Aminoalkylphenols, methods of using and making the same

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

Reexamination Certificate

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C514S649000, C514S650000, C514S654000, C514S655000, C564S337000, C564S366000, C564S373000, C564S374000, C564S381000, C564S382000, C564S390000

Reexamination Certificate

active

07834062

ABSTRACT:
The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genusPlasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.

REFERENCES:
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Burckhalter et al. “Aminoalkylphenols as Antimalarials. I. Simply Substituted α-Aminocresols”, Journal of the American Chemical Society, 1946, Vol. 68, pp. 1894-1901.
Duncan et al. “2-(ω-Aminoalkyl)-4-t-butyl-6-phenylphenols as Antimalarial Agents”, Journal of the American Chemical Society, 1969, vol. 12, pp. 711-712.
Finn et al. Chemical Abstracts, 1951, 45:49820.
Provent et al. “Double Wittig Reactions with 4-Carboxybutylidene Triphenylphosphorane as the Key Step in the Synthesis of Benzene Derivatives Metadisubstituted with ωω′-Difunctionalized Six-Carbon Chains”, Tetrahedron Letters, 1996, vol. 37, pp. 1393-1396.
Schmidt et al. “Antimalarial Activities of WR-194,965, an α-Amino-o-Cresol Derivative”, Antimicrobial Agents and Chemotherapy, 1978, Vol. 14, pp. 672-679.
Stokker et al. “2-(Aminomethyl)phenols, a New Class of Saluretic Agents. 1. Effects of Nuclear Substitution”, Journal of the American Chemical Society, 1980, vol. 23, pp. 1414-1427.
Zhang et al. “Base and Cation Effects on the Suzuki Cross-Coupling of Bulky Arylboronic Acid with Halopyridines: Sythesis of Pyridylphenols”, Journal of Organic Chemistry, 1998, vol. 63, pp. 6886-6890.

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