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Claims for Patent: 9,085,573

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Claims for Patent: 9,085,573

Title:Nucleoside phosphoramidate prodrugs
Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: ##STR00001## Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
Inventor(s): Du; Jinfa (Redwood City, CA), Nagarathnam; Dhanapalan (Bethany, CT), Sofia; Michael Joseph (Doylestown, MN), Wang; Peiyuan (Totowa, NJ)
Assignee: GILEAD PHARMASSET LLC (Foster City, CA)
Application Number:14/013,237
Patent Claims: 1. cited by applicant .
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Hrebabecky, et al., "Synthesis of 1-(3-azido-2,3-diDE-oxy-4-C-hydroxymethyl-alpha-L-threo-pentofuranosyl)th- ymine, 1-(2, 3-d id eoxy-4-C-hyd roxy-methyl-alpha-L-glycero-pentofuranosyl)thymine and 1-(2,3-diDE-oxy-4-C-hydroxymethyl-alpha-L-glycero-pent-2-enofuranosyl)thy- mine," Collect Czech. Chem. Commun., vol. 58, pp. 409-420, (1992). cited by applicant .
Hrebabecky, et al., "Synthesis of 1-(3-azido-2,3-diDE-oxy-.beta.-D-allofuranosyl)thymine, 1-(2,3-diDE-oxy-.beta.-D-allofuranosyl)thymine, and 1-(2,3-diDE-oxy-.about.-D-erythro-hex-2-enofuranosyl)thymine," Carbohydrate Research, vol. 216, pp. 179-186, (1991). cited by applicant .
Hrebabecky, et al., "Synthesis of 1-(3-azido-2,3-diDE-oxy-.beta.-d-ribo-hexofuranosyl)-, 1-(2,3-did eoxy-.beta.-d-erythro-hexofu ranosyl )- and 1-(2,3-d iDE-oxy-.beta.-d-erythro-hex-2-enofuranosyl)pyrimidine nucleosiDE-s," Collect. Czhech. Chem. Commun., vol. 59, pp. 412-420, (1993). cited by applicant .
Written Opinion of PCT/US2010/035641 mailed Sep. 28, 2010. cited by applicant .
Written Opinion of PCT/EP2006/069060 mailed Jan. 30, 2007. cited by applicant .
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Written Opinion of PCT/US2005/032406 mailed May 8, 2008. cited by applicant .
International Search Report issued in International PCT application No. PCT/US2008/058183 mailed Mar. 31, 2010 (7 pages). cited by applicant .
Lin, et al., "A stereospecific synthesis of 2',3'-diDE-oxy-.beta.-L-cytidine (.beta.-L-ddC), a potent inhibitor against human hepatitis B virus (HBV) and human immunoDE-ficiency virus (HIV)," Tetrahedron Letters, vol. 35, No. 21, pp. 3477-3480, (1994). cited by applicant .
McGuigan et al., "Synthesis, anti-human immunoDE-ficiency virus activity and esterase lability of some novel carboxylic ester-modified phosphoramidate DE-rivatives of stavudine (d4T)," Antiviral Chemistry & Chemotherapy, vol. 9, pp. 473-479 (1998). cited by applicant .
Mourier, et al., "Enantioselective synthesis and biological evaluation of 5-o-carboranyl-pyrimidine-nucleosides," Bioorganic & Medicinal Chemistry, vol. 7, pp. 2759-2766, (1999). cited by applicant .
Response filed Oct. 25, 2010 at the EPO for European patent application No. EP08732818.3. cited by applicant .
Response to non-final Office Action dated Oct. 1, 2009 for U.S. Appl. No. 12/142,554. cited by applicant .
Robins, et al., "Nucleic acid related compounds. 91. Biomimetic reactions are in harmony with loss of 2'-substituents as free radicals (not anions) during mechanism-based inactivation of ribonucleotiDE-reductases. differential interactions of aziDE-, halogen, and alkylthio groups with tributylstannane and triphenylsilane," Journal of the American Chemical Society, vol. 118, No. 46, pp. 11341-11348, (1996). cited by applicant .
Saneyoshi, "Facile synthesis of 2'-O-cyanoethyluridine by ring-opening reaction of 2,2'-anhydrouridine with cyanoethyl trimethylsilyl ether in the presence of BF.sub.3 Et.sub.2O," Tetrahedron Letters, vol. 48, pp. 8554-8557, (2007). cited by applicant .
Selected Prosecution documents from U.S. Appl. No. 10/828,753 (1) Feb. 26, 2007 Amendment; (2) Mar. 30, 2007 Office Action; (3) Jun. 9, 2007 Interview Summary; (4) Sep. 12, 2007 Amendment; (5) Sep. 12, 2007 Declaration; (6) Sep. 24, 2007 Declaration; (7) Nov. 28, 2007 Amendment; (8) Feb. 26, 2008 Office Action; (9) Mar. 11, 2008 Amendment; and (10) May 29, 2008 Notice of Allowance). cited by applicant .
Selected Proscution Documents from U.S. Appl. No. 11/854,218: (1) Sep. 12, 2007 Amendment; (2) Oct. 1, 2008 Office Action; (3) Mar. 31, 2010 Response; (4) Mar. 31, 2011 Declaration; (5) Jul. 22, 2010 Office Action; (6) Oct. 11, 2010 Amendment; (7) Oct. 11, 2010 Declaration; (8) Dec. 23, 2010 Office Action; (9) Jun. 28, 2011 Amendment. cited by applicant .
U.S. Appl. No. 12/142,554, Pending claims filed on Dec. 17, 2009. cited by applicant .
U.S. Appl. No. 13/956,195, filed Jul. 31, 2013. cited by applicant .
Van Rompaey, et al., "Mycobacterium tuberculosis thymidine monophosphate kinase inhibitors; biological evaluation and conformational analysis of 2'-and 3'-modified thymidine analogues," Eur. J. Org. Chem., pp. 2911-2918, (2003). cited by applicant .
Vanheusde-N, et al., "Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase," J. Med. Chem., vol. 47, pp. 6187-6194, (2004). cited by applicant .
Vanheusde-N, et al., "Synthesis and evaluation of thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase," Bioorganic & Medicinal Chemistry Letters, vol. 12, pp. 2695-2698, (2002). cited by applicant .
Wu et al., "Targeting NS5B RNA-DE-penDE-nt RNA Polymerase for Anti-HCV Chemotherapy," Current Drug Targets- Infectious DisorDE-rs, vol. 3, No. 3, pp. 207-219 {2003). cited by applicant .
U.S. Appl. No. 11/225,724 pending claims filed Oct. 2, 2009. cited by applicant .
Selected Prosecution documents from U.S. Appl. No. 12/053,015: (1) Jun. 15, 2010 Resitriction Requirements; (2) Oct. 28, 2010 Amendment ; (3) Jan. 5, 2011 Notice of Alloance; and (4) Apr. 1, 2011 Amendment. cited by applicant .
U.S. Appl. No. 12/783,680 filed May 20, 210--Originally filed claims. cited by applicant .
U.S. Appl. No. 13/076,552, filed Mar. 31, 2011--Originally filed claims. cited by applicant .
U.S. Appl. No. 12/645,710, filed Dec. 23, 2009--Originally filed claims. cited by applicant .
U.S. Appl. No. 12/878,262--Pending Claims as of Sep. 1, 2011. cited by applicant .
Selected Proscution Documents for U.S. Appl. No. 12/878,262: (1) Sep. 9, 2010 Amendment; (2) Jun. 8, 2011 Office Action; and (3) Sep. 1, 2011 Amendment. cited by applicant .
Office Action for Australian Application No. 2012241173 dated Apr. 8, 2014. cited by applicant .
Office Action for Colombian Application No. 09-120.744A dated Jun. 25, 2014. cited by applicant .
Extended Search Report for European Application No. 14151876.1 dated Sep. 18, 2014. cited by applicant .
Communication pursuant to Rules 70(2) and 70a(2) EPC and reference to Rule 39(1) EPC for European Application No. 14179593.0 dated Jan. 19, 2015. cited by applicant .
English Translation of Office Action for Korean Application No. 10-2009-7022652 dated Dec. 19, 2013. cited by applicant .
Office Action for Korean Application No. 10-2012-7004146 dated Oct. 29, 2014. cited by applicant .
English Translation of Office Action for Israeli Application No. 222810 dated Jan. 4, 2015. cited by applicant .
English Translation of Office Action in Mexican Application No. MX/a/2012/000289 dated Jan. 22, 2015. cited by applicant .
English Translation of Office Action in Mexican Application No. MX/a/2012/000289 dated Oct. 30, 2014. cited by applicant .
Office Action in Chinese Application No. 200880018024.2 dated Oct. 31, 2014. cited by applicant .
Office Action in Japanese Application No. 2014-093905 dated Jan. 13, 2015. cited by applicant .
Subsequent Substantive Examination Report for Phillipines Application No. 1/2009/501847 dated Nov. 10, 2014. cited by applicant .
Opposition by the Initiative for Medicines, Access & Knowledge (I-Mak) to Indian Application No. 3658/KOLNP/2009 N. cited by applicant .
Opposition by NATCO Pharma Limited to Indian Application No. 3658/KOLNP/2009 dated Mar. 3, 2014. cited by applicant .
Opposition by SANKLAP Rehabilitation Trust to Indian Application No. 3658/KOLNP/2009 dated Sep. 10, 2014. cited by applicant .
Opposition by Indian Pharmaceutical Alliance to Indian Application No. 3658/KOLNP/2009 dated Feb. 17, 2015. cited by applicant .
Opposition by Actavis Group PTC ehf to European Application No. 08732818.3 dated Feb. 23, 2015. cited by applicant .
Opposition by Teva Pharmaceutical Industries to European Application No. 08732818.3 dated Feb. 10, 2015. cited by applicant .
Opposition by Medecins Du Monde to European Application No. 08732818.3 dated Feb. 10, 2015. cited by applicant .
Opposition by Ellis IP Ltd. to European Application No. 08732818.3 dated Feb. 10, 2015. cited by applicant .
Opposition by Mr. Holm Herbert Fleisher to European Application No. 08732818.3 dated Feb. 19, 2015. cited by applicant .
Opposition by Generics [UK] Ltd (trading as Mylan) to European Application No. 08732818.3 dated Feb. 19, 2015. cited by applicant .
Opposition by IPS to European Application No. 08732818.3 dated Feb. 23, 2015. cited by applicant .
Opposition by Pharmaceutical Works Polpharma S.A. to European Application No. 08732818.3 dated Feb. 19, 2015. cited by applicant .
Opposition by Stada Arzneimittel AG to European Application No. 08732818.3 dated Feb. 19, 2015. cited by applicant .
Opposition by ZBM Patents=Zea, Barlocci & Markvardsen to European Application No. 08732818.3 dated Feb. 23, 2015. cited by applicant .
Furman et al., "The Anti-Hepatitis B Virus Activities, Cytoxicities, and Anabolic Profiles of the (-) and (+) Enantiomers of cis-5-Fluoro-1-[2-(Hydroxymenthyl)-1,3-Ozathiolan-5-yl]Cytosine," Antimicrobial Agents and Chemotherapy, (1992), 36(2):2686-2692. cited by applicant .
Chang et al., "Deoxyctidine-resistant Stereoisomer Is the Active Form of (.+-.)-2',3'-Dideoxy-3'-thiacytidine in the Inhibition of Hepatitis B Virsu Replication," J. Bio. Chem, (1992), 267(20):13938-13942. cited by applicant .
Trousdale. et al.,"Activity of 1-(2'-Fluoro-2'-Deoxy-.beta.-D-Arabinofuranosyl)Thymine Against Herpes Simplex Virsu in Cell Cultires and Rabbit Eyes," Antimicrobial Agents and Chemotherapy, (1983), 23(6):808-813. cited by applicant .
Klumpp, et al., "The Novel Nucleoside Analog R1479(4'-Azidocytidine) Is a Potent Inhibitorof NS5B-dependent RCA Synthesis and Hepatitis C Virus Replication in Cell Culture," J. Bio. Chem., (2006), 281:3793-3799. cited by applicant .
Landowski et al, "Targeted delivery to PEPT1-overexpressing cells: Acidic, basic, and secondary floxurdine amino acid ester prodrugs," MCT, (2005), 4(4):659-667. cited by applicant .
McGuigan, "Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine," Antiviral Chemistry & Chemotherapy, (2000), 11:111-116. cited by applicant .
Perrone, Thesis entitled "Design Synthesis an dBiological Evaluation of Novel Nucleotide Prodrugs as Potential Anti-Hepatitis C Virus Agents," (2007). cited by applicant .
Zemlicka, Lipophilic phosporamidates as antiviral pornucleotides, Biochem Biophys Acta, (2002), 276-286. cited by applicant .
Sofia, "Discovery of a beta-D-2'-Deoxy-2'-alpha-fluoro-2'-beta-C-methyluridine Nucleotide Prodrug (PSI-7977) for the Treament of Hepatitis C Virus," J. Med. Chem., (2010), 53. cited by applicant .
Abstract, 100, presented at the 19.sup.th International Conference of Antiviral Research, May 7-11, 2006. cited by applicant .
Guinic, et al., "Cyclic monophosphate prodrugs of base=modified 2'-C-methyl ribonucleosides as potent inhibitors of hepatitis C virus RNA replicaion," Bioorg Med Chem Lett., (2007), 17(9):2456-2458. cited by applicant.

Primary Examiner: Lewis; Patrick
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