PERHYDROISOINDOLE DERIVATIVES AS ANTAGONISTS OF SUBSTANCE P

摘要

New perhydroinsoindole having the general formula (I) wherein R1 is optionally substituted phenyl or is cyclohexadienyl, naphtyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is phenyl optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF3, and R4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N3 or -NHCN, and the radicals R which are similar or different represent H, alkyl or phenyl, in their isomer forms having the structure (Ia) or mixtures thereof, optionally their salts when they exist and preparation thereof. The new derivatives of the invention are particularly useful as antagonists of substance P.