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Guanidinobenzoic acid compound

A kind of guanidinobenzoyl, compound technology, applied in the field of pharmaceutical compositions, can solve the problems such as undisclosed or enlightenment

Active Publication Date: 2014-05-14
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, specific compounds of the compound of formula (I) or a salt thereof of the invention of the present application described later are not disclosed or suggested.

Method used

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  • Guanidinobenzoic acid compound
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  • Guanidinobenzoic acid compound

Examples

Experimental program
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Embodiment

[0289] 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 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 .

[0290] In addition, the following abbreviations are sometimes used in Examples, Production Examples, and Tables described below.

[0291] PEx: Manufacturing example number (the compound with "*" in the table indicates that the compound is an optically active substance), Ex: Example number (in addition, the compound with "*" in the table indicates that the compound ...

manufacture example 1

[0298] Potassium carbonate (1.61g) and benzyl bromide (1.46mL) were added to a solution of 4-(4-hydroxyphenyl)butyric acid (2.00g) in N,N-dimethylformamide (28.0mL), at room temperature Stir overnight. After concentrating the reaction suspension under reduced pressure, water was added to the residue, followed by extraction with ethyl acetate. The organic layer was washed with water and a saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane-ethyl acetate) to obtain benzyl 4-(4-hydroxyphenyl)butyrate (2.64 g).

manufacture example 2

[0300] To a solution of 4-[N',N''-bis(tert-butoxycarbonyl)guanidino]benzoic acid (2.96 g) in dichloromethane (20.0 mL) was added 1-[3-(dimethylamino)propane Base]-3-ethylcarbodiimide hydrochloride (1.80g), 4-(4-hydroxyphenyl)butyric acid benzyl ester (2.00g) and N,N-dimethyl-4-aminopyridine ( 286 mg), stirred overnight at room temperature. After adding 1M hydrochloric acid to the reaction solution, it was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (hexane-ethyl acetate) to obtain 4-[N',N''-bis(tert-butoxycarbonyl)guanidino]benzoic acid 4-[4-(benzyloxy) -4-oxobutyl]phenyl ester (3.98 g).

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Abstract

The object of the present invention is to provide a compound useful as a renal disease preventive and / or therapeutic agent. The inventors of the present invention investigated compounds having a trypsin inhibitory activity, verified that a guanidinobenzoic acid compound has a trypsin inhibitory activity, and achieved the present invention. This guanidinobenzoic acid compound can be used as: a renal disease preventive and / or therapeutic agent that serves as a substitute drug in a low-protein diet regimen; and a preventive and / or therapeutic agent against diseases to which trypsin contributes such as pancreatitis, reflux esophagitis, hepatic encephalopathy, and influenza.

Description

technical field [0001] The present invention relates to a pharmaceutical composition, for example, a guanidinobenzoic acid compound useful as an active ingredient of a pharmaceutical composition for treating renal failure. Background technique [0002] For Chronic Kidney Disease (Chronic Kidney Disease (hereinafter referred to as CKD)), low-protein diet therapy has been practiced since ancient times. The mechanism of its effect is not yet clear. It is believed that by inhibiting the intake of protein from the diet, it mainly (1) reduces the total amount of nitrogen compounds produced by protein, thereby reducing the load on the glomeruli; (2) inhibits uremia that causes kidney damage. (3) Inhibit the accumulation of phosphorus and potassium; (4) Inhibit the production of acid; etc. In recent years, clinical trials have also demonstrated the effect of low-protein diet therapy on delaying the progress of CKD ((a) "The New England Journal of Medicine", 1989, Vol. 321, No. 26, ...

Claims

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Application Information

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IPC IPC(8): C07C279/18A61K31/404A61P13/12A61P43/00C07C307/10C07D207/16C07D209/20C07D209/42C07D211/62C07D213/79C07D215/20C07D215/48C07D215/50C07D233/64C07D257/04C07D271/06C07D277/20C07D277/56C07D295/12C07D333/38C07D333/40A61K31/155A61K31/245A61K31/381A61K31/401A61K31/405A61K31/4172A61K31/4245A61K31/426A61K31/44A61K31/445A61K31/4453A61K31/47A61K31/5375
CPCC07D213/79C07D215/20C07D215/48C07D215/50C07D333/38C07D333/40C07D233/64C07D257/04C07D271/06C07D207/16C07D277/20C07D277/56C07D209/20C07D209/42C07D295/12C07D211/62C07B2200/07C07C2601/02C07C2601/14C07C279/18C07D217/26C07D271/07C07D295/13A61P13/12A61P43/00
Inventor 藤安次郎大根和彦山木晋今泉智祯本渡猛松浦圭介佐藤知兴笹村智司
Owner ASTELLAS PHARMA INC
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