Fused thiophene compounds and uses thereof

Details Fused thiophene compounds and uses thereof Fused thiophene compounds and uses thereof

1991-07-08

1992-08-25

Bond, Robert T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514215, 540453, 540455, 540461, 540490, 540521, C07D28536, C07D28538, A61K 3155, A61K 3138

Patent

active

051419300

ABSTRACT:
A fused thiophene compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof. In the above formula, one of E.sup.1, E.sup.2 and E.sup.3 is sulfur atom and other two of them are C--R.sup.1 and C--R.sup.2 respectively. R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, nitro, amino, cyano, hydroxyl, formyl, alkyl, alkoxy, haloalkyl, arylalkyl, acyl, alkoxyalkyl, acyloxyalkyl, hydroxyalkyl, acyloxyalkanoyl, alkoxyalkanoyl, hydroxyalkanoyl, aryloxyalkanoyl, haloalkanoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, hydroxysulfonyl, halosulfonyl, sulfamoyl, substituted sulfamoyl, carboxyl, acylamino, alkoxycharbonyl, carbamoyl, substituted carbamoyl or substituted amino. D is --CH.sub.2 -- or --S(O).sub.m -- (m is 0, 1 or 2). Q is straight or branched chain alkylene. T is primary amino, secondary amino or tertiary amino. A and B are the same or different and each is carbonyl or thiocarbonyl, or one of A and B is absent and the other of them is carbonyl or thiocarbonyl, or A is --CH.sub.2 -- and B is carbonyl or thiocarbonyl, and n is 1, 2 or 3 with the proviso that n is 2 or 3 when one of A and B is absent and the other of them is carbonyl or thiocarbonyl, and n is 1 or 2 when A and B are other combinations. In the above definitions, (hetero)aromatic ring and heterocyclic ring may optionally be substituted by 1 to 3 substituents. Said compounds have selective affinity for 5-HT.sub.1A receptor, or high affinity for 5-HT.sub.1A and dopamine D.sub.2 receptors so that they are useful as antianxietic drug, antipsychotic drug or drug for the disease of circulatory system. The intermediates for said fused thiophene compounds are also disclosed.

REFERENCES:
patent: 4735940 (1988-04-01), Fischer et al.
patent: 4833142 (1989-05-01), Hartog et al.
patent: 4895841 (1990-01-01), Sugimoto et al.
Chemical Abstracts, vol. 55, 1961, col. 23488.
Chemical Abstracts, vol. 59, 1963, col. 3862.
Chemical Abstracts, vol. 64, 1966, col. 586.
Chemical Abstracts, vol. 69, 1968, 18565x.

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