Intimal hypertrophy inhibitors

Details Intimal hypertrophy inhibitors Intimal hypertrophy inhibitors

A - Human Necessities

61

K

A61K 31/44 (2006.01) A61K 31/40 (2006.01) C07D 209/34 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2214759

The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof: Image (wherein R1 represents a hydrogen atom; a phenyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, or a halogen atom; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R2 represents a phenyl group which may be substituted; or a pyridyl group which may be substituted by a lower alkyl group, a lower alkoxy group, a lower alkylaminoalkoxy group, a hydroxy group, an amino group, a lower alkylamino group, a halogen atom, a lower alkoxycarbonyl group, or a carboxyl group; R3 represents a hydrogen atom; a lower alkyl, benzyl, or a benzenesulfonyl group which may be substituted; or an aryl group; R4 represents a hydrogen atom; a lower alkoxy group, a halogen atom, an amino group, a lower alkylamino group, a carboxyl group, a lower alkoxycarbonyl group; a phenylcarbomoyl group which may be substituted; or a trifluoromethyl group; X represents CH or N; n represents a number between 0 and 4 inclusive that indicates the number of substituents; and the broken/solid double line denotes a single bond or a double bond). The intimal hypertrophy inhibitor of the present invention exhibits excellent inhibitory action against intimal hypertrophy, and thus is useful as a preventive/therapeutic/ameliorating agent for proliferative vascular diseases such as restenosis after PTCA, arteriosclerosis, peripheral embolism, and angiitis.

Inihibiteurs d'épaississement de l'intima dont le principe actif est des dérivés d'oxyndole, représentés par la formule générale (1) ou leurs sels, formule dans laquelle R<1> représente hydrogène, phényle facultativement substitué par alkyle inférieur, alcoxy inférieur, alkylaminoalcoxy inférieur, hydroxy, amino, alkylamino ou halogéno inférieur, ou pyridyle facultativement substitué par alkyle inférieur, alcoxy inférieur, alkylaminoalcoxy inférieur, hydroxy, amino, alkylamino inférieur, halogéno, alcoxycarbonyle ou carboxy inférieur; R<2> représente phényle facultativement substitué ou pyridyle facultativement substitué par alkyle inférieur, alcoxy inférieur, alkylamino-alcoxy inférieur, hydroxy, amino, alkylamino inférieur, halogéno, alkoxycarbonyle ou carboxy inférieur; R<3> représente hydrogène, alkyle inférieur facultativement substitué, benzyle ou benzènesulfonyle ou acyle; R<4> représente hydrogène, alcoxy inférieur, halogéno, amino, alkylamino inférieur, carboxy, alcoxycarbonyle inférieur, phénylcarbamoyle facultativement substitué ou trifluorométhyle; X représente CH ou N; m représente le nombre des substituants allant de 0 à 4; et la double ligne composée de lignes pointillées et pleines signifie que cette liaision est une liaison soit simple soit double. Ces médicaments présentent d'excellents effets d'inhibition d'épaississement de l'intima et sont par conséquent utiles dans la prévention, le traitement et la récidive de lésions vasculaires prolifératives telles qu'une reconstriction vasculaire après recanalisation coronaire transluminale percutanée, l'arthériosclérose, l'embolie périphérique et l'angéite.

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