abstract |
Perhydroisoindole derivatives of formula described in the specification, in which R1 is phenyl which is optionally substituted, cyclohexadienyl, naphthyl, indenyl, or a heterocycle which may be substituted, R2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxyl, alkyloxycarbonyl which is optionally substituted, benzyloxycarbonyl, amino or acylamino, R3 is a phenyl radical which is optionally substituted in the 2-position with alkyl or alkyloxy (1 or 2C) or with a fluorine atom, or disubstituted with trifluoromethyl, and R4 is OH and R5 and R'5 are identical or different and one represents H or OH or alkyl and the other represents H or alkyl, or R4 is F and R5 and R'5 are H or alkyl, or R4 together R6 is H or alkyl, hydroxyl or hydroxyalkyl, and one of the symbols R is H, alkyl, hydroxyl or hydroxyalkyl, and the other is H, alkyl, phenyl or hydroxyalkyl, in their isomeric forms of structure described in the specification and their mixtures, and optionally their salts when such exist are particularly advantageous as antagonists of substance P. |