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Carbamate compound or salt thereof

A technology of compounds and base esters, applied in the field of carbamate compounds or their salts, which can solve the problems of insufficient effect in patients with nocturia

Inactive Publication Date: 2011-10-05
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is because the causes of daytime frequent urination and nocturia are different. The causes of nocturia include nocturnal polyuria, decreased nighttime bladder capacity, and sleep disturbance. Shows an effect in patients with frequent urination, but not sufficiently in patients with nocturia (Int Urogynecol J, Vol. 18, pp. 737-741, 2007)

Method used

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  • Carbamate compound or salt thereof
  • Carbamate compound or salt thereof
  • Carbamate compound or salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0162] Hereinafter, the production method of the compound of formula (I) is demonstrated in more detail based on an Example. In addition, 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 as 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.

[0163] In addition, the following abbreviations may be used in Examples, manufacture examples, and the table|surface mentioned later.

[0164] Pre: Production example number, Ex: Example number, Cpd: Compound number, Str: Structural formula, Syn: Preparation method (indicates the production example number or example number that was produced in the sa...

manufacture example 1

[0166] Add 4-fluorobenzene-1,2-diamine acetic acid (10ml) solution to 2,2,2-methyl trichloroacetimidate (1.53g) in acetic acid (10ml) solution under ice-cooling, at room temperature Stirring was continued for 3 hours. The reaction solution was concentrated under reduced pressure, water was added to the obtained residue, neutralized with saturated aqueous sodium bicarbonate solution, and extracted with EtOAc. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. iPr for residue 2 Recrystallization from O / EtOAc / MeOH afforded 5-fluoro-2-(trichloromethyl)-benzimidazole (1.5 g) as a beige powder. To 1M aqueous sodium hydroxide solution (30 ml) was added 5-fluoro-2-(trichloromethyl)-benzimidazole (500 mg) under ice-cooling, followed by stirring for 1 hour. 1M hydrochloric acid was added to the reaction solution to make it acidic. The resulting solid was filtered off and dried under reduced pressur...

manufacture example 2

[0168] A mixture of tert-butyl piperazine-1-carboxylate (1.75 g), benzimidazole-2-carboxylic acid (1.69 g), HOBt (1.52 g), WSC (1.75 g) and DMF (35 ml) was stirred overnight at room temperature . Saturated aqueous sodium bicarbonate solution was added to the reaction liquid, followed by extraction with EtOAc. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and then concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent: Hex:EtOAc=2:1 (V / V)) to give 4-(benzimidazol-2-ylcarbonyl)piperazine-1-carboxylic acid as white powder tert-Butyl ester (2.4 g).

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Abstract

Disclosed is a compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases. Extensive studies have been made on compounds having an FAAH-inhibiting activity, and it is confirmed that a piperazine-1-carboxylate compound having a benzimidazol-2-ylcarbonyl, a benzofuran-2-ylcarbonyl or the like bound to position-4 in the piperazine moiety has an excellent FAAH-inhibiting activity and has an activity to increase the effective bladder capacity, an activity to ameliorate sleep disorder, an anti-diuretic activity and an analgesic activity on lower urinary tract pain including bladder pain. The carbamate compound has an excellent FAAH-inhibiting activity and can be used as a prophylactic and / or therapeutic agent for FAAH-related diseases, particularly nycturia, interstitial cystitis, painful bladder syndrome or chronic non-bacterial prostatitis / chronic pelvic pain syndrome.

Description

technical field [0001] The present invention relates to a carbamate compound or a salt thereof useful as an active ingredient of a pharmaceutical composition, particularly a pharmaceutical composition for treating FAAH-related diseases. Background technique [0002] Frequent urination can be broadly classified into diurnal frequency and nocturia (Journal of the Japanese Society of Urinary Function, Vol. 14, 2003). Daytime frequent urination refers to a self-reported symptom of a patient who urinates excessively during the day, and the number of daytime frequent urination (for example, more than 8 times) is sometimes specified for convenience. On the other hand, nocturia refers to "complaints of having to wake up at night to urinate one or more times" and is defined as a new disease (International Continence Society: ICS, 2002). The occurrence of nocturia is considered to be related to various causes, and the main factors include nocturnal polyuria, decreased nocturnal bladd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/496A61P7/12A61P13/00A61P13/08A61P13/10A61P25/20C07D405/12C07D409/12C07D417/12
CPCC07D413/04C07D409/12C07D405/12C07D401/12C07D417/12A61K31/496A61P13/00A61P13/08A61P13/10A61P25/20A61P43/00A61P7/12C07D401/14C07D409/14
Inventor 石井孝拓菅根隆史宗像亮介青木敏桧垣雅英染谷晃好
Owner ASTELLAS PHARMA INC
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