.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 9,290,533

« Back to Dashboard

Details for Patent: 9,290,533

Title:.beta.-L-2'-deoxy-nucleosides for the treatment of hepatitis B
Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside has the formula: ##STR00001## wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
Inventor(s): Gosselin; Gilles (Montpellier, FR), Imbach; Jean-Louis (Montpellier, FR), Bryant; Martin L. (Franklin, TN)
Assignee: Novartis AG (Basel, CH) Centre National de la Recherche Scientifique (Paris, FR) L'Universite Montpellier II (Montpellier, FR)
Filing Date:Mar 22, 2013
Application Number:13/849,243
Claims:1. A method for the treatment of a hepatitis B infection in a human, said method comprising administering an effective amount of 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt thereof, of the formula: ##STR00021## wherein R is selected from the group consisting of, (C.dbd.O)-alkyl, (C.dbd.O)-aryl, (C.dbd.O)-alkoxyalkyl, (C.dbd.O)-aryloxyalkyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid acyl residue, and a stabilized nucleotide or nucleoside prodrug, wherein the stabilized nucleotide or nucleoside prodrug is a 5'- or N.sup.6-alkylated derivative, a 5'-phospholipid, or a 5'-ether lipid.

2. The method of claim 1, wherein the amino acid is L-valinyl.

3. A method for the treatment of a hepatitis B infection in a human, said method comprising administering an effective amount of a combination of the compounds ##STR00022## or a combination of the compounds ##STR00023## or a combination of the compounds ##STR00024## wherein R is selected from the group consisting of H, (C.dbd.O)-alkyl, (C.dbd.O)-aryl, (C.dbd.O)-alkoxyalkyl, (C.dbd.O)-aryloxyalkyl alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid acyl residue, and a stabilized nucleotide or nucleoside prodrug wherein the stabilized nucleotide or nucleoside prodrug is a 5'- or N.sup.6-alkylated derivative, a 5'-phospholipid, or a 5'-ether lipid.

4. The method of claim 3, wherein the amino acid is L-valinyl.

5. A method for the treatment of a hepatitis B infection in a human, said method comprising administering an effective amount of ##STR00025## in combination or alternation with an additional anti-hepatitis B agent, wherein R is selected from the group consisting of, (C.dbd.O)-alkyl, (C.dbd.O)-aryl, (C.dbd.O)-alkoxyalkyl, (C.dbd.O)-aryloxyalkyl alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid acyl residue, mono, di, and triphosphate, and a stabilized nucleotide prodrug, wherein the stabilized nucleotide or nucleoside prodrug is a 5'- or N.sup.6-alkylated derivative, a 5'-phospholipid, or a 5'-ether lipid and wherein the additional anti-hepatitis B agent is selected from the group consisting of .beta.-L-2-hydroxymethyl-5-(cytosine-1-yl)-1,3-oxathiolane (3TC), cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), .beta.-L-2''-fluoro-5-methyl-arabinafuranosyluridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl- ]-6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil), 9-((1R,2R,3S0-2,3-bis(hydroxymethyl)cyclobutyl)guanine (lobucavir), ganciclovir, and ribavarin.

6. The method of claim 5, wherein the amino acid is L-valinyl.

7. A pharmaceutical composition comprising an effective amount of a compound or pharmaceutically acceptable salt thereof of the formula: ##STR00026## wherein R is selected from the group consisting of, (C.dbd.O)-alkoxyalkyl, (C.dbd.O)-aryloxyalkyl alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid acyl residue, and a stabilized nucleotide or nucleoside prodrug, wherein the stabilized nucleotide or nucleoside prodrug is a 5'-phospholipid, or a 5'-ether lipid; in combination with an anti-hepatitis B agent selected from the group consisting of .beta.-L-2-hydroxymethyl-5-(cytosine-1-yl)-1,3-oxathiolane (3TC), cis-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane (FTC), .beta.-L-2'-fluoro-5-methyl-arabinofuranosyluridine (L-FMAU), .beta.-D-2,6-diaminopurine dioxolane (DAPD), famciclovir, penciclovir, 2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl- ]-6H-purin-6-one (entecavir, BMS-200475), 9-[2-(phosphono-methoxy)ethyl]adenine (PMEA, adefovir, dipivoxil), 9-((1R,2R,3S0-2,3-bis(hydroxymethyl)cyclobutyl)guanine (lobucavir), ganciclovir, and ribavarin; in combination with a pharmaceutically acceptable carrier.

8. The pharmaceutical composition of claim 7 wherein R is L-valinyl.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc