Title:
FUSED TRIAZOLE COMPOUNDS
Document Type and Number:
WIPO Patent Application WO/1997/003986
Kind Code:
A1
Abstract:
Fused triazole compounds represented by general formula (1), optical isomers thereof, pharmaceutically acceptable salts thereof, medicinal compositions comprising the same, and radioactive fused triazole optical isomers thereof and salts thereof, wherein each symbol is as defined in the specification. The fused triazole compounds, optical isomers thereof or pharmaceutically acceptable salts thereof are D4 receptor antagonists having a selective and potent blocking effect on the D4 receptor. Thus, they are a useful antipsychotic agent which is efficacious against not only positive symptoms typified by hallucination, delusion, etc., characteristic to the acute state of schizophrenia but also negative symptoms such as apathy, autism, etc. Also, they are expected as an antipsychotic agent with relieved side effects, for example, extrapyramidal symptoms and endocrine abnormalities accompanying the administration of conventional antipsychotic agents having D2 receptor antagonism. Thus the compounds are usable as a remedy for diseases such as schizophrenia. Further, the radioactive fused triazole compounds are useful as a radioligand having an affinity for the human or animal D4 receptor.
Inventors:
TANAKA HIROSHI (JP)
KUROITA TAKANOBU (JP)
ISHIBUCHI SEIGO (JP)
USHIO HIROYUKI (JP)
FUTAMURA TAKASHI (JP)
OHASHI YOSHITAKA (JP)
YANO KAZUHIRO (JP)
KUROITA TAKANOBU (JP)
ISHIBUCHI SEIGO (JP)
USHIO HIROYUKI (JP)
FUTAMURA TAKASHI (JP)
OHASHI YOSHITAKA (JP)
YANO KAZUHIRO (JP)
Application Number:
PCT/JP1996/002004
Publication Date:
February 06, 1997
Filing Date:
July 17, 1996
Export Citation:
Assignee:
YOSHITOMI PHARMACEUTICAL (JP)
TANAKA HIROSHI (JP)
KUROITA TAKANOBU (JP)
ISHIBUCHI SEIGO (JP)
USHIO HIROYUKI (JP)
FUTAMURA TAKASHI (JP)
OHASHI YOSHITAKA (JP)
YANO KAZUHIRO (JP)
TANAKA HIROSHI (JP)
KUROITA TAKANOBU (JP)
ISHIBUCHI SEIGO (JP)
USHIO HIROYUKI (JP)
FUTAMURA TAKASHI (JP)
OHASHI YOSHITAKA (JP)
YANO KAZUHIRO (JP)
International Classes:
C07D498/04; (IPC1-7): C07D487/04; A61K31/435; A61K31/445; A61K31/495; A61K31/55; C07D495/14; C07D498/04
Foreign References:
| US3992539A | 1976-11-16 | |||
| US3814711A | 1974-06-04 | |||
| FR1573135A | 1969-07-04 | |||
| JPH06501488A | 1994-02-17 |
Other References:
CHEMICAL ABSTRACTS, Vol. 18, Abstract No. 91434, 1974; & EUR. J. MED. CHEM.-CHIM. THER., 9(2) 197-201, issued 1974.
TAKEDA KENKYUSHO HO, 32(2), 106-10 issued June 1973 (Osaka Japan), YUGUCHI, SYOJIRO et al., "Syntheses of N. Heterocyclic Compounds. XV. Reaction of Fused S-Triazolo Derivatives".
TAKEDA KENKYUSHO HO, 32(2), 106-10 issued June 1973 (Osaka Japan), YUGUCHI, SYOJIRO et al., "Syntheses of N. Heterocyclic Compounds. XV. Reaction of Fused S-Triazolo Derivatives".
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