Compounds of the 3-aryl 2,4 dioxo oxazolidine family and use the

Details Compounds of the 3-aryl 2,4 dioxo oxazolidine family and use the Compounds of the 3-aryl 2,4 dioxo oxazolidine family and use the

1999-04-05

2000-05-02

Lambkin, Deborah C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548227, 548226, A61K 3142, C07D26306

Patent

active

060573511

DESCRIPTION:

BRIEF SUMMARY
This invention relates to new compounds of the aryl 2,4 dioxo oxazolidine family. It also relates to a method for synthesizing same, compositions containing said compounds as well as the use of at least one of these compounds to induce and/or stimulate hair growth and/or control hair loss and/or treat hyperseborrhea and/or acne.
In humans, hair growth and renewal are mostly determined by the activity of the hair follicles. Their activity is cyclical and contains essentially three phases, being the anagen phase, the intermediate phase and the telogen phase.
The active anagen phase, or growth phase that lasts several years and during which the hair grows longer, is followed by a very short and temporary intermediate phase that lasts a few weeks, then by a rest phase, called telogen phase, that lasts several months.
At the end of the rest period, the hair falls out and another cycle starts up. Therefore, scalp hair renews itself permanently, and of the approximate 150 000 scalp hairs, at every moment, approximately 10% of them are resting and will therefore be replaced in a few months.
However, different causes may lead to a large loss, temporary or final, of ones hair. Alopecia is mostly due to a disturbance of the hair renewal which leads, at first, to an acceleration of the cycle frequencies at the expense of the quality of the hair then of their quantity. A progressive thinning of the hair occurs by regression of the hair called "terminal" at the fluff stage. Certain areas are hit more often, in particular the temporal and frontal gulfs in men, and in women, we notice an alopecia disseminata of the vertex.
The term alopecia covers a whole family of diseases of the hair follicle that lead to the permanent partial or general loss of hair.
In many cases, early hair loss happens to subjects who are genetically prone to hair loss and it affects men in particular. It is more particularly androgenetic or androgenic or even androgeno-genetic alopecia.
For several years, the cosmetic or pharmaceutical industry, has researched substances that will make it possible to eliminate or reduce alopecia, and in particular induce or stimulate hair growth or control hair loss.
In this regard, many active and varied compounds have already been proposed, such as for example the 3-oxide pyrimidine 6-piperidino 2,4-diamino or "Minoxidil" described in the patents U.S. Pat. Nos. 4,139,619 and 4,596,812 or yet its many derivatives such as for example those described in the requests for patents EP 0353123, EP 0356271, EP 0408442, EP 0522964, EP 0420707, EP 0459890, EP 0519819.
Nevertheless, generally speaking, it would be interesting and useful to be able to have access to active compounds other than those already known, potentially more active and/or less toxic.
This objective and others are reached through this invention which relates to new compounds that match the general formula (I): ##STR1## where R1 is a halogen atom or a cyano group or an alkyl group, in C.sub.1 -C.sub.4 substituted by at least one halogen atom; -C.sub.4 ; substituted by at least one halogen atom; one halogen atom or one aryl group, possibly substituted by one or several halogen atoms, by one or several carboxylic, cyano or perfluoroalkyl groups.
The invention also relates to optical isomers, alone or in a mixture in all percentages, acylated forms or even pharmaceutically acceptable salts of these compounds.
By halogen atoms we mean preferably as set forth in the invention, fluorine, chlorine or bromine atoms.
By alkyl group in C.sub.1 -C.sub.4, we mean preferably as set forth in the invention the linear or ramified alkyl radicals in C.sub.1 -C.sub.4, and in particular the methyl, ethyl, propyl, isopropyl, butyl, isobutyl or tertiobutyl radicals and more specifically the methyl radical.
By alkyl radical substituted by at least one halogen atom we mean preferably the radicals described above for which at least one hydrogen atom is substituted by a halogen atom, including the perhalogenated radicals for which all hydrogen atoms are replaced by as many halogen

REFERENCES:
patent: 3703526 (1972-11-01), Sato et al.
patent: 3995049 (1976-11-01), Mangold et al.
patent: 4000291 (1976-12-01), Perronnet et al.
patent: 4342773 (1982-08-01), Di Toro et al.
patent: 4810799 (1989-03-01), Zanker et al.
patent: 5100457 (1992-03-01), Hirai et al.

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