Perhydroisoindole derivatives, their preparation and...

Details Perhydroisoindole derivatives, their preparation and... Perhydroisoindole derivatives, their preparation and...

C - Chemistry, Metallurgy

07

D

C07D 209/44 (2006.01) A61K 31/395 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2158663

Perhydroisoindole derivatives of general formula (I), wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl radical; R1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.

Dérivés de perhydroisoindole de formule générale (I) dans laquelle les radicaux R sont des radicaux phényle pouvant être substitués par un atome d'halogène ou un radical méthyle en position 2 ou 3, R1 est phényle éventuellement substitué, cyclohexadiényle, naphtyle, indényle, ou hétérocyclyle pouvant être substitué, R2 est H, halogène, OH, alcoyle, aminoalcoyle, alcoylaminoalcoyle, dialcoylaminoalcoyle, alcoyloxy, alcoylthio, acyloxy, carboxy, alcoyloxycarbonyle éventuellement substitué, benzyloxycarbonyle, amino ou acylamino R3 est phényle pouvant être substitué en position 2, éventuellement leurs sels lorsqu'ils existent et leur préparation. Les dérivés selon l'invention sont particulièrement intéressants comme antagonistes de la neurokinine A.

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