Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2008-01-29
2008-01-29
Habte, Kahsay (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C544S003000, C544S008000, C544S127000, C546S123000, C514S222500, C514S234500, C514S300000
Reexamination Certificate
active
07323460
ABSTRACT:
N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I):wherein R1′, R2′and R3′are defined herein. The 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 described.
REFERENCES:
patent: 3945995 (1976-03-01), Yamada et al.
patent: 4416884 (1983-11-01), Ishikawa et al.
patent: 4996213 (1991-02-01), Mendes et al.
patent: 5294620 (1994-03-01), Ratcliffe et al.
patent: 5633262 (1997-05-01), Hong et al.
patent: 5753666 (1998-05-01), Beasley et al.
patent: 5776944 (1998-07-01), Hong et al.
patent: 5945431 (1999-08-01), Jin et al.
patent: 6211376 (2001-04-01), Romines et al.
patent: 6262055 (2001-07-01), Young et al.
patent: 6294547 (2001-09-01), Oka et al.
patent: 6306891 (2001-10-01), Selnick et al.
patent: 6380249 (2002-04-01), Young et al.
patent: 6525042 (2003-02-01), Kobayashi et al.
patent: 6841558 (2005-01-01), Anthony et al.
patent: 2003/0055071 (2003-03-01), Anthony et al.
patent: 2003/0119823 (2003-06-01), Anthony et al.
patent: 2004/0034221 (2004-02-01), Anthony et al.
patent: 2004/0039060 (2004-02-01), Kiyama et al.
patent: 2004/0106627 (2004-06-01), Gardelli et al.
patent: 2004/0127708 (2004-07-01), Fuji et al.
patent: 2005/0010048 (2005-01-01), Zhuang et al.
patent: 0652218 (1995-05-01), None
patent: WO 96/25399 (1996-08-01), None
patent: WO 98/11073 (1998-03-01), None
patent: WO 98/13350 (1998-04-01), None
patent: WO 99/10347 (1999-03-01), None
patent: WO 99/15526 (1999-04-01), None
patent: WO 99/32450 (1999-07-01), None
patent: WO 99/62513 (1999-12-01), None
patent: WO 99/62520 (1999-12-01), None
patent: WO 99/62897 (1999-12-01), None
patent: WO 00/03992 (2000-01-01), None
patent: WO 00/09504 (2000-02-01), None
patent: WO 01/00578 (2001-01-01), None
patent: WO 02/04443 (2002-01-01), None
patent: WO 02/06246 (2002-01-01), None
patent: WO 02/30930 (2002-04-01), None
patent: WO 03/035076 (2003-05-01), None
patent: WO 03/035077 (2003-05-01), None
patent: WO 03/077857 (2003-09-01), None
patent: WO 03/086319 (2003-10-01), None
Parrill AL. Current Medicinal Chemistry. 2003, 10(18): 1811-24, abstract (one page).
Zouhiri et al. J. Med. Chem. 2000, 43, 1533-1540.
Ikeura, Y., et al., “Potent NK1 Receptor Antagonists: Synthesis and Antagonistic Activity of Various Heterocyles with anN-[3,5-Bis(trifluromethyl)benzyl]-N-methylcarbamoyl Substituent”, Chemical and Pharmaceutical Bulletin, vol. 45, No. 10, pp. 1642-1652 (1997).
Ratner, L., et al., “Complete Nucleotide Sequence of the AIDS Virus, HTLV-III”, Nature, vol. 313, pp. 277-284, (1985).
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).
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).
Pearl, L.H., et al., “A Structural Model for the Retroviral Proteases”, Nature, vol. 329, pp. 351-354, (1987).
Chemical Abstract No. 33-2525, Abstract of Otiai, et al., “Synthesis of 2,5 napthyridine derivatives. II”, J. Pharm. Soc. Japan, vol. 58, pp. 764-770 (1938).
CAPLUS Accession No. 2002-293653, Document No. 136:309919, Abstract of WO2002/030931, Anthony et al., “Preparation of Aza- and Polyaza-naphthalenyl Carboxamides as HIV Integrase Inhibitors”, p. 97 (Oct. 24, 2002).
CAPLUS Accession No. 2002-293652, Document No. 136:325531, Abstract of WO2002/030930, Anthony et al., “Preparation of Aza- and (Poly) azanaphthalenyl Carboxamides as HIV Integrase Inhibitors”, p. 434 (Apr. 18, 2002).
Derwent Abstract No. 97-048296/05, Abstract of JP08301849, A. Takeda, Chem, Ind. Ltd., 1995.
CAPLUS Asccession No. 2001-923611, Document No. 136:53570, Abstract of WO2001/095905, Kiyama et al., “Dual Divalent Metal Ion Chelators as HIV Integrase Inhibitors”, p. 146 (Dec. 20, 2001) (Equivalent of Cite No. 16).
Derwent Abstract No. 2002-732783, Abstract of WO02/070486, Fuji, M., New Nitrogenous Heteroaromatic Compounds are HIV Integrase Inhibitors for Treating HIV Infections, AIDS and AIDS Related Diseases, Shionogi & Co., Ltd. (2002) (Equivalent of Cite No. 17).
Chan, L., et al., “Discovery of 1,6-Naphthyridines as a Novel Class of Potent and Selective Human Cytomegalovirus Inhibitors”, J. Med. Chem, vol. 42, pp. 3023-3025 (1999).
Ouali, M., et al., “Modeling of the Inhibition of Retroviral Integrases by Styrylquinoline Derivatives”, J. Med. Chem., vol. 43, pp. 1949-1957 (2000).
Pommier, Y., et al., “Retroviral Integrase Inhibitors Year 2000: Update and Perspectives”, Antiviral Research, vol. 47, pp. 139-148 (2000).
De Clercq, E., “New Anti-HIV Agents and Targets”, Medicinal Research Reviews, vol. 22, No. 6, pp. 531-565 (2002).
Bedard, J., et al., “Antiviral Properties of a Series of 1,6-Naphthyridine and 7,8-Dihydroisoquinoline Derivatives Exhibiting Potent Activity against Human Cytomegalovirus”, Antimicrobial Agents and Chemotherapy, vol. 44, No. 4, pp. 929-937 (2000).
Egbertson Melissa
Embrey Mark
Han Wei
Langford H. Marie
Melamed Jeffrey Y.
Habte Kahsay
Heber Sheldon O.
Merck & Co. , Inc.
Walton Kenneth R.
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