申请人:Hoechst-Roussel Pharmaceuticals Incorporated
公开号:US05360811A1
公开(公告)日:1994-11-01
Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols of the formula RCH(OR.sup.1)CH(NR.sup.2 R.sup.3)R.sup.4 or RCH.sub.2 CR.sup.35 (NR.sup.2 R.sup.3)R.sup.4 wherein R is ##STR1## wherein R.sup.5 is CH.sub.3 (CH.sub.2).sub.m C.tbd.C, CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH,CH.sub.3 (CH.sub.2).sub.m CH.sub.2 CH.sub.2, ##STR2## wherein m is 3 to 15, n is 0 to 12, and W and X are independently hydrogen, hydroxy, alkyl, alkoxy, halogen, or trifluoromethyl, ##STR3## wherein R.sup.23 loweralkyl; Z is S, O, or C.dbd.O; and A is S or O; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.35 and R.sup.40 are as defined in the specification, the optical isomers thereof, or the pharmaceutically acceptable salts thereof, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
1-烷基、1-烯基和1-炔基芳基-2-氨基-1,3-丙二醇的公式为RCH(OR1)CH(NR2R3)R4或RCH2CR35(NR2R3)R4,其中R是##STR1##,其中R5是CH3(CH2)mC≡C,CH3(CH2)mCH═CH,CH3(CH2)mCH2CH2,##STR2##,其中m是3到15,n是0到12,W和X独立的是氢、羟基、烷基、烷氧基、卤素或三氟甲基,##STR3##,其中R23是较低烷基;Z是S、O或C═O;A是S或O;R1、R2、R3、R4、R35和R40按说明书定义,其光学异构体,或其药物可接受的盐,中间体及其制备方法,以及用于减少炎症和细胞增殖,缓解记忆功能障碍,抑制细菌和真菌生长的方法被披露。