发明名称 6-substituted estradiol derivatives for use in remyelination of nerve axons
摘要 Disclosed is a method of remyelinating axons with 6-substituted estradiol compounds of the formula;;The methods can be used to treat a variety of demyelinating diseases.
申请公布号 US9636348(B2) 申请公布日期 2017.05.02
申请号 US201615179349 申请日期 2016.06.10
申请人 Endece LLC 发明人 Yarger James G.;Nye Steven H.
分类号 A61K31/568;A61K31/5685;A61K31/565;A61K31/57;A61K31/566;A61K45/06 主分类号 A61K31/568
代理机构 Reinhart Boerner Van Deuren s.c. 代理人 Reinhart Boerner Van Deuren s.c.
主权项 1. A method of treating demyelination and/or enhancing remyelination of an axon of a nerve cell that is in need of remyelination, comprising: providing a compound of a formula: wherein the “a” ring is R1, R2, R3 and R4 are independently selected from the group consisting of H, C1-C6 alkyl, halo, a sulfate, a glucuronide, and —OH; R11 is selected from the group consisting of H, C1-C6 alkyl, a sulfate, a glucoronide, —SO2NH2, —OSO2alkyl, and —NH2; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, —SH, —SCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)nCH3, —C2-C8 alkenyl-NH—(CH2)nCH3, —(CH2)m—OH, —(CH2)m—NH2, —(CH2)m—O—NH2, —(CH2)m—S—NH2, —NH(CH2)mCH3, —NH(CH2)mOCH3, —N(CH3)2, —(CH2)m(NH)CH2OH, and —(CH2)m N(CH3)—SO2—NH3; Y is selected from the group consisting of OH, and ═O; Z is selected from the group consisting of H and methyl; m is an integer selected from 0-20; n is an integer selected from 0-8; the symbol represents either a single or a double bond capable of forming a keto group at position 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, tautomers and pharmaceutically acceptable salts of said compounds; and contacting one or more progenitor cells with an effective amount of a said compound to differentiate the one or more progenitor cells to one or more cells that form myelin, thereby enhancing remyelination of the axon of a nerve cell.
地址 Mequon WI US