PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATING PSYCHIATRIC DISORDERS Russian patent published in 2010 - IPC C07D409/12 A61K31/435 A61P25/00 

Abstract RU 2402549 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel heterocyclic compounds of formula (1) , where ring Q represented by is , (where is NH-CH2-, -N-CH-, -CH2-NH- or -CH=N-; and the carbon-carbon bond between the 3rd position and the 4th position of the heterocyclic skeleton which contains Z and Y, is a single or double bond); ring Q can have at least one substitute selected from a group consisting of a lower alkyl group, lower alkenyl group, lower alkynyl group, hydroxy group, lower alkoxy group, halogenated lower alkyl group, aryl group, aryl lower alkyl group, aryl lower alkoxy group, arylcarbonyl group, lower alkenyloxy group, lower alkanoyl group, lower alkanoyloxy group, cycloalkyl group, cycloalkyl lower alkyl group, halogen atom, carbamoyl group which can have a lower alkyl group, carboxy group, lower alkoxycarbonyl group, amino group which can have a lower alkanoyl group, nitro group, hydroxy lower alkyl group, amino lower alkyl group which can have a lower alkyl group, thienyl group, lower alkyl group substituted with a saturated 3-8-member monoheterocyclic group containing 1-2 nitrogen atoms, and an oxo group; R2 is a hydrogen atom or a lower alkyl group; and A is -O-A1- (where A1 is an alkylene group which can be substituted with a hydroxy group (where the alkylene group may contain one oxygen atom) or a lower alkenylene group or a lower alkylene group; provided that if A is a lower alkylene group, Q is a bicyclic group selected from a group consisting of: (where the carbon-carbon bond is a single or double bond)] or salts thereof. The invention also relates to a pharmaceutical composition, to a method of preparing the pharmaceutical composition, to use of the formula (1) heterocyclic compound, as well as a method for synthesis of the heterocyclic compound.

EFFECT: obtaining novel biologically active compounds which have activity as a dopamine D2 receptor partial agonist and a serotonin receptor 5-HT2A antagonist, and an adrenaline receptor α1 antagonist, and serotonin uptake inhibitor or serotonin reuptake inhibitor.

15 cl, 197 ex, 24 tbl

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Authors

Jamasita Khirosi

Matsubara Dzun

Osima Kunio

Kuroda Khideaki

Ito Nobuaki

Mijamura Sin

Simizu Satosi

Tanaka Tatsuesi

Takakhasi Kharuka

Dates

2010-10-27Published

2006-04-12Filed