US 6,187,774 B1 · Fused heterocyclic compounds and pharmaceutical applications thereof

Abstract

The present invention relates to a fused heterocyclic compound of the formula (I) wherein each symbol is as defined in the specification, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive, and a medicament containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof. The compound of the present invention is a useful antipsychotic agent effective not only for positive symptoms centering on hallucination and delusion characteristic of the acute stage of schizophrenia, but also negative symptoms of apathy, abulia and autism. The inventive compound is expected to make a highly safe antipsychotic agent associated with less side effects, such as extrapyramidal symptoms and endocrine disturbance, which are observed when a conventional antipsychotic agent having a D2 receptor blocking action is administered. Therefore, the inventive compound can be used as a therapeutic agent for the diseases such as schizophrenia.

Claims9

Dependent claims

A compound of the formula (I)

wherein
R is a group having the following formula (3),
wherein
Y is a linear or branched C1-C4 alkylene optionally having a substituent R1a at an optional position, wherein R1a is alkyl, hydroxy, alkoxy, amino or alkylamino,
A is void, or an oxygen atom, a sulfur atom, SO, SO2 or N—R7 wherein R7 is hydrogen, alkyl, arylalkyl or acyl,
B is a linear or branched C1-C4 alkylene optionally having a substituent R1b at an optional position, wherein R1b is alkyl, hydroxy, alkoxy, amino or alkylamino, and
R3 is a hydrogen, an alkyl, an acyl or an aryl;
D is void, or a linear or branched alkylene having 1 to 8 carbon atoms;
Q—T is CH2—N;
G is void, or a linear or branched alkylene having 1 to 8 carbon atoms or a carbonyl;
R5 is a hydrogen or an alkyl;
and
R6 is an optionally substituted aryl, an optionally substituted heteroaryl or an optionally substituted fused heteroaryl, the optional substituent being selected from the group consisting of halogen, haloalkyl, alkyl, alkoxy, hydroxy, nitro, amino, methylamino and dimethylamino,
an optical isomer thereof or a pharmaceutically acceptable salt thereof.

11 more elements

Dependencies are inferred from the claim text.

Fused heterocyclic compounds and pharmaceutical applications thereof

Life of this patent

Fused heterocyclic compounds and pharmaceutical applications thereof

Life of this patent

Abstract

Claims9