Carboxylic acid derivatives and pharmaceutical compositions comprising the same as an active ingredient
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a technology of carboxylic acid and active ingredient, which is applied in the direction of application, extracellular fluid disorder, metabolic disorder, etc., and can solve the problem that the direct impact of s1p on intracellular substances has never been identified
Inactive Publication Date: 2007-04-19
ONO PHARMA CO LTD
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[0215] The above combination takes effects on whichever disease treating and / or preventing effect of the compounds of the present invention represented by formula (I) is complemented and / or enhanced.
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However, intracellular substance affected directly by S1P has never identified.
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reference example 1
methyl 3-[4-(5-phenylpentyloxy)phenyl]propanoate
[0231]
[0232] To a mixture of 5-phenylpentanol (3.7 mL), methyl 3-(4-hydroxyphenyl)propanoate (3.6g), triphenylphosphine (5.77 g) and dichloromethane (200 mL) was added 1,1′-(azodicarbonyl)dipiperidine (5.55 g). The reaction mixture was stirred at room temperature for 4 days. Diethyl ether was added to the reaction mixture, which was filtered and the filtrate was concentrated. Hexane-diethyl ether (1:1) (200 mL) was added to the residue, which was filtered and the filtrate was concentrated. The obtained residue was purified by column chromatography on silica gel (hexane: ethyl acetate=9:1→4:1) to give the title compound (6.16 g) having the following physical data.
[0236] To a solution of the compound prepared in Reference Example 1 (12 g) in methanol (60 mL) and tetrahydrofuran (80 mL) was added 2N aqueous sodium hydroxide solution (40 mL). The reaction mixture was refluxed for 4 hours. On ice bath, 1N hydrochloric acid was added to the reaction mixture, which was extracted with ethyl acetate. The extract was dried over anhydrous magnesium sulfate and concentrated to give the title compound (11.32 g) having the following physical data.
[0240] To a solution of the compound prepared in Reference Example 2 (151 mg) in dichloromethane (1 mL) was poured a drop of dimethylformamide. Further, to the mixture was added oxalyl chloride (0.13 mL) on ice bath. The reaction mixture was stirred at room temperature for 1 hour. The reaction mixture was concentrated to give the title compound (167 mg).
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Abstract
Compounds represented by formula (I), prodrugs thereof and salts thereof, and pharmaceutical compositions comprising the same as an active ingredient (wherein each symbol has the meaning as defined in the specification.). Because of having an EDG-1 agonism, the compounds represented by formula (I) are useful in preventing and / or treating peripheral arterial disease such as arteriosclerosis obliterans, thromboangiitis obliterans, Buerger's disease or diabetic neuropathy, sepsis, angiitis, nephritis, pneumonia, stroke, myocardial infarction, edematous state, atherosclerosis, varicosity such as hemorrhoid, anal fissure or fistula ani, dissecting aneurysm of the aorta, angina, DIC, pleuritis, congestive heart failure, multiple organ failure, bedsore, burn, chronic ulcerative colitis, Crohn's disease, heart transplantation, renal transplantation, dermal graft, liver transplantation, osteoporosis, pulmonary fibrosis, interstitial pneumonia, chronic hepatitis, liver cirrhosis, chronic renal failure, or glomerular sclerosis.
Description
TECHNICAL FIELD [0001] The present invention relates to carboxylic acid derivatives and pharmaceutical compositions comprising the same as an active ingredient. More specifically, the present invention relates to (1) carboxylic acid derivatives represented by formula (I) prodrugs thereof, non-toxic salts thereof, (2) the process for preparation thereof, and (3) EDG-1 agonist comprising carboxylic acid derivatives represented by above formula (I), prodrugs thereof and non-toxic salts thereof as an active ingredient. BACKGROUND ART [0002] In recent years, it is known that various lipid mediators such as eicosanoid, platelet activating factor (PAF) and lysophosphatidic acid (LPA) are produced by the activity of phospholipase from cell membranes. Moreover, sphingosine 1-phosphate (hereinafter abbreviated as S1P) is a lipid which is produced by metabolic turnover of sphingolipid, acts as a mediator for signal transduction and delivers various signals into cells. Firstly, it was reporte...
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Patent Type & Authority Applications(United States)