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Details for Patent: 5,736,531

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Details for Patent: 5,736,531

Title: Compositions of chemotherapeutic agent or antiviral agent with acylated pyrimidine nucleosides
Abstract:The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents. Disclosed are acylated derivatives of non-methylated pyrimidine nucleosides. These compounds are capable of attenuating damage to the hematopoietic system in animals receiving antiviral or antineoplastic chemotherapy.
Inventor(s): von Borstel; Reid W. (Potomac, MD), Bamat; Michael K. (Potomac, MD)
Assignee: Pro-Neuron, Inc. (Rockville, MD)
Filing Date:Dec 30, 1993
Application Number:08/176,485
Claims:1. A composition comprising: an acyl derivative of uridine or cytidine; and an antineoplastic pyrimidine nucleoside analog, pyrimidine analog or inhibitor of pyrimidine biosynthesis.

2. A composition as in claim 1 wherein said antineoplastic pyrimidine nucleoside analog, pyrimidine analog or inhibitor of pyrimidine biosynthesis is selected from the group consisting of 5-fluorouracil (5FU), TEGAFUR.RTM. 5'-deoxy-5-fluorouridine 5-fluorouridine, 2'-deoxy-5-fluorouridine, fluorocytosine, 5-trifluoromethyl-2'-deoxyuridine, arabinoxyl cytosine, cyclocytidine, 5-aza-2'-deoxycytidine, arabinosyl 5-azacytosine, 6-azacytidine, N-phosphonoacetyl-L-aspartic acid (PALA), pyrazofurin, 6-azauridine, azaribine, and 3-deazauridine.

3. A composition as in claim 1, wherein said acyl derivative is an acyl derivative of cytidine, and said antineoplastic pyrimidine nucleoside analog is an analog of cytidine.

4. A composition as in claim 3 wherein said antineoplastic pyrimidine nucleoside analog is arabinosyl cytosine, cyclocytidine, 5-aza-2'-deoxycytidine, arabinosyl 5-azacytosine, or 6-azacytidine.

5. A composition as in claim 1, wherein said acyl derivative is an acyl derivative of cytidine, and said antineoplastic pyrimidine nucleoside analog is an analog of cytidine.

6. A composition as in claim 5 wherein said antineoplastic pyrimidine nucleoside analog of cytidine is arabinosyl cytosine, cyclocytidine, 5-aza-2'-deoxycytidine, arabinosyl 5-azacytosine, or 6-azacytidine.

7. A composition as in claim 1, wherein said acyl derivative is an acyl derivative of uridine, and said antineoplastic pyrimidine nucleoside analog is a fluorinated pyrimidine.

8. A composition as in claim 7 wherein said flurorinated pyrimidine is TEGAFUR.RTM., 5'-deoxy-5-fluorouridine, 5-fluorouracil, 5-fluorouridine, N.sup.4 -trimethoxybenzoyl-5'-deoxy-5-fluorocytidine, or 2'-deoxy-5-fluorouridine.

9. A composition as in claim 7, wherein the molar ratio of said acyl derivative of uridine to said fluorinated pyrimidine is 1:1 to 12:1.

10. A composition as in claim 7, wherein the molar ratio of said acyl derivative of uridine to said fluorinated pyrimidine is 2:1 to 8:1.

11. A composition as in claim 7, wherein the molar ratio of said acyl derivative of uridine to said fluorinated pyrimidine is 4:1.

12. A composition as in claim 7, wherein said acyl derivative of uridine is triacetyluridine, and said antineoplastic pyrimidine nucleoside analog is a fluorinated pyrimidine.

13. A composition as in claim 7, wherein said acyl derivative of uridine is triacetyluridine, and said antineoplastic pyrimidine nucleoside analog is tegafur.
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