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2-aminobenzoyl derivatives

A technology of aminobenzoyl and formyl, applied in the field of 2-aminobenzoyl derivatives, can solve problems such as promoting excitotoxicity and neurotoxicity

Inactive Publication Date: 2010-09-29
NEURIM PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Endogenous quinolinic acid may cause activation of NMDA receptors to promote excitotoxicity and neurotoxicity, leading to physiological and pathological processes mediated by NMDA receptors

Method used

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  • 2-aminobenzoyl derivatives
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  • 2-aminobenzoyl derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: 2-(2-aminobenzoyl)-N-(2,4-dinitrophenyl)ethylamine

[0035]

[0036] Kynuramine.2HBr (125 mg) was dissolved in 5 cc of absolute ethanol in a 50 cc flask. Then 5 cc of ethanol solution of 71 mg of 2,4-dinitrofluorobenzene was added (a clear yellow solution was formed). After five minutes, drop 2cc of 10% NaHCO into the flask 3 solution. React overnight at room temperature. The yellowish precipitate formed the next morning was filtered, washed with water and ethanol and dried in UHV to afford 80 mg of product (63% approximate yield).

Embodiment 2

[0037] Example 2: 3-(2-aminobenzoyl)-2-(2,4-dinitroanilino)propionic acid

[0038]

[0039] L-kynurenine (125 mg) was dissolved in 5 cc of absolute ethanol in a 50 cc flask. Then 5 cc of ethanol solution of 71 mg of 2,4-dinitrofluorobenzene was added (a clear yellow solution was formed). After five minutes, drop 2cc of 10% NaHCO into the flask 3 solution. React overnight at room temperature. The next morning the pale yellow precipitate formed was filtered, washed with water and ethanol and dried in UHV to afford 80 mg of product (approximate yield 71%).

[0040] The present invention also includes the pharmaceutically acceptable salts of the compounds of the general formula (I) and the possible isomers contained in the general formula (I), which exist in isolated or mixed form.

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Abstract

The invention relates to 2-aminobenzoyl-alkylamines, -alkylamides and - alkylthioamides, and their application for treatment or prevention of various physiological conditions.

Description

technical field [0001] The present invention relates to novel 2-aminobenzoyl derivatives, pharmaceutical preparations containing them, and the use of these compounds in the preparation of medicines for treating or preventing various diseases. Background technique [0002] In general, the present invention relates to novel compounds, their use in therapy, and pharmaceutical formulations containing them. [0003] The amino acid tryptophan is biotransformed via the "kynurenine pathway" (Beadle, G.W., Mitchell, H.K., and Nyc, J.F., Proc. Nat. Acad. SC., 33, 155 (1948); see Charles Heidelberger, Mary E . Gullberg, Agnes Fay Morgan, and Samuel Lepkovsky TRYPTOPHAN METABOLISM. I. CONCERNING THEMECHANISM OF THE MAMMALIAN CONVERSION OFTRYPTOPHAN INTO KYNURENINE, KYNURENIC ACID, ANDNICOTINIC ACID. J. Biol. Chem. (1949) 179: 1). More than 95% of all tryptophan is metabolized to kynurenine (Wolf, H.-Studies on tryptophan metabolism inman. Scand J Clin Lab Invest 136(suppl.): 1-186, 197...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C225/00C07C67/02A61KC07CC07C225/22
CPCC07C225/22A61P13/08A61P13/10A61P15/08A61P15/10A61P15/18A61P17/00A61P23/00A61P25/00A61P25/04A61P25/06A61P25/08A61P25/18A61P25/22A61P25/26A61P25/36A61P27/02A61P27/06A61P29/00A61P35/00A61P3/04A61P37/00A61P43/00A61P5/02A61P7/00A61P7/02A61P9/00A61P9/10A61P9/12A61P3/10C07C225/16A61K31/132A61K31/136
Inventor 纳瓦·奇撒贝尔姆士·劳丹迪佛拉·戴立
Owner NEURIM PHARMA