BENZOTHIOPHENE DERIVATIVES, USE AND COMPOSITION THEREOF

1. Benzothiophene derivative compounds of the general formula (I): where: Z is: -CO-, -CH(OR6)-, -C(NOR7)-; R1 is: H, C1-C6 alkyl, halogen, or -OR8; R2 and R3 are independently H, C1-C6 alkyl, halogen, -OR8, nitro, cyano, -NR9R10, -COR8, -CO2R8, -SO2NR9R10, -SO2R8, -SR8, -CONR9R10; R4 and R5 are the...

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Hauptverfasser: DEL CASTILLO NIETO, JUAN CARLOS, MONGE VEGA, ANTONIO, ROCA ACIN, JUAN, BOSCH ROVIRA, ANNA, DEL RIO ZAMBRANA, JOAQUIN, LASHERAS ALDAZ, BERTA, PALOPCUBILLO, JUAN ANTONIO
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:1. Benzothiophene derivative compounds of the general formula (I): where: Z is: -CO-, -CH(OR6)-, -C(NOR7)-; R1 is: H, C1-C6 alkyl, halogen, or -OR8; R2 and R3 are independently H, C1-C6 alkyl, halogen, -OR8, nitro, cyano, -NR9R10, -COR8, -CO2R8, -SO2NR9R10, -SO2R8, -SR8, -CONR9R10; R4 and R5 are the same or different and stand for: H, C1-C6 alkyl, halogen, haloalkyl, -OR8, nitro, -NR9R10, -COR8, -CO2R8, -SO2NR9R10, -SO2R8, -SR8, cyano, -CONR9R10, or R4 and R5 together form a benzene ring fused to the phenyl ring; R6 is H, C1-C6 alkyl, CO2R8, -C(O)NR9R10, naphthyl or phenyl optionally substituted by one or more substituents selected from H, haloalkyl, alkyl, halogen, C1-C6 alkoxy, methylenedioxy, nitro, cyano; R7 is H or C1-C6 alkyl; R8 is H, C1-C6 alkyl, or phenyl; R9 and R10 are independent and stand for H, C1-C6 alkyl or phenyl or R9 and R10, together with the atom of N to which they are attached, form a 5- or 6- membered ring in which there may optionally be an atom of N, O or S; or a salt or a solvate, or a geometric isomer or an optical isomer or polymorphs thereof. 2. The compounds of Claim 1, where Z is -CO-: 1-(benzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan- 1-one hydrochloride; 1-(3,5-dimethylbenzo[b]thiophen-2-yl)-3-[4-(2-methoxyphenyl)piperazin- 1-yl]propan-1-one hydrochloride; 1-(5-fluorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl ]propan-1-one; 1-(5-chlorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl ]propan-1-one hydrochloride; 3. The compounds of Claim 1, where Z is -CH(OR6)-: 1-(benzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan- 1-ol; 1-(benzo[b]thiophen-3-yl)-3-[4-(2-hydroxyphenyl)piperazin-1-yl]propan- 1-ol; 1-(3,5-dimethylbenzo[b]thiophen-2-yl)-3-[4-(2-methoxyphenyl)piperazin- 1-yl]propan-1-ol; 1-(3-methylbenzol[b]thiophen-2-yl)-3-[4-(2-hydroxyphenyl)piperazin-1-y l]propan-1-ol; 1-(5-chlorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl ]propan-1-ol; 1-(5-fluorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl ]propan-1-ol; 4. The compounds of Claim 1, where Z is -C(NOR7)-: 1-(benzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan- 1-one oxime; 5. The use of a compound according to any one of Claims 1 to 4 for the preparation of a pharmaceutical composition for the treatment of neurological disorders. 6. The use of Claim 5, for the preparation of a pharmaceutical composition for the treatment of anxiety and/or depression. 7. A pharmaceuti