THIOPHENE COMPOUNDS AND MEDICINAL USE THEREOF

Title:

THIOPHENE COMPOUNDS AND MEDICINAL USE THEREOF

Document Type and Number:

WIPO Patent Application WO/1998/031679

Kind Code:

A1

Abstract:

Thiophene compounds represented by general formula (1), optical isomers thereof, pharmaceutically acceptable salts thereof, or hydrates of the same, wherein each symbol is as defined in the specification; and medicinal compositions containing as the active ingredient the compounds of general formula (1), optical isomers thereof, pharmaceutically acceptable salts thereof, or hydrates of the same together with pharmaceutically acceptable additives. Because of exerting selective and potent blocking effects on D�4? receptors rather than D�2? receptors, these compounds are useful as antipsychotic agents efficacious not only against positive symptoms typified by hallucination and delusion characteristic to the acute stage of schizophrenia but also negative symptoms such as emotional torpidity, abulia and autism. Moreover, they are applicable as useful antipsychotic agents which are excellent in oral absorbability, bioavailability and intracerebral transmigration properties while showing relieved side effects caused by the administration of the existing antipsychotic agents with a D�2? receptor antagonism, such as extrapyramidal symptoms and disendocriasis. These compounds are also usable as remedies for alcohol dependence and drug abuse.

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Inventors:

KUROITA TAKANOBU (JP)
TOGO YOSHIFUMI (JP)
FUJIO MASAKAZU (JP)
FUTAMURA TAKASHI (JP)

Application Number:

PCT/JP1998/000077

Publication Date:

July 23, 1998

Filing Date:

January 09, 1998

Export Citation:

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Assignee:

YOSHITOMI PHARMACEUTICAL (JP)
KUROITA TAKANOBU (JP)
TOGO YOSHIFUMI (JP)
FUJIO MASAKAZU (JP)
FUTAMURA TAKASHI (JP)

International Classes:

C07D333/56; C07D333/58; (IPC1-7): C07D333/58; A61K31/38; A61K31/44; A61K31/495; C07D409/06

Foreign References:

JPS473521A
JPH0285277A	1990-03-26
JPH05262759A	1993-10-12
JPH08325257A	1996-12-10

Attorney, Agent or Firm:

Takashima, Hajime (3-9 Hiranomachi 3-chome, Chuo-k, Osaka-shi Osaka 541, JP)

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