A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.
申请公布号
WO2004064743(A2)
申请公布日期
2004.08.05
申请号
WO2004US01324
申请日期
2004.01.16
申请人
WISCONSIN ALUMNI RESEARCH FOUNDATION;DELUCA, HECTOR, F.;CLAGETT-DAME, MARGARET;GOWLUGARI, SUMITHRA