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A kind of technology of heterocycloheptatriene and compound, applied in the field of benzazepine compound, can solve problems such as no disclosure
Active Publication Date: 2015-05-27
ASTELLAS PHARMA INC
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[0016] However, the above-mentioned documents disclosing tricyclic benzazepine derivatives do not disclose 2,3,4,6,7,8,9,10-octahydro-1H-azepane Trieno[4,5-g]quinoline derivatives and 3,4,6,7,9,10-hexahydro[1,4] 5-HT of azino[2,3-h][3]benzazepine derivatives 2C receptor agonist activity
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[0243] Hereinafter, the production method of the compound of formula (I) and its raw material compound is demonstrated in more detail based on an Example. It should be noted that the present invention is not limited to the compounds described in the following examples. In addition, the production method of the raw material compound is shown in the production example. In addition, the production method of the compound of formula (I) is not limited to the production method of the specific examples shown below, and the compound of formula (I) can also be produced by a combination of these production methods or methods obvious to those skilled in the art manufacture.
[0244] In addition, the following abbreviations may be used in the manufacture examples, an Example, and the table|surface mentioned later.
[0245] PEx: Production example number, Ex: Example number, PSyn: Production example number produced by the same method, Syn: Example number produced by the same method, No: ...
manufacture example 1
[0251] Add 75 g of N-bromosuccinimide and 0.81 g of azobisisobutyronitrile to a solution of 27.11 g of 3-chloro-o-xylene in 300 ml of carbon tetrachloride, and heat to reflux for 2 hours. The reaction mixture was washed with water and saturated aqueous sodium bicarbonate, the organic layer was dried over anhydrous magnesium sulfate and filtered, and the filtrate was concentrated under reduced pressure to obtain 63.297 g of 1,2-bis(bromomethyl)-3- chlorobenzene.
manufacture example 2
[0253] To 9.5 g of sodium cyanide in 120 ml of aqueous solution was added 57.533 g of 1,2-bis(bromomethyl)-3-chlorobenzene in 120 ml of EtOH and heated to reflux for 30 minutes. The reaction mixture was poured into ice and stirred, and the precipitated solid was filtered off to obtain 32.941 g of 2,2'-(3-chloro-1,2-phenylene)diacetonitrile as a tan solid.
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Abstract
[Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
Description
technical field [0001] The present invention relates to as a pharmaceutical composition, especially as 5-HT 2C Receptor-related diseases, especially urinary incontinence such as stress urinary incontinence, urge urinary incontinence, and mixed urinary incontinence, sexual dysfunction such as erectile dysfunction, obesity, etc. The active ingredient of the pharmaceutical composition for the treatment or prevention of useful benzos Azepine compounds. Background technique [0002] 5-hydroxytryptamine 2C (5-HT 2C ) receptor is one of the receptors for the transmitter 5-hydroxytryptamine involved in various physiological functions in the organism. Its expression is mainly observed in the central nervous system (brain, spinal cord). [0003] as central 5-HT 2C The physiological function of the receptor is known to have an appetite suppressing effect, and it has been reported that various 5-HT in rats 2C Effect of receptor agonists on reducing food intake (Non-Patent Documents...
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