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Aminoalkyl-substituted n-thienyl benzamide derivative

An alkyl and amino technology, applied in the field of N-thienylbenzamide derivatives, can solve the problems of no revelation of NPT-IIb inhibitory effect, no disclosure, etc.

Active Publication Date: 2014-07-02
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] However, in Patent Documents 4 to 6, there is neither disclosure nor suggestion that these compounds have NPT-IIb inhibitory effect or can be used for the prevention or treatment of hyperphosphatemia

Method used

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  • Aminoalkyl-substituted n-thienyl benzamide derivative
  • Aminoalkyl-substituted n-thienyl benzamide derivative
  • Aminoalkyl-substituted n-thienyl benzamide derivative

Examples

Experimental program
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Embodiment

[0187] 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 methods of the raw material compounds are shown in the production examples, respectively. 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 .

[0188] In addition, the following abbreviations are sometimes used in Examples, Production Examples, and Tables described below.

[0189] Pr: Manufacturing example number, Ex: Example number, Str: Structural formula (the compound with "*" in the structural formula is a chiral compound whose carbon atom is the asymmetric center. In the structural f...

manufacture example 1

[0193] To a mixture of 6.2 mL of 2-(methylamino)ethanol, 6.48 g of sodium bicarbonate, 60 mL of THF and 30 mL of water was added dropwise 10 mL of ethyl succinic acid chloride over 30 minutes under ice-cooling, followed by stirring for 3 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (hexane:ethyl acetate=1:4) to obtain 4-[(2-hydroxyethyl)(methyl)amino]-4-oxo Ethyl butyrate 12.0g.

manufacture example 2

[0195] Slowly add 26.0 g of Dess-Martin periodinane to a mixture of 11.9 g of ethyl 4-[(2-hydroxyethyl)(methyl)amino]-4-oxobutanoate and 120 mL of dichloromethane under ice cooling , and warmed to room temperature over 3 hours. Aqueous sodium bicarbonate and aqueous sodium thiosulfate were added to the reaction mixture, followed by stirring at room temperature for 30 minutes. The aqueous layer was extracted with dichloromethane, the organic layers were combined, dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (hexane:ethyl acetate=1:4) to obtain 4.48 g of ethyl 4-[methyl(2-oxoethyl)amino]-4-oxobutanoate.

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Abstract

The objective of the present invention is to provide a compound having inhibitory activity against an intestinal phosphate transporter (NPT-IIb), and useful as an active ingredient in a hyperphosphatemia therapeutic agent and / or preventive. A thiophene compound represented by formula (I) may be used as a hyperphosphatemia therapeutic agent and / or preventive having NPT-IIb inhibitory activity. (In the formula, R1-6 each represent H or a lower alkyl or the like, L1-4 each represent a lower alkyl or the like, X1 represents CH2 or O, X2-3 each represent CH or N, k is 1-3, and n is 0-1.)

Description

technical field [0001] The present invention relates to an aminoalkyl-substituted N-thienylbenzamide derivative useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating hyperphosphatemia. Background technique [0002] Phosphorus is an essential element for sustaining life and plays a very important role in various biological functions. Phosphorus is mainly absorbed from food in the form of phosphoric acid through the digestive tract, and almost all of it is excreted into urine, thereby maintaining and regulating the total amount in the body. It is known that almost all phosphoric acid is filtered by the glomeruli during the production of urine, and only the necessary amount of phosphoric acid is reabsorbed by the renal tubules. Therefore, when the glomerular filtration capacity decreases with the progress of renal failure, phosphorus excretion becomes insufficient, showing an abnormal increase in serum phosphorus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D333/68A61K31/381A61K31/439A61K31/4436A61K31/444A61K31/4535A61K31/496A61K31/506A61K31/5377A61P7/00A61P13/12A61P19/00A61P43/00C07D333/78C07D333/80C07D409/12C07D409/14C07D413/12C07D417/12C07D453/02C07D495/04
CPCC07D453/02C07D409/14C07D495/04C07D333/68C07D413/12C07D409/12C07D333/80C07D333/78C07D417/12C07D333/38C07D498/04C07F9/655354A61P13/12A61P19/00A61P3/12A61P43/00A61P7/00
Inventor 三浦理宪加贺大辅四月朔日晋八谷俊一郎奥田崇男佐藤一平矶村真衣寺居和宏寺田央
Owner ASTELLAS PHARMA INC
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