Perhydroisoindole derivatives as substance p antagonists

Details Perhydroisoindole derivatives as substance p antagonists Perhydroisoindole derivatives as substance p antagonists

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) C07F 7/10 (2006.01)

Patent

CA 2168233

Novel perhydroisoindole derivatives of general formula (I), wherein 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, R3 is a phenyl radical optionally 2-substituted by C1-2 alkyloxy or alkyl or a fluorine atom, or disubstituted by trifluoromethyl, and R5 and R'5 are the same or different, one representing H or OH or alkyl while the other represents H or alkyl, R4 is OH, or else R4 is F when R5 and R'5 are H or alkyl, or R4 and R5 together form a bond, and R6 is H or alkyl, hydroxy or hydroxyalkyl; and one of the symbols R is H, alkyl, hydroxy or hydroxyalkyl while the other is H, alkyl, phenyl or hydroxyalkyl; isomeric forms with structure (Ia) or mixtures thereof; optionally salts thereof where applicable; and preparation thereof. Said novel derivatives are particularly suitable for use as P substance antagonists.

Nouveaux dérivés de perhydroisoindole de formule générale (I) dans laquelle 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, benzy- loxycarbonyle, amino ou acylamino, R3 est un radical phényle éventuellement substitué en position -2 par alcoyle ou alcoyloxy (1 ou 2C) ou par un atome de fluor, ou disubstitué par trifluorométhyl, et R5 et R'5 sont identiques, ou différents et représentent l'un H ou OH ou alcoyle et l'autre H ou alcoyle, et R4 est OH, ou bien R4 est F si les symboles R5 et R'5 sont H ou alcoyle, ou bien R4 forme avec R5 une liaison, et R6 est H ou alcoyle, hydroxy ou hydroxyalcoyle, et les symboles R sont l'un H, alcoyle, hydroxy ou hydroxyalcoyle et l'autre H, alcoyle, phényle ou hydroxyalcoyle, sous leurs formes isomères de structure (Ia) ou leurs mélanges, éventuellement leurs sels lorsqu'ils existent et leur préparation. Les nouveaux dérivés selon l'invention sont particulièrement intéressants de antagonistes substance P.

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