C - Chemistry – Metallurgy – 08 – B
Patent
C - Chemistry, Metallurgy
08
B
260/226, 260/220
C08B 37/10 (2006.01) C07D 213/55 (2006.01) C07D 213/80 (2006.01) C07D 213/82 (2006.01) C07D 295/15 (2006.01) C07H 3/04 (2006.01) C07H 3/06 (2006.01) C07H 13/04 (2006.01) C07H 13/10 (2006.01)
Patent
CA 1268456
Abstract of the Disclosure The invention provides novel orally active ion multiplets of the formula Image (I) in which Image 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 > 3 and < 7; sr is equal to pv; and R+ is Image (a) (b) (c) Image or Image (d) (e) in which RiV is C1-C3 alkyl; R' and R" are C1-C7 alkyl, the same of different, or combined so that -NR'R" represents the residue of a saturated monocy- clic secondary amine; R''' is identical to the corres- onding portion of a natural amino acid; the alkylene groups contain 1 to 3 carbon atoms; and Rv is H, -CONH2 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 rlease heparinic acid to achieve long-lasting antico- agulant activity. Novel quaternary salts which are intermediates to the multiplets of the invention are also disclosed.
481938
Bodor Nicholas S.
Swabey Ogilvy Renault
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