Orally active heparin salts containing multivalent cationic units

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United States of America Patent

PATENT NO 4703042
SERIAL NO

06808689

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention provides novel orally active salts of the formula ##STR1## in which .circle. is the skeleton of a polyol, n is the number of OH's in the polyol (3 to 24); p is .gtoreq.3 and .ltoreq.n; r is the available valence of the heparin unit and .gtoreq.3 and .ltoreq.7; sr is equal to pv; and R.sup.+ is ##STR2## in which R.sup.iv is C.sub.1 -C.sub.3 alkyl; R' and R' are C.sub.1 -C.sub.7 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 R.sup.v is H, --CONH.sub.2 or --COO(C.sub.1 -C.sub.7 alkyl). The salts are stable lipoidal 'ion pairs' or complexes which can be absorbed through the gastrointestional wall and which slowly release heparinic acid to achieve long-lasting anticoagulant activity. Novel quaternary salts which are intermediates to the heparin salts of the invention are also disclosed.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bodor, Nicholas S 7211 SW. 97th La., Gainesville, FL 32608 121 2006

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