| 摘要 |
<p>Novel orally active ion multiplets of formula (I) in which $(1,5)$ is the skeleton of a polyol, n is the number of OH's in the polyol (3 to 24); p is >= 3 and <= n; r is the available valence of the heparin unit and is >= 3 and <= 7; sr is equal to pv; and R+ is (a), (b), (c), (d) or (e), in which Riv is C1-C3 alkyl; R' and R" are C1-C7 alkyl, the same or different, or combined so that -NR'R" represents the residue of a saturated monocyclic secondary amine; R''' is identical to the corresponding portion of a natural amino acid; the alkylene groups contain 1 to 3 carbon atoms; and Rv is H, -CONH¿2? or -COO(C1-C7 alkyl). The multiplets are stable lipoidal "ion-pairs" or complexes which can be absorbed through the gastrointestinal wall and which slowly release heparinic acid to achieve long-lasting anticoagulant activity. Novel quarternary salts which are intermediates to the multiplets of the invention are also disclosed.</p> |
