Treating skin afflictions/conditions with...

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice

Reexamination Certificate

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C424S070100, C514S269000, C514S880000

Reexamination Certificate

active

06455054

ABSTRACT:

CROSS-REFERENCE TO PRIORITY APPLICATION
This application claims priority under 35 U.S.C. §119 of FR-98/14211, filed Nov. 12, 1998, hereby expressly incorporated by reference.
BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to treating, for example soothing or calming, a variety of skin afflictions/conditions by administering to a candidate individual in need of such treatment an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide compound.
2. Description of the Prior Art
It is known to this art that humans are subject to adverse cutaneous challenges or stimuli which are characterized by a sensation of skin discomfort, tautness, itchiness, a sensation of burning or warmth on the skin, or red blotches.
Active agents for controlling these types of conditions/afflictions have long been sought by researchers in this art.
Although various active agents have already been proposed, a constant interest remains to develop alternatives providing improved skin-soothing/calmant or anti-inflammatory activity, in particular for treating minor skin afflictions/conditions, such as, for example, sensitive skin, skin discomfort, tautness of the skin, itchiness of the skin, swelling of the skin, red blotchy skin or a sensation of burning or warmth on the skin.
SUMMARY OF THE INVENTION
Accordingly, a major object of the present invention is the provision of improved regime/regimen for treating and alleviating the symptoms of a variety of objectionable skin afflictions/conditions, while at the same time avoiding any appreciable side effects.
Briefly, the present invention features treating the aforesaid skin conditions/afflictions with a skin-soothing, -calmant or anti-inflammatory effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide compound formulated into a physiologically acceptable medium therefor.
DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED EMBODIMENTS OF THE INVENTION
More particularly according to the present invention, by the expression “physiologically acceptable medium” is intended a medium (e.g., vehicle, diluent or carrier) which is compatible with the skin, the mucous membranes, the nails and the hair of a human subject (hereinafter, simply the skin and/or the scalp).
The compounds of the 2-amino-4-alkylaminopyrimidine 3-oxide family which are well suited for administration according to the invention have the general formula (I):
in which R
1
is an alkyl radical having from 1 to 20 carbon atoms, and Z is a hydrogen atom or a radical —OR
2
, wherein R
2
is an alkyl radical having from 1 to 12 carbon atoms, as well as the acyl derivatives and acid addition salts thereof.
According to the invention, by the expression “alkyl radical” is intended a linear or branched acyclic radical originating via the removal of a hydrogen atom from the molecule of a hydrocarbon, such as, for example, a methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl, tetradecyl, pentadecyl, hexadecyl, heptadecyl, octadecyl, nonadecyl or eicosadecyl radical.
In one preferred embodiment of the invention, R
1
is an alkyl radical having from 6 to 12 carbon atoms, such as, for example, a hexyl, heptyl, octyl, nonyl, decyl, undecyl or dodecyl radical.
In another preferred embodiment of the invention, R
2
is an alkyl radical having from 2 to 6 carbon atoms, such as, for example, an ethyl, propyl, butyl, pentyl or hexyl radical.
Preferred compounds according to the invention include:
2-amino-4-methylaminopyrimidine 3-oxide;
2-amino-4-ethylaminopyrimidine 3-oxide;
2-amino-4-propylaminopyrimidine 3-oxide;
2-amino-4-butylaminopyrimidine 3-oxide;
2-amino-4-pentylaminopyrimidine 3-oxide;
2-amino-4-hexylaminopyrimidine 3-oxide;
2-amino-4-heptylaminopyrimidine 3-oxide;
2-amino-4-octylaminopyrimidine 3-oxide;
2-amino-4-nonylaminopyrimidine 3-oxide;
2-amino-4-decylaminopyrimidine 3-oxide;
2-amino-4-undecylaminopyrimidine 3-oxide;
2-amino-4-dodecylaminopyrimidine 3-oxide;
2-amino-4-tridecylaminopyrimidine 3-oxide;
2-amino-4-tetradecylaminopyrimidine 3-oxide;
2-amino-4-pentadecylaminopyrimidine 3-oxide;
2-amino-4-hexadecylaminopyrimidine 3-oxide;
2-amino-4-heptadecylaminopyrimidine 3-oxide;
2-amino-4-octadecylaminopyrimidine 3-oxide;
2-amino-4-nonadecylaminopyrimidine 3-oxide;
2-amino-4-eicosadecylaminopyrimidine 3-oxide;
2-amino-4-methylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-ethylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-propylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-butylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-pentylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-hexylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-heptylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-octylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-nonylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-decylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-undecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-dodecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-tridecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-tetradecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-pentadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-hexadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-heptadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-octadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-nonadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-eicosadecylamino-6-methoxypyrimidine 3-oxide;
2-amino-4-methylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-ethylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-propylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-butylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-pentylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-hexylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-heptylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-octylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-nonylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-decylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-undecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-dodecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-tridecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-tetradecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-pentadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-hexadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-heptadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-octadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-nonadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-eicosadecylamino-6-ethoxypyrimidine 3-oxide;
2-amino-4-methylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-ethylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-propylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-butylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-pentylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-hexylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-heptylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-octylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-nonylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-decylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-undecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-dodecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-tridecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-tetradecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-pentadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-hexadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-heptadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-octadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-nonadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-eicosadecylamino-6-propyloxypyrimidine 3-oxide;
2-amino-4-methylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-ethylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-propylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-butylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-pentylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-hexylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-heptylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-octylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-nonylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-decylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-undecylamino-6-butyloxypyrimidine 3-oxide;
2-amino-4-dodecyl

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