Derivatives of substituted imidazol-2-one and process for their preparation
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsMario Varasi, Franco Heidempergher, Nicola Carfagna, Ruggero Fariello
Life of this patent
Estimating the term…
Abstract
Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents a group ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addition agents and analgesic.
Claims4
A compound of formula (I ) ##STR11## wherein each of R, R.sub.1, and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, CF.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxycarbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl;
- or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;
- n is an integer of 1 or 2;
- and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl;
- or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- (endo)-1-(8-methyl-8-azabicyclo [3.2.1] oct-3-yl)-3-(3-chlorophenyl)-imidazolidin-2-one;
- (exo)-1-(8-methyl-8-azabicyclo [3.2.1] oct-3-yl)-3-(3-chlorophenyl)-imidazolidin-2-one;
- (endo)-1-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-3-(3-chlorophenyl)-imidazolidin-2-one;
- (exo)-1-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-3-(3-chlorophenyl)-imidazolidin-2-one;
- (endo)-1-(8-methyl-8-azabicyclo [3.2.1] oct-3-yl)-3-(5-chloro-2-methoxyphenyl)-imidazolidin-2-one;
- (endo)-1-(9-methyl-9-azabicyclo [3.3.1] non-3-yl)-3-(5-chloro-2-methoxyphenyl)-imidazolidin-2-one;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.