Dual molecules containing a peroxide derivative, synthesis...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S159000

Reexamination Certificate

active

06949569

ABSTRACT:
The invention relates to dual molecules formed from coupling products complying with the formulawhereinA represents a residue of molecule with anti-malarial activity,Y1and Y2, represent a linear or ramified alkylene chain at C1 to C5, with the possibility of either Y1or Y2being absent,U is an amine, amide, sulphonamide, carboxyl, ether or thioether function, said function linking Y1and Y2,Z1and Z2, represent a linear arylene or alkylene, with the possibility of either Z1or Z2being absent, or Z1+Z2together represent a polycyclic structure including the junction carbons Ci and Cj,R1and R2, represent a hydrogen atom or a functional group capable of increasing the hydrosolubility of the dual molecule,Rxand Ryform a cyclic peroxide with 4 to 8 chain links, Cj being one of the peaks of said cyclic peroxide, orRxor Ryis a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one representing a halogen atom, an —OH group, a —CF3group, an aryl, an alkyl or alkoxy at C1 to C5, —NO2, the other substituent(s) having one of these correspondences or a hydrogen,and their addition salts with pharmacological acceptable acids.Application as medicinal products with anti-malarial activity.

REFERENCES:
patent: WO97/18193 (1997-05-01), None
Cabaret et al, CHEMBIOCHEM, No. 4, p. 281-283, 2000.
G. E. Bass et al.,Mechanism of Antimalarial Activity of Chloroquine Analogs, Journal of Medicinal Chemistry, vol. 14, No. 4, 1971, pp. 275-283, XP002171170.

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