Compounds with sulphonamide group and pharmaceutical compositions containing these compounds
申请人:——
公开号:US20040014781A1
公开(公告)日:2004-01-22
The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.
本发明涉及的化合物作为原药和/或支持物,可使活性剂被红细胞吸收和/或使活性剂与红细胞结合。这些化合物被红细胞吸收和/或与红细胞结合是通过式 -SO2NR1R2 的基团实现的,其中 R1 和 R2 相互独立地表示氢原子、酰基、烷基、环烷基、芳基、氰基或羟基。本发明的原药可以有效地口服具有高 "第一路径 "效应的活性剂,如内源性物质、天然物质和具有治疗作用的合成物质,或显著提高其口服活性。