Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-06-02
1997-09-09
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514934, 514262, 514261, 514272, 514269, 544 92, A61K 31535
Patent
active
056657200
ABSTRACT:
Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
REFERENCES:
patent: 3526621 (1970-09-01), Bernardi et al.
patent: 3682933 (1972-08-01), Engel
patent: 4313873 (1982-02-01), Lim et al.
patent: 4857511 (1989-08-01), Rideout et al.
patent: 5179093 (1993-01-01), Afonso et al.
patent: 5434152 (1995-07-01), Huffman et al.
Ratner, et al., "Complete Nucleotide Sequence of the AIDS Virus . . ."Nature, vol. 313, pp. 227 (1985).
Toh et al., "Close Structural Resemblance Between Putative Polymerase . . .", Embo. Jour., vol. 4, 1267 (1985).
Power, et al., "Nucleotide Sequence of SPV-1 . . .", Science, vol. 231, p. 1567 (1986).
Pearl, , et al., "A Structural Model for the Retroviral Proteases", Nature, vol. 329, p. 351 (1987).
Horowitz, et al., "Nucleosides, V. The Monomesylates of 1-(2'-. . .", J. Org. Chem., vol. 29, p. 2076 (1964).
Glinski, et al., "Nucleotide Synthesis. IV. Phosphorylated . . .", J. Org. Chem., vol. 38, No. 25, (1973).
Chu, et al., "An Efficient Total Synthesis of 3'-Azido . . .", Tetrahedron Letters, vol. 29, p. 5349 (1988).
Horowitz, et al., "Nucleosides. XI., 2', 3'-Dideoxycytidine", J. Org. Chem., vol. 32, p. 817 (1967).
Marumoto, et al., "One-Step Halogenation at the 2'-Position of Uridine . . .", Chem. Pharm. Bull., vol. 22, p. 128 (1974).
Lin, et al., "Synthesis and Antiviral Activity of Various 3'-Azido, 3'-Amino, 2', 3'-Unsaturated . . .", J. Med. Chem., vol. 30, p. 440 (1987).
Herdewijn, et al., "3'-Substituted 2', 2'-Dideoxynucleoside Analogues as Potential . . .", J. Med. Chem., vol. 30, pp. 1270-8 (1987).
Miyasaka, et al., "A Novel Lead for Specific Anti-HIV-1 Agents . . .", J. Med. Chem., vol. 30, pp. 1270-1278 (1987).
Nunberg, et al., "Viral Resistance touman Immunodeficiency Virus Type 1-Specific . . .", J. Virology, vol. 65, No. 9, pp. 4887-4892 (1991).
Rosowsky, et al., "Synthesis and Antitumor Activity of an Acyclonucleoside Derivative of . . .", J. Med. Chem., vol. 24, No. 10, p. 1177 (1981).
Schoberth, et al., "Eine einfache Herstellungsmethode fur Cyclopropylacetylen", Communications, p. 703 (1972).
Hudson, et al., "A Quantitative Analysis of Cyclopropyl . . .", J. of the A,erican Chem. Soc., pp. 1158-1163 (1972).
Lewin, et al., "Antibacterial Activity of Fluoroquinolones . . .", J. Med. Microbiol., vol. 33, pp. 127-131 (1990).
Nozaki-Renard et al., "Fluoroquinolones Protect the Human Lymphocyte . . .", Cell Structure & Function, vol. 15, No. 5, pp. 295-299 (1990).
Nordmann, et al., "In-vitro Antimicrobial Susceptibility of Rhodococcus equi", J. of American Antimicro Chemotherapy, vol. 29, pp. 383-393 (1992).
Young et al., "Activity of Ciproflaxacin and Other Fluorinated Quinolones . . .", American J. of Medicine, vol. 82, Suppl. 4A, pp. 22-23 (1987).
Bernardi, et al., "Central Depressant Properties of 3,1-Benzoxazine Derivatives", Experientia, vol. 25, No. 8, pp. 787-188 (1969).
Carretero, et al., "A Practical Route to C-8 Substituted Fluoroquinolones", Tetrahedron, vol. 48, No. 35, pp. 7373-7382 (1992).
Rastogi, et al., "Enhancement of Drug Susceptibility . . .", Antimiicrobial Agents & Chemo., vol. 34, No. 5, pp. 759-764 (1990).
Kukla, et al., "Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro . . .", J. Med. Chem., vol. 34, No. 11, pp. 3187-3197 (1991).
Gioia, et al., "Identification of the Metabolites of Brofoxine . . .", Adv. Mass. Spectrum., 7 Beta . . . , pp. 1622-1627 (1978).
Benerjee, et al., "Evaluation of the Activity of a Number of Antimicrobial . . . ", J. of Antimicrobial Chemotherapy, vol. 31, pp. 289-302 (1993).
Hartmann, et al., "Effects of Brofoxine, A New Anxiolytic . . . ", Proc. West Pharmacol, Soc., vol. 21, pp. 51-53 (1978).
Nozaki-Renard, et al., "A fluoroquinolone (DR-3355) protects human . . . ", AIDS (London), vol. 4, No. 12, pp. 1283-1286 (1990).
Menozzi, et al., "Interaction of Brofoxine with Serum Proteins", vol. 42, No. 11, pp. 808-809 (1990).
Lewin, et al., "Susceptibility of Bacterial Isolates from AIDS . . . ", J. Pharm. & Pharmacol., vol. 42, No. 11, pp. 808-809 (1990).
Science, vol. 260, pp. 1253-1293 (May 1993).
Young, et al., Chem Ab. vol. 120, 270423, p. 1074 (1994).
Britcher Susan F.
Lumma, Jr. William C.
Payne Linda S.
Tran Lekhanh O.
Young Steven D.
Camara Valerie J.
Daniel Mark R.
Grumbling Matthew V.
Merck & Co. , Inc.
LandOfFree
Benzoxazinones as inhibitors of HIV reverse transcriptase does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Benzoxazinones as inhibitors of HIV reverse transcriptase, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Benzoxazinones as inhibitors of HIV reverse transcriptase will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-70170