Dihydroxypyrimidine carboxamide inhibitors of HIV integrase

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S252140, C514S269000, C544S123000, C544S295000, C544S319000

Reexamination Certificate

active

07459452

ABSTRACT:
4,5-Dihydroxypyrimidine-6-carboxamides of formula:are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3and R4are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

REFERENCES:
patent: 5420129 (1995-05-01), Breu et al.
patent: 5654311 (1997-08-01), Kurtz et al.
patent: 6306891 (2001-10-01), Selnick et al.
patent: 6841558 (2005-01-01), Anthony et al.
patent: 6919351 (2005-07-01), Anthony et al.
patent: 6921759 (2005-07-01), Anthony et al.
patent: 7037908 (2006-05-01), Naidu et al.
patent: 7091209 (2006-08-01), Gardelli et al.
patent: 7109186 (2006-09-01), Walker et al.
patent: 7135467 (2006-11-01), Walker et al.
patent: 7148237 (2006-12-01), Fuji et al.
patent: 7169780 (2007-01-01), Crescenzi et al.
patent: 7217713 (2007-05-01), Crescenzi et al.
patent: 7232819 (2007-06-01), Di Francesco et al.
patent: 2003/0055071 (2003-03-01), Anthony et al.
patent: 2004/0106627 (2004-06-01), Gardelli et al.
patent: 2004/0110804 (2004-06-01), Walker et al.
patent: 2004/0127708 (2004-07-01), Fuji et al.
patent: 2004/0204498 (2004-10-01), Walker et al.
patent: 2004/0229892 (2004-11-01), Naidu et al.
patent: 2004/0229909 (2004-11-01), Kiyama et al.
patent: 2005/0010048 (2005-01-01), Zhuang et al.
patent: 2339272 (2000-03-01), None
patent: 0 601 386 (1994-06-01), None
patent: 1 422 218 (2004-05-01), None
patent: WO 99/32117 (1999-07-01), None
patent: WO 99/62520 (1999-12-01), None
patent: WO 99/62897 (1999-12-01), None
patent: WO 00/51990 (2000-09-01), None
patent: WO 01/00578 (2001-01-01), None
patent: WO 01/85700 (2001-11-01), None
patent: WO 02/06246 (2002-01-01), None
patent: WO 2004/004657 (2004-01-01), None
patent: WO 2004/062613 (2004-07-01), None
Miles, Medline Abstract (Community Pract, vol. 78, Issue 8, pp. 292-294) Aug. 2005.
van Heeswijk et al., PubMed Abstract (Antivir Ther. 6(4):201-29) Dec. 2001.
Marcus et al., PubMed Abstract (Intervirology 45(4-6):260-6) 2002.
Culbertson, Townley P., et al., “Synthesis of 5,6-Dihydroxy-2-phenyl-4-pyrimidinecarboxylic Acid, Methyl Ester, a Corrected Structure”, Journal of Heterocyclic Chemistry , vol. 16, pp. 1423-1424, (1979).
Ivin, B.A., et al., “Unsaturated Hydantoin Derivatives, XI.”, Chemistry of Heterocyclic Compounds, vol. 10, No. 11, pp. 1342-1535 (1976).
Mauss, S., et al., “Influence of HIV Protease Inhibitors on Hepatitis C Viral Load in Individuals with HIV and HCV Coinfection”, Program and Abstracts of the Interscience Conference on Antimicrobial Agents and Chemotherapy, p. 218 (1997).
Pearl, L.H., et al., “A Structural Model for the Retroviral Proteases”, Nature, vol. 329, pp. 351-354, (1987).
Power, M.D., et al., “Nucleotide Sequence of SRV-1, a Type D Simian Acquired Immune Deficiency Syndrome Retrovirus”, Science, vol. 231, pp. 1567-1572, (1986).
Ratner, L., et al., “Complete Nucleotide Sequence of the AIDS Virus, HTLV-III”, Nature, vol. 313, pp. 277-284, (1985).
Sunderland, C., et al., “6-Carboximido-5,4-Hydroxypyrimidinones: A New Class of Heterocyclic Ligands and Their Evaluation as Gadolinium Chelating Agents”, Inorganic Chemistry, vol. 40, No. 26, pp. 6746-6756 (2001).
Toh, H., et al., “Close Structural Resemblance Between Putative Polymerase of a Drosphila Transposable Genetic Element 17.6 and Pol Gene Product of Moloney Murine Leukemia Virus”, EMBO Journal, vol. 4, No. 5, pp. 1267-1272, (1985).
Caplus No. 1992:571466, “Preparation of 2-Phenylpyrimidines as Agrochemical Fungicides”, 1992, Abstract of DE4029654, plus compunds therein indexed in the CAS Registry File.
Derwent Abstract No. 2003-505255/47, “HIV Integrase Inhibitor Comprises New and Known Cyclic Compounds”, 2003, Abstract of WO 03/47564.
Derwent Abstract No. 2000-237546, “Antiviral Agent Containing New or Known Pyrazine, Pyrimidine, Pyridazine or Triazine Caboxamide”, 2000, Abstract of WO 00/10569 (See CA 2,339,272).

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