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Claims for Patent: 6,258,795

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Claims for Patent: 6,258,795

Title: Acylated uridine and cytidine and uses thereof
Abstract:The invention relates to compositions comprising acyl derivatives of cytidine and uridine. The invention also relates to methods of treating hepatopathies, diabetes, heart disease, cerebrovascular disorders, Parkinson's disease, infant respiratory distress syndrome and for enhancement of phospholipid biosynthesis comprising administering the acyl derivatives of the invention to an animal.
Inventor(s): von Borstel; Reid Warren (Darnestown, MD), Bamat; Michael Kevin (Darnestown, MD)
Assignee: Pro-Neuron, Inc. (Gaithersburg, MD)
Application Number:08/466,145
Patent Claims: 1. An acyl derivative of uridine having the formula (II) ##STR4##

wherein R.sub.1, R.sub.2, and R.sub.3 are the same or different and each is hydrogen or an acyl radical of

(a) an unbranched fatty acid with 5 to 22 carbon atoms,

(b) an amino acid selected from the group consisting of glycine, L-forms of alanine, valine, leucine, isoleucine, tyrosine, proline, hydroxyproline, serine, threonine, cystine, cysteine, aspartic acid, glutamic acid, arginine, lysine, histidine, carnitine, and ornithine,

(c) a dicarboxylic acid of 3 to 22 carbon atoms, or

(d) a carboxylic acid selected from one or more of the group consisting of glycolic acid, pyruvic acid, lactic acid, enolpyruvic acid, lipoic acid, pantothenic acid, acetoacetic acid, p-aminobenzoic acid, betahydroxybutyric acid, orotic acid, and creatine,

provided that at least one of said substituents R.sub.1, R.sub.2, and R.sub.3 is not hydrogen, and further provided that if any of said substituents R.sub.1, R.sub.2, and R.sub.3 is hydrogen and if said remaining substituents are acyl radicals of a straight chain fatty acid, then said straight chain fatty acid has 8 to 22 carbon atoms, or a pharmaceutically acceptable salt thereof.

2. An acyl derivative of uridine having the formula (I) ##STR5##

wherein R.sub.1, R.sub.2, and R.sub.3 are the same or different and each is hydrogen or an acyl radical of a carboxylic acid selected from one or more of the group consisting of a fatty acid of 2 to 22 carbon atoms, glycolic acid, pyruvic acid, lactic acid, enolpyruvic acid, an amino acid, lipoic acid, pantothenic acid, succinic acid, fumaric acid, adipic acid, acetoacetic acid, p-aminobenzoic acid, betahydroxybutyric acid, orotic acid, and creatine, and R.sub.4 is an acyl radical of a carboxylic acid selected from one or more of the group consisting of a fatty acid of 2 to 22 carbon atoms, glycolic acid, pyruvic acid, lactic acid, enolpyruvic acid, and amino acid, lipoic acid, pantothenic acid, succinic acid, fumaric acid, adipic acid, acetoacetic acid, p-aminobenzoic acid, betahydroxybutyric acid, orotic acid, and creatine, or a pharmaceutically acceptable salt thereof.

3. The acyl derivative of claim 2 wherein said amino acid is selected from the group consisting of glycine, the L forms of alanine, valine, leucine, isoleucine, proline, phenylalanine, tyrosine, cysteine, cystine, methionine, tryptophan, aspartic acid, glutamic acid, arginine, lysine, histidine, ornithine, carnitine, and hydroxylysine.

4. A composition comprising the acyl derivative of claim 1 and a pharmaceutically acceptable carrier.

5. A unit dose of the composition of claim 4 comprising an amount of said acyl derivative being the equivalent of 10-3000 mg of uridine.

6. A composition comprising a mixture of at least one acyl derivative of claim 1, at least one acyl derivative of cytidine selected from the group consisting of 2',3',5'-tri-O-acetyl cytidine, 2',3',5'-tri-O-propionyl cytidine, or 2',3',5'-tri-O-butyryl cytidine and a pharmaceutically acceptable carrier.

7. A unit dose of the composition of claim 6 comprising amounts of said acyl derivatives being the equivalent of 10-3000 mg of uridine and 10-3000 mg of cytidine.

8. The composition of claim 4 in the form of a liquid, a suspension, a tablet, a dragee, an injectable solution, or a suppository.

9. A composition as recited in claim 1 wherein said acyl derivative of uridine is 2',3',5'-tri-O-acetyl uridine, 2',3',5'-tri-O-propionyl uridine, or 2',3',5'-tri-O-butyryl uridine.

10. A pharmaceutical composition comprising an acyl derivative of uridine having the formula (I) ##STR6##

wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is hydrogen or an acyl radical of a carboxylic acid selected from the group consisting of glycolic acid, pyruvic acid, lactic acid, enolpyruvic acid, an amino acid, a fatty acid of 2 to 22 carbon atoms, lipoic acid, pantothenic acid, succinic acid, fumaric acid, adipic acid, acetoacetic acid, p-aminobenzoic acid, betahydroxybutyric acid, orotic acid, and creatine, provided that at least one of said R substituents is not hydrogen, or a pharmaceutically acceptable salt thereof,

and a pharmaceutically acceptable carrier,

wherein said composition is in the form of an oral suspension, tablet, dragee or capsule.

11. A pharmaceutical composition comprising an acyl derivative of cytidine having the formula (III) ##STR7##

wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is hydrogen or an acyl radical of a carboxylic acid selected from the group consisting of glycolic acid, pyruvic acid, lactic acid, enolpyruvic acid, an amino acid, a fatty acid of 2 to 22 carbon atoms, lipoic acid, pantothenic acid, succinic acid, fumaric acid, adipic acid, acetoacetic acid, p-aminobenzoic acid, betahydroxybutyric acid, orotic acid, and creatine, provided that at least one of said R substituents is not hydrogen, and R.sub.4 is an amino acid, or a pharmaceutically acceptable salt thereof,

and a pharmaceutically acceptable carrier,

wherein said composition is in the form of an oral suspension, tablet, dragee or capsule.

12. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a filler selected from the group consisting of a sugar, a cellulose preparation and a calcium phosphate.

13. A composition as in claim 12 wherein said sugar is lactose, sucrose, mannitol or sorbitol.

14. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a binder selected from the group consisting of maize starch, wheat starch, rice starch, potato starch, gelatin, tragacanth, methyl cellulose, hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose, and polyvinyl pyrrolidone.

15. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is selected from the group consisting of carboxymethylstarch, cross-linked polyvinyl pyrrolidone, agar, or alginic acid or a salt thereof.

16. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a flow-regulating agent or lubricant selected from the group consisting of silica, talc, stearic acid or salts thereof, and polyethylene glycol.

17. A composition as in claim 16 wherein said salt is magnesium stearate or calcium stearate.

18. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a coating selected from the group consisting of sugar solutions which optionally contain gum arabic, talc, polyvinyl pyrrolidone, polyethylene glycol and/or titanium dioxide, lacquer solutions, and a cellulose preparation.

19. A composition as in claim 18 wherein said cellulose preparation is acetylcellulose phthalate or hydroxylpropylmethylcellulose phthalate.

20. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is gelatin.

21. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a base selected from the group consisting of triglycerides, paraffin hydrocarbons, polyethylene glycols and higher alkanols.

22. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is a lipophilic solvent or vehicle selected from the group consisting of fatty oils and fatty acid esters.

23. A composition as in claim 10 or 11 wherein said pharmaceutically acceptable carrier is an aqueous injection suspension selected from the group consisting of sodium carboxymethylcellulose, sorbitol, and dextran.
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