Tetraisoquinoline compounds which have useful pharmaceutical utility
AssigneeThe Boots Company PLC
InventorsAntonin Kozlik, Bruce J. Sargent, Patricia L. Needham
Life of this patent
Estimating the term…
Abstract
Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts and lipophilic ester thereof have utility as analgesics and in the treatment of psychoses, Parinson's disease, Lesch-Nyan syndrome, attention deficit disorder or cognitive impairment or in the relief of drug dependence or tardive dyskinesia.
Claims18
A tetrahydroisoquinoline compound of formula I ##STR39## or a pharmaceutically acceptable salt thereof, in which, R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl of 1 to 3 carbon atoms (optionally substituted by hydroxy), alkoxy of 1 to 3 carbon atoms, alkylthio of 1 to 3 carbon atoms, alkylsulphinyl of 1 to 3 carbon atoms, alkylsulphonyl of 1 to 3 carbon atoms, nitro, cyano, polyhaloalkyl of 1 to 3 carbon atoms, polyhaloalkoxy of 1 to 3 carbon atoms, phenyl (optionally substituted by one or more substituents selected from halo, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms), or R.sub.1 is carbamoyl optionally alkylated by one or two alkyl groups each independently of 1 to 3 carbon atoms;
- R.sub.2 represents an aliphatic group containing 1 to 3 carbon atoms optionally substituted by hydroxy or alkoxy containing 1 to 3 carbon atoms;
- E represents an alkylene chain containing 2 to 5 carbon atoms optionally substituted by one or more alkyl groups containing 1 to 3 carbon atoms,
- and G represents phenyl or phenyl substituted by one or more substituents which may be the same or different, and which are independently alkyl of 1 to 3 carbon polyhaloalkyl of 1 to 3 carbon atoms, halo, hydroxy, polyhaloalkyl of 1 to 3 carbon atoms, polyhaloalkoxy of atoms, alkylsulphinyl of 1 to 3 carbon atoms, alkylsulphonyl of 1 to 3 carbon atoms, phenyl (optionally substituted by one or more substituents selected from halo, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms), carbamoyl optionally alkylated by one or two alkyl groups each independently of 1 to 3 carbon atoms, or G represents a phenyl ring having fused thereto a heterocyclic or aromatic carbocyctic ring;
- and compounds of formula I which are O-acylated in the 5, 6, 7, or 8-position in the tetrahydroisoquinoline ring.
A tetrahydroisoquinoline compound of formula II ##STR40## or a pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, E and G are as defined in any preceding claim and compounds of formula II which are O-acylated in the 7 position in the tetrahydroisoquinoline ring.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I, together with a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.