Fused thiophene compounds and uses thereof

专利名称：Fused thiophene compounds and uses

thereof

发明人：Nakao, Tohru,Tanaka, Hiroshi,Yamato,

Hirotake,Akagi, Takeshi,Takehara, Shuzo

申请号：EP91306095.0申请日：19910704公开号：EP04652A1公开日：19920108

摘要：A fused thiophene compound of the formula: or a pharmaceutically acceptableacid addition salt thereof. In the above formula, one of E¹, E² and E³ is sulfur atom andother two of them are C-R¹ and C-R² respectively. R¹ and R² are the same or different andeach 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, substitutedsulfamoyl, carboxyl, acylamino, alkoxycarbonyl, carbamoyl, substituted carbamoyl orsubstituted amino. D is -CH₂- or -S(0)- (m is 0, 1 or 2). Q is straight or branched chainalkylene. T is primary amino, secondary amino or tertiary amino. A and B are the same ordifferent and each is carbonyl or thiocarbonyl, or one of A and B is absent and the otherof them is carbonyl or thiocarbonyl, or A is -CH₂- and B is carbonyl or thiocarbonyl, and nis 1, 2 or 3 with the proviso that n is 2 or 3 when one of A and B is absent and the other ofthem is carbonyl or thiocarbonyl, and n is 1 or 2 when A and B are other combinations. Inthe above definitions, (hetero)aromatic ring and heterocyclic ring may optionally be

substituted by 1 to 3 substituents. Said compounds have selective affinity for 5-HTreceptor, or high affinity for 5-HT and dopamine D₂ receptors so that they are useful asantianxietic drug, antipsychotic drug or drug for the disease of circulatory system. Theintermediates for said fused thiophene compounds are also disclosed.

申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

地址：6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 1 JP

国籍：JP

代理机构：Hardisty, David Robert

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