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Sulfonamide compound or salt thereof

一种化合物、磺酰胺的技术，应用在EP1受体拮抗剂领域，能够解决EP1受体拮抗作用未报道等问题

Inactive Publication Date: 2009-08-05
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0040] However, EP1 receptor antagonism of these compounds has not been reported at all

Method used

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  • Sulfonamide compound or salt thereof
  • Sulfonamide compound or salt thereof
  • Sulfonamide compound or salt thereof

Examples

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Effect test

reference example 1

[0336] 18.7 g of 3-chloro-dimethylaniline was dissolved in 120 mL of pyridine, 22.9 g of p-toluenesulfonyl chloride was added thereto in small portions over 30 minutes, and the mixture was stirred at room temperature overnight. The reaction solution was concentrated under reduced pressure, and water was added to the resulting residue, followed by extraction with ethyl acetate. The organic layer was washed with 1M hydrochloric acid, saturated brine, saturated aqueous sodium bicarbonate solution, and saturated brine, and then dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 34.6 g of N-(3-chloro-2-methylphenyl)-4-methylbenzenesulfonamide.

reference example 2

[0338] 34.5 g of N-(3-chloro-2-methylphenyl)-4-methylbenzenesulfonamide was dissolved in 232 mL of DMF, 21.4 g of ethyl bromoacetate and 19.3 g of potassium carbonate were added thereto, and the mixture was stirred at 100° C. 1 hour. The reaction solution was cooled to room temperature, and then water was added, followed by extraction with ethyl acetate. The organic layer was washed with brine, and then dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the resulting residue was purified by silica gel column chromatography (hexane:ethyl acetate=80:20) to obtain 34.6 g of N-(3-chloro-2-methylphenyl)-N-[ (4-Methylphenyl)sulfonyl]glycine ethyl ester.

reference example 3

[0340] 35.8 g of N-(3-chloro-2-methylphenyl)-N-[(4-methylphenyl)sulfonyl]glycine ethyl ester were dissolved in 157 mL of ethanol and 157 mL of 1,4-dioxane, Thereto was added 157 mL of a 1M aqueous sodium hydroxide solution, and the mixture was stirred at 60°C overnight. The reaction solution was cooled to room temperature, and then concentrated under reduced pressure. The residue was dissolved in water, and 1M hydrochloric acid was added to make it acidic, followed by extraction with ethyl acetate. The organic layer was washed with saturated brine, and then dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 29.3 g of N-(3-chloro-2-methylphenyl)-N-[(4-methylphenyl)sulfonyl]glycine.

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Abstract

Disclosed is a sulfonamide compound having a chemical structure characterized in that the compound has an amide structure wherein a carbon atom in the amide binds to a nitrogen atom in a sulfonamide through a lower alkylene, or a salt of the compound. The compound or the salt has a potent antagonistic activity against an EP1 receptor and is therefore useful as a therapeutic agent for a disease associated with an EP1 receptor, particularly lower urinary tract symptom.

Description

technical field [0001] The present invention relates to EP1 receptor antagonists useful as therapeutic drugs for lower urinary tract symptoms. The present invention also relates to sulfonamide compounds or pharmaceutically acceptable salts thereof useful as EP1 receptor antagonists. Background technique [0002] Overactive bladder, one of the diseases causing lower urinary tract symptoms, is a pathological condition in which a feeling of urgency to urinate occurs regardless of the presence or absence of urinary incontinence, and is usually accompanied by frequent urination and nocturnal urination (Non-Patent Document 1). At present, its treatment mainly uses anticholinergic drugs, showing a certain therapeutic effect. However, it is known to have side effects such as thirst, constipation, and vertigo, and in addition to the risk of urinary retention, it has been reported that it is difficult to use in patients with benign prostatic hypertrophy or the elderly. In addition, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61K31/18A61K31/195A61K31/197A61K31/198A61K31/235A61K31/24A61K31/275A61K31/341A61K31/343A61K31/381A61K31/40A61K31/4015A61K31/404A61K31/415A61K31/4196A61K31/423A61K31/426A61K31/44A61K31/4402A61K31/4406A61K31/4409A61K31/472A61K31/4965A61K31/50A61K31/505A61K31/5375A61P13/02A61P13/08A61P13/10A61P43/00C07C311/21C07C311/29C07D207/27C07D207/325C07D209/08C07D213/40C07D213/68C07D213/70C07D213/79C07D213/89C07D215/12C07D217/06C07D231/12C07D237/08C07D239/26C07D241/12C07D249/08C07D263/32C07D263/58C07D277/20C07D277/28C07D277/36C07D295/12C07D307/52C07D307/81C07D333/20C07D333/34C07D333/38C07D333/40C07D333/58C07K7/00
CPCA61K31/4402A61K31/381A61K31/275C07D333/34A61K31/415A61K31/235C07C311/47C07D213/79A61K31/4015A61K31/24A61K31/404C07D263/58A61K31/195C07D237/08C07C2102/10A61K31/216C07D215/12C07D307/81A61K31/18C07D209/08C07D333/40C07D217/06C07D333/58C07D213/70C07D207/325C07D333/38C07D213/40A61K31/343C07D277/28C07C2101/08A61K31/198C07D213/89A61K31/4196C07D213/68A61K31/426C07D333/20C07C311/14C07D277/20C07D239/26C07D231/12C07D249/08C07C2102/08C07C2101/14A61K31/341C07C311/19C07C323/49C07D295/12C07C311/21C07D241/12C07C2101/02C07D207/27A61K31/197C07D307/52A61K31/44C07D263/32C07D277/36C07C311/51A61K31/4406C07C311/29A61K31/423A61K31/40C07C2601/02C07C2601/08C07C2601/14C07C2602/08C07C2602/10A61P13/00A61P13/02A61P13/08A61P13/10A61P25/04A61P29/00A61P35/00A61P43/00
Inventor 久保田秀树户田进塚本一成福田悠太若山龙太郎大野一树渡边亨薊英范
Owner ASTELLAS PHARMA INC
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