NOVEL THIOPHENE DERIVATIVES AND DRUG COMPOSITIONS CONTAINING THE SAME

Title:

NOVEL THIOPHENE DERIVATIVES AND DRUG COMPOSITIONS CONTAINING THE SAME

Document Type and Number:

WIPO Patent Application WO/1998/000420

Kind Code:

A1

Abstract:

Thiophene derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds act as an anti-PCP agonist, thus being useful as psychotropic or antischizophrenic agents and so on. In said formula R�1? is -A�1?-X�1?-R�3?; R�2? is -A�2?-X�2?-R�4? or nil; B is a four- to ten-membered nitrogenous cycloalkyl or a five- or six-membered nitrogenous unsaturated heterocycle; Ar is aryl or heteroaryl; A�1?, A�2? and A�3? are each independently a bond or lower alkylene; X�1? and X�2? are each independently a bond, -O-, -S- or the like; and R�3? and R�4? are each independently hydrogen, cyclic imido, lower alkyl, cycloalkyl, aryl or aralkyl, with the provisos that when Ar is a thiazole ring, at least either of A�1? and A�2? is lower alkylene and that when Ar is a benzene ring, compounds wherein one of R�1? and R�2? is methyl or halogeno and the other thereof is hydrogen are excepted.

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Inventors:

KIMURA TAKENORI (JP)
MURAKAMI TAKESHI (JP)
OHMORI JUNYA (JP)
MORITA TAKUMA (JP)
TSUKAMOTO SHIN-ICHI (JP)

Application Number:

PCT/JP1997/002255

Publication Date:

January 08, 1998

Filing Date:

June 30, 1997

Export Citation:

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Assignee:

YAMANOUCHI PHARMA CO LTD (JP)
KIMURA TAKENORI (JP)
MURAKAMI TAKESHI (JP)
OHMORI JUNYA (JP)
MORITA TAKUMA (JP)
TSUKAMOTO SHIN ICHI (JP)

International Classes:

A61K31/4245; C07D333/24; C07D409/04; C07D409/06; C07D409/14; C07D413/04; C07D413/14; C07D417/04; C07D471/04; C07D487/04; C07D521/00; (IPC1-7): C07D333/24; C07D413/04; C07D409/04; C07D417/04; C07D413/14; C07D487/04; A61K31/38; A61K31/41; A61K31/415; A61K31/55

Domestic Patent References:

WO1994025450A1	1994-11-10
WO1993003025A1	1993-02-18

Foreign References:

JPH06509561A	1994-10-27
JPH04235145A	1992-08-24

Other References:

EFFENBERGER F, WUERTHNER F, STEYBE F: "SYNTHESIS AND SOLVATOCHROMIC PROPERTIES OF DONOR-ACCEPTOR-SUBSTITUTED OLIGOTHIOPHENES", THE JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 60, no. 07, 1 January 1995 (1995-01-01), US, pages 2082 - 2091, XP002907328, ISSN: 0022-3263, DOI: 10.1021/jo00112a032
See also references of EP 0921123A4

Attorney, Agent or Firm:

Nagai, Shozo (Patent & Information Dept., 17-1, Hasune 3-chom, Itabashi-ku Tokyo, JP)

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