Process for the production of a pharmaceutical agent for oral or

Details Process for the production of a pharmaceutical agent for oral or Process for the production of a pharmaceutical agent for oral or

1995-06-06

1999-11-09

Brouillette, D. Gabrielle

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Cosmetic, antiperspirant, dentifrice

424 7806, 424601, 514859, 514928, A61K 600

Patent

active

059809159

ABSTRACT:
The invention concerns a new pharmaceutical agent for oral or topical administration in the treatment of protozoal diseases, in particular of leishmaniasis, which contains as the active substance one or several compounds having the general formula I ##STR1## in which R.sup.1 is a saturated or monounsaturated or polyunsaturated hydrocarbon residue with 12 to 20 C atoms and R.sup.2, R.sup.3 and R.sup.4 denote independently of one another hydrogen, a C.sub.1 -C.sub.5 alkys group, a C.sub.3 -C.sub.6 cycloalkyl group or a C.sub.1 -C.sub.5 hydroxyalkyl group whereby two of the residues R.sup.2, R.sup.3 and R.sup.4 can together form a C.sub.2 -C.sub.5 alkylene group which, if desired, can be substituted with an --O--, --S-- or NR.sup.5 group, in which R.sup.5 is hydrogen, a C.sub.1 -C.sub.5 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group or a C.sub.1 -C.sub.5 hydroxyalkyl group as well as, if desired the usual pharmaceutical auxiliary, diluting, carrier or/and filling substances.

REFERENCES:
patent: 4837023 (1989-06-01), Eibl
patent: 5049552 (1991-09-01), Eibl
patent: 5087721 (1992-02-01), Counsell
patent: 5155099 (1992-10-01), Brachwitz
Biochemical Pharmacology, vol. 36, No. 16, pp. 2633-2636 Pergamon Press, 1987, "The Activity of Alkyl Phosphorlycholines and Related Derivatives Against Leishmania Donovani".
Antimicrobial Agents and Chemotherapy, vol. 36, No. 8, pp. 1630-1634, Aug. 1992, "Hexadecylphosphocholine: Oral Treatment of Visceral Leishmaniasis in Mice".
British Medical Journal, Sep. 14, 1985, "Topical Treatment of Recurrent Cutaneous Leishmaniasis with Ointment Containing Paramomycin and Methylbenzethonium Chloride".
The American Journal of Tropical Medicine and Hygiene, vol. 35, No. 6, Nov. 1986, pp. 110-1116, "Leishmania Major: Antileishmanial Activity of Methylbenzethonium Chloride".
Biochemical Pharmacology, vol. 36, No. 16, pp. 2633-2636; "The Activity of Alkyl Phosphorylcholines and Related Derivatives Against Leishmania", by S. L. Croft et al; Date: 1987.
107: 168296e, The activity of alkyl phosphorylcholines and related derivatives against Leishmania donovani Croft, S.L; Neal R.A., et al. vol. 107 (1987).

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