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Generated: February 18, 2018

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Claims for Patent: RE39155

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Summary for Patent: RE39155
Title:Use of 1,3-oxathiolane nucleoside analogues in the treatment of hepatitis B
Abstract:Use of a compound of formula (I) or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of hepatitis B is disclosed. ##STR00001##
Inventor(s): Belleau; Pierrette (Montreal, CA), Nguyen-Ba; Nghe (La Praire, CA), Belleau; Bernard (Westmont, CA)
Assignee: Shire BioChem Inc. (Quebec, CA)
Application Number:09/585,431
Patent Claims: 1. A method for the treatment of .Iadd.hepatitis B infection, in .Iaddend.a mammal, including a human, suffering from hepatitis B infection, comprising administration of an effective amount of a compound of formula (I) ##STR00005## or a pharmaceutically acceptable salt, ester, or salt of an ester thereof to said mammal.

2. The method according to claim 1 wherein the hepatitis B infection is human hepatitis B.

3. The method according to claim 1 wherein the compound of formula (I) comprises (.+-.)-cis-4-amino-1-( 2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one or a pharmaceutically acceptable salt, ester, or salt of an ester thereof.

4. The method according to claim 1 wherein the compound of formula (I) comprises (-)-cis-4-amino-1-( 2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one or a pharmaceutically acceptable salt, ester, or salt of an ester thereof.

5. The method according to claim 4 wherein the compound of formula (I) is substantially free of the corresponding (+)-enantiomer.

6. The method according to any one of claims 1 to 5 wherein the compound of formula (I) is adapted for oral administration.

7. The method according to any one of claims 1 to 5 wherein the compound of formula (I) is adapted for parenteral administration.

8. The method according to any one of claims 1 to 5 wherein the compound of formula (I) is in unit dosage form.

9. The method according to claim 8 wherein the compound is present in an amount of from 10 to 1500 mg.

.Iadd.10. A method for the treatment of hepatitis B infection, in a human, suffering from hepatitis B infection, comprising administering to said human an effective amount of a compound of formula (I) ##STR00006## or a pharmaceutically acceptable salt, ester, or salt of an ester thereof. .Iaddend.

.Iadd.11. The method according to claim 10, wherein the compound of formula (I) is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one or a pharmaceutically acceptable salt, ester or salt of an ester thereof. .Iaddend.

.Iadd.12. A method for the treatment of hepatitis B infection, in a human, suffering from hepatitis B infection, comprising administering to said human an effective amount of a compound of formula (I) ##STR00007## or a pharmaceutically acceptable salt thereof. .Iaddend.

.Iadd.13. The method according to claim 12, wherein the compound of formula (I) is (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one or a pharmaceutically acceptable salt thereof. .Iaddend.

.Iadd.14. The method according to claim 10, comprising administering a compound of formula (I). .Iaddend.

.Iadd.15. The method according to claim 13, comprising administering (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one. .Iaddend.

.Iadd.16. The method according to claim 11, wherein the (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one or pharmaceutically acceptable salt thereof is substantially free of the corresponding (+)-enantiomer. .Iaddend.

.Iadd.17. The method according to claim 13, wherein the (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one or pharmaceutically acceptable salt thereof is substantially free of the corresponding (+)-enantiomer. .Iaddend.

.Iadd.18. The method according to claim 15, wherein the (-)-cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-- one is substantially free of the corresponding (+)-enantiomer. .Iaddend.

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