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Details for Patent: 7,244,718

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Details for Patent: 7,244,718

Title:Water soluble prodrugs of hindered alcohols
Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.
Inventor(s): Stella; Valentino J. (Lawrence, KS), Zygmunt; Jan J. (Longmont, CO), Georg; Ingrid Gunda (Lawrence, KS), Safadi; Muhammad S. (Nazareth, IL)
Assignee: University of Kansas (Lawrence, KS)
Filing Date:Nov 17, 2004
Application Number:10/991,348
Claims:1. A method of producing an anesthetic effect in a dog which comprises administering to a dog in need thereof an effective anesthetic amount of the compound according to formula I, ##STR00054## wherein, R-O is a residue of propofol, R.sup.1 is hydrogen or an alkali metal ion or a protonated amine or a protonated amino acid, R.sup.2 is hydrogen or an alkali metal ion or a protonated amine or a protonated amino acid, and n is an integer of 1 or 2; and pharmaceutically acceptable salts thereof.

2. The method according to claim 1, wherein the alkali metal ion of R.sup.1 and R.sup.2 is independently selected from the group consisting of sodium, potassium and lithium.

3. The method according to claim 1, wherein said compound has the formula II, ##STR00055## Wherein Z is selected from the group consisting of hydrogen, alkali metal ion and amine, and n is an integer of 1 or 2; and pharmaceutically acceptable salts thereof.

4. The method according to claim 3, wherein Z is independently selected from the group consisting of sodium, tromethamine, triethanolamine, triethylamine, arginine, lysine, ethanolamine and N-methylglucamine.

5. The method according to claim 1, wherein said compound has the formula (III), ##STR00056## wherein R-O is a residue of propofol Y is a phosphono protecting group, and n is an integer of 1 or 2; and pharmaceutically acceptable salts thereof.

6. The method according to claim 5, wherein the compound has the formula IV, ##STR00057## wherein Y is a phosphono protecting group.

7. The method according to claim 6, wherein said phosphono protecting group is selected from the group consisting of a benzyl group, a t-butyl group, an allyl group, and other acceptable phosphate protecting groups.
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