Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-12-16
2000-08-29
Jones, Dwayne C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514336, A01N 4360, A61K 31495
Patent
active
061109177
DESCRIPTION:
BRIEF SUMMARY
The subject-matter of the present invention is a specific salt of an active pharmaceutical agent. More particularly, the invention relates to the methanesulfonate salt of an arylpiperazide derived from tryptamine which acts at the level of the serotonin (5-HT) receptors, more specifically as selective agonist of 5-HT.sub.1D/1B receptors. This compound is consequently found to be of use in the treatment of pathological conditions for which a selective agonist of these receptors is indicated.
Agonists of the .sup.5 -HT.sub.1D/1B receptors (according to the recent nomenclature proposed in TiPS, 17, 103, 1996) which demonstrate a selective vasoconstrictive activity have recently been described as useful in the treatment of migraine (cf., for example, A. Doenicke et al., The Lancet, 1, 1309, 1988). The salt of the present invention, which shows a powerful agonist activity at the level of the 5-HT.sub.1D/1B receptors, is consequently particularly useful in the treatment, both curative and preventive, of classic migraine (with aura), common migraine (without aura) and associated or closely related disorders, such as vasospastic disorders, vascular facial pain or chronic vascular headaches.
Patent Application PCT FR 9401343 (WO-9514004) discloses a class of arylpiperazines derived from indole as selective and effective agonists of 5-HT.sub.1D/1B receptors and consequently as particularly useful in the treatment of migraine and associated disorders.
The present invention relates to the mesylate (or methanesulfonate) salt of 4-(4-{2-[3-(2-aminoethyl)-1H-indol-5-yloxy]acetyl}piperazin-1-yl)benzonitr ile of formula (I): ##STR1## and its solvates (in particular its hydrates) which are acceptable for the therapeutic use.
The pharmaceutically acceptable salts of 4-(4-{2-[3-(2-aminoethyl)-1H-indol-5-yloxy]acetyl}piperazin-1-yl)benzonitr ile form part, in a general way, of Patent Application WO-9514004. In fact, the hydrochloride, hydrobromide, sulfate, maleate and fumarate salts are specifically referred to in Application WO-9514004. However, this patent application in no case describes or suggests the specific salt of formula (I) forming part of the present invention.
The salt of formula (I) above, in an entirely unexpected way, possesses attractive advantages, in particular for its use as therapeutic agent. For example, the compound of formula (I) exhibits a solubility which is markedly greater than the other salts of 4-(4-{2-[3-(2-aminoethyl)-1H-indol-5-yloxy]acetyl}piperazin-1-yl)benzonitr ile specifically claimed in Application WO-9514004.
Another aspect of the present invention has as subject-matter the compositions for pharmaceutical use comprising the methanesulfonate salt (I) in combination with one or more pharmaceutical vehicles which are acceptable for the therapeutic use.
The present invention also relates to the medicaments comprising at least one compound of formula (I) in the pure state or in the form of a composition in which it is combined with any other pharmaceutically compatible product, which can be inert or physiologically active. The medicaments according to the invention can be employed orally, parenterally, rectally or nasally or by any other administration route.
Tablets, pills, powders (gelatin capsules or cachets) or granules can be used as solid compositions for oral administration. In these compositions, the active principle according to the invention is mixed with one or more inert diluents, such as starch, cellulose, sucrose, lactose or silica, under an argon stream. These compositions can also comprise substances other than diluents, for example one or more lubricating agents, such as magnesium stearate or talc, a colorant, a coating agent (dragees) or a varnish.
Pharmaceutically acceptable solutions, suspensions, emulsions, syrups and elixirs comprising inert diluents, such as water, ethanol, glycerol, vegetable oils or liquid paraffin, can be used as liquid compositions for oral administration. These compositions can comprise substances other than the diluents, for example wetting, swee
Halazy Serge
Perez Michel
Jones Dwayne C.
Pierre Fabre Medicament
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