To obtain the subject new compound consisting of a specific tetracyclic 1,4-oxazine compound, having high affinity to D3 dopaminergic receptor, free from affinity to D2 dopaminergic receptor and useful e.g. for the treatment of Parkinson's disease, depression and psychosis.
The objective compound is a new tetracyclic 1,4-oxazine compound (the configuration of the link between the 1,4-oxazine ring and the adjacent group is trans) expressed by formula I [A-D-E is group of formula II ((p) is 2 or 3), group of formula III ((m) is 0, 1 or 2), etc.; X is CH2 or O; (n) is 0 or 1 when X is CH2 and is 1 when X is O; R is H, a 1-10C alkyl, a 3-10C alkenyl, a (substituted)phenyl, a (substituted)thienyl, a (substituted)pyridyl, etc.], its racemic compound, optical isomer or salt. The compound is useful e.g. for the treatment of Parkinson's disease, disturbance of memory, depression and psychosis. The compound can be produced e.g. by cyclizing a compound of formula IV [A'-D-E is (CH2)3, S(CH2)2, etc.] with an acid halide and oxidizing the product.
BERUTORAN GUMAN
JIYANNKURISUTOFU ARUMANJIYU
MARUKU MIRAN
BUARERII ODEINO
Next Patent: CALIXARENE DERIVATIVE