chain; each of R8 and R9 is independently a linear or branched aliphatic C2-C20 hydrocarbon chain which is optionally substituted with a C3-C9 aliphatic or aromatic cyclohydrocarbon or heterocyclic group or having 1-3 substituents independently selected from the group consisting of halogen atoms, amino, hydroxy, carboxylic acid group, ester, amide, and cyano wherein one or more of the hydroxy, carboxylic acid, amine, or amide group is optionally glycosylated with a saccharide group; R10 is —C≡CH, —CH═CH2, or —CH2—CH3; R11 is a saturated, unsaturated with at least one double or triple bond, branched or unbranched C1-30 alkyl group, optionally substituted with an aliphatic or aromatic C3-9 cyclohydrocarbon or heterocyclic group; Y is a bond or —CH2-aryl-O—, wherein the aryl group is optionally substituted with one or more substituents independently selected from C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 thioalkyl, —N(C1-C3 alkyl)(C1-C3 alkyl), —NH(C1-C3 alkyl), —NH2, —NO2, and —CN; each of m and n is independently an integer having a value of 0, 1, 2, 3, 4, 5, or 6; and o is 1, 2, or 3; or a pharmaceutically acceptable salt or prodrug thereof.
地址 New York NY US