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Generated: August 23, 2019

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Claims for Patent: 7,902,202

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Summary for Patent: 7,902,202
Title:Compounds and pharmaceutical compositions for the treatment of viral infections
Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
Inventor(s): Sommadossi; Jean-Pierre (Cambridge, MA), Gosselin; Gilles (Montpellier, FR), Pierra; Claire (Montarnaud, FR), Perigaud; Christian (Grabels, FR), Peyrottes; Suzanne (Grabels, FR)
Assignee: Idenix Pharmaceuticals, Inc. (Cambridge, MA) L\'Universite Montpellier II (Montpellier, FR)
Application Number:12/150,327
Patent Claims:1. A compound of the formula: ##STR00278## or a pharmaceutically acceptable salt, a stereoisomeric, or tautomeric form thereof, wherein: R.sup.y is alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkenyl, amino, heterocyclyl or heteroaryl; R.sup.a and R.sup.b are selected as follows: i) R.sup.a and R.sup.b are each independently hydrogen, alkyl, carboxyalkyl, hydroxyalkyl, hydroxyarylalkyl, acyloxyalkyl, aminocarbonylalkyl, alkoxycarbonylalkyl, aryl, arylalkyl, cycloalkyl, heteroaryl or heterocyclyl; or ii) R.sup.a and R.sup.b together with the nitrogen atom on which they are substituted form a 3-7 membered heterocyclic or heteroaryl ring; A is H, alkyl, alkenyl, alkynyl, azido, carboxylic acid, CO.sub.2-alkyl, cyano, or carboxamide; and R.sup.L is independently H, carbamyl, alkyl; acyl; CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, a lipid, an amino acid or a carbohydrate.

2. The compound of claim 1, wherein R.sup.L is hydrogen, R.sup.y is optionally substituted alkyl and R.sup.a and R.sup.b are each independently hydrogen, optionally substituted alkyl or optionally substituted benzyl.

3. The compound of claim 1, wherein R.sup.L is hydrogen; R.sup.y is hydroxyalkyl, aminoalkyl, hydroxyaryl or aminoaryl; and R.sup.a and R.sup.b are each independently hydrogen, alkyl, hydroxyalkyl or aminoalkyl.

4. The compound of claim 1, wherein R.sup.L is hydrogen; R.sup.y is hydroxyalkyl, aminoalkyl, hydroxyaryl, aminoaryl; and R.sup.a and R.sup.b are each independently hydrogen, benzyl, hydroxybenzyl or aminobenzyl.

5. The compound of claim 1, wherein R.sup.L is hydrogen, and R.sup.a and R.sup.b are independently substituted alkyl.

6. The compound of claim 1, wherein R.sup.y is selected from the group consisting of alkyl and hydroxyalkyl.

7. The compound of claim 1 having the formula: ##STR00279##

8. The compound of claim 1 having the formula: ##STR00280## wherein R.sup.b1 is halo, alkoxy or haloalkyl.

9. The compound of claim 8 having the formula: ##STR00281##

10. A compound of the formula: ##STR00282## or a pharmaceutically acceptable salt, a stereoisomeric, or tautomeric form thereof.

11. The compound of claim 1 having the formula: ##STR00283##

12. A method for the treatment of a host infected with a Flaviviridae virus or hepatitis B virus, comprising administering an effective treatment amount of a compound of claim 1 or 10.

13. A method for the treatment of a host infected with a Flaviviridae virus or hepatitis B virus, comprising contacting a cell infected with the virus with a compound of claim 1 or 10.

14. The method of claim 12, wherein the virus is hepatitis C.

15. The method of claim 12, wherein the host is a human.

16. The method of claim 12, wherein the compound is ##STR00284## or a pharmaceutically acceptable salt or stereoisomer thereof.

17. The method of claim 12, wherein the compound is ##STR00285## or a pharmaceutically acceptable salt or stereoisomer thereof.

18. The method of claim 12, wherein said administration directs a substantial amount of said compound or pharmaceutically acceptable salt or stereoisomer thereof to the liver of said host.

19. The method of claim 12, wherein said compound or pharmaceutically acceptable salt or stereoisomer thereof is administered in combination or alternation with a second anti-viral agent optionally selected from the group consisting of an interferon, ribavirin, an interleukin, a NS3 protease inhibitor, a cysteine protease inhibitor, a phenanthrenequinone, a thiazolidine derivative, a thiazolidine, a benzanilide, a helicase inhibitor, a polymerase inhibitor, a nucleotide analogue, a gliotoxin, a cerulenin, an antisense phosphorothioate oligodeoxynucleotide, an inhibitor of IRES-dependent translation, and a ribozyme.

20. The method of claim 19, wherein the second agent is selected from the group consisting of pegylated interferon alpha 2a, interferon alphacon-1, natural interferon, albuferon, interferon beta-1a, omega interferon, interferon alpha, interferon gamma, interferon tau, interferon delta and interferon .gamma.-1b.

21. The method of claim 19, wherein said compound or pharmaceutically acceptable salt or stereoisomer thereof is administered in combination or alternation with ribavirin.

22. A pharmaceutical composition comprising a compound of claim 1 or 10 and a pharmaceutically acceptable excipient, carrier or diluent.

23. The composition of claim 22, wherein the compound is ##STR00286## or a pharmaceutically acceptable salt or stereoisomer thereof.

24. The composition of claim 22, wherein the compound is ##STR00287## or a pharmaceutically acceptable salt or stereoisomer thereof.

25. The composition of claim 23, wherein the composition is an oral formulation.

26. The composition of claim 24, wherein the composition is an oral formulation.

27. A compound of the formula: ##STR00288## or a pharmaceutically acceptable salt, a stereoisomeric or tautomeric form thereof, wherein: R.sup.y is alkyl, alkenyl, alkynyl, aryl, aryl alkyl, cycloalkyl, cycloalkenyl, amino, aminoalkyl, hydroxyalkyl, heterocyclyl or heteroaryl, all optionally substituted; R.sup.a and R.sup.b are selected as follows: i) R.sup.a and R.sup.b are each independently hydrogen, alkyl, carboxyalkyl, hydroxyalkyl, hydroxyarylalkyl, acyloxyalkyl, aminocarbonylalkyl, alkoxycarbonylalkyl, aryl, aryl alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl, all optionally substituted; or ii) R.sup.a and R.sup.b together with the nitrogen atom on which they are substituted form a 3-7 membered heterocyclic or heteroaryl ring; and R.sup.L is independently H, carbamyl, alkyl; acyl; CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl, a lipid, an amino acid or a carbohydrate.

28. The compound of claim 27, wherein: R.sup.L is hydrogen; R.sup.y is --OR.sup.c, --C(R.sup.c).sub.3 or --NHR.sup.c; each R.sup.c is independently alkyl, substituted alkyl, aryl or substituted aryl, for instance hydroxy- or amino-substituted alkyl or aryl; and R.sup.a and R.sup.b are independently hydrogen, alkyl, substituted alkyl, benzyl or substituted benzyl.

29. The compound of claim 28, wherein R.sup.y is --C(CH.sub.3).sub.2CH.sub.2OH.

Details for Patent 7,902,202

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Biogen AVONEX interferon beta-1a VIAL 103628 001 1996-05-17   Try a Free Trial Idenix Pharmaceuticals, Inc. (Cambridge, MA) L\'Universite Montpellier II (Montpellier, FR) 2026-12-28 RX search
Serono Inc REBIF interferon beta-1a SYRINGE 103780 001 2002-03-07   Try a Free Trial Idenix Pharmaceuticals, Inc. (Cambridge, MA) L\'Universite Montpellier II (Montpellier, FR) 2026-12-28 RX search
Serono Inc REBIF interferon beta-1a SYRINGE 103780 002 2002-03-07   Try a Free Trial Idenix Pharmaceuticals, Inc. (Cambridge, MA) L\'Universite Montpellier II (Montpellier, FR) 2026-12-28 RX search
Vidara Therapeutics Research Ltd ACTIMMUNE interferon gamma-1b VIAL; SINGLE-USE 103836 001 1999-02-25   Try a Free Trial Idenix Pharmaceuticals, Inc. (Cambridge, MA) L\'Universite Montpellier II (Montpellier, FR) 2026-12-28 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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