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Indole carboxamide derivatives

A kind of technology of carboxamide and indole, applied in the field of indole carboxamide derivatives, can solve the problems without any reports etc.

Active Publication Date: 2017-03-08
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0032] However, there is no report in any of the literatures that MT1 and / or MT2 receptor agonists act on the urethra to be useful for the treatment of urinary incontinence, etc.

Method used

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  • Indole carboxamide derivatives
  • Indole carboxamide derivatives
  • Indole carboxamide derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0356] Hereinafter, the production method of the compound of formula (I) 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 obtained by a combination of these production methods or methods that are obvious to those skilled in the art to manufacture.

[0357] In addition, the following abbreviations may be used in Examples, Production Examples, and Tables described later.

[0358] PEx: production example number, Ex: example number, PSyn: production example number produced by the same method, Syn: example number produced by the same method, Str: chemical structural formula (Me: me...

manufacture example 1

[0362] Sodium borohydride (1.92 g), stirred at room temperature for 2 hours. Acetic acid was added to the reaction mixture under ice cooling, followed by water, and the precipitated solid was collected by filtration and dried to obtain 5-methoxy-3-(2-nitroethyl)-1H-indole- Ethyl 2-carboxylate (4.01 g).

manufacture example 2

[0364] Using continuous hydrogenation reaction device H-Cube (registered trademark) (ThalesNano company), 5-methoxy-3-(2-nitroethyl)-1H-indole-2-carboxylic acid ethyl ester (500mg), tetrahydrofuran (40.0mL) and acetic anhydride (2.00mL) mixed solution into the Raney nickel box (catalyst box: CatCart (registered trademark) (ThalesNano company) type Raney nickel, hydrogen pressure: 60bar, reaction temperature: 60 ℃, flow rate : 1mL / s, solution concentration: 0.05M). The resulting mixture was concentrated under reduced pressure, and the resulting residue was washed with a mixed solvent of hexane:ethyl acetate=2:1 to obtain 3-(2-acetamidoethyl)-5-methoxyl in the form of a white solid - 1H-Indole-2-carboxylic acid ethyl ester (450 mg).

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PUM

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Abstract

The object of the present invention is to provide compounds useful as MT1 and / or MT2 receptor agonists. The compound represented by the following formula (I) has MT1 and / or MT2 receptor agonist action, and central migration is low, thus can be used as the prevention and treatment of urinary system diseases such as urinary incontinence, lower urinary tract symptoms or symptoms of storage period. / or therapeutic agent use (wherein, Y is N or CR1, R1, R3, R4 are H or halogen etc., R2 is alkyl etc., R51, R52 are H or alkyl etc., X is bond, -NR11- or ‑NR11‑O‑(R11 is H or alkyl, etc.), R6 is alkyl or cycloalkyl, etc., R7, R8 are H or halogen, etc.).

Description

technical field [0001] The present invention relates to an indolecarboxamide derivative useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating stress urinary incontinence. Background technique [0002] Urinary incontinence refers to a state in which urine leaks unintentionally and is seen by others, which becomes a problem in society or hygiene (Non-Patent Document 1). Typical examples of urinary incontinence include urge incontinence, stress incontinence, functional incontinence, reflex incontinence, overflow incontinence, true incontinence, and mixed incontinence in which these incontinences are mixed. . [0003] The most common type of urinary incontinence is stress urinary incontinence, and it has been reported that 50% of women suffering from urinary incontinence are stress urinary incontinence (Non-Patent Document 2). Stress urinary incontinence is a disease in which urine inadvertently leaks out even th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/42A61K31/4045A61K31/407A61K31/437A61P13/10C07D471/04C07D491/048
CPCC07D209/42C07D471/04C07D491/048C07D491/147C07D491/052A61P13/00A61P13/10A61K31/4045A61K31/407
Inventor 金山隆俊久保田秀树松本俊一郎斋藤智之清水乔史加藤直人松井滋生
Owner ASTELLAS PHARMA INC