Abstract:
PURPOSE: A 2-(2-amido methyl)-2-methyl-2H-benzypyrane compound is provided to ensure selective suppression to 11 beta-HSD 1 enzyme and to prevent and treat clucocorticoid regulatory diseases. CONSTITUTION: A 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is denoted by chemical formula 1. The 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is 3-methoxy-N-methyl-N-[(2-methyl-8-nitro-2H-chromen-2-yl)methyl]benzamide or 3-chloro-N-[(2,6-dimethyl-2H-chromen-2-yl)methyl]-N-methylbenzamide. A pharmaceutical composition contains the 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound and prevents and treats impaired glucose tolerance(IGT), type 1 and 2 diabetes, insulin resistance, dyslipidemia or hypertension.
Abstract:
An external skin composition for skin whitening comprising the extract of Cassia tora or emodin isolated therefrom is provided to inhibit maturation and differentiation of melanin cells by inhibiting activity of c-Kit participating in signal transfer related to promotion of melanin synthesis caused by ultraviolet rays. An external skin composition for skin whitening comprises the extract of Cassia tora which is prepared by extracting Cassia tora with water, C1-C4 alcohol, mixed solvents thereof or chloroform, or emodin extracted from the Cassia tora extract which is obtained by extracting Cassia tora with methanol, fractioning the methanol extract with hexane and chloroform sequentially to obtain a chloroform fraction, and subjecting the chloroform fraction to the column chromatography using mixed solvents containing chloroform and methanol in a volume ratio of 20:1 to 5:1, and is a pharmaceutical composition for preventing and treating hemochromatosis or a cosmetic composition for skin whitening.
Abstract:
The present invention relates to 4,5-dihydroisoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 and D4 receptors represented by the following Formula (1), and its preparation method through reductive amination reaction in the presence of reducing agent,wherein R1, R2, X and n are the same as defined in the specification.
Abstract:
PURPOSE: Title derivatives are prepared which has a good therapeutic activity of dys-mnesia and senile athymia. CONSTITUTION: Title compounds (formula 1; R is -H, -CH3, -CH2CH3, -CH2(CH2)3CH3, -CH2CH=CH2, etc.) and their pharmaceutical salt are prepared. Thus, 1.24 g of hydroxylamine hydrochloride is dissolved in water, and controlled to pH 7 by NaHCO3 saturated aqueous solution. The solution is refluxed for 2 hours in a mixed solution of 5-acetylpyrimidine and 50 ml of benzene using Dean-Stark column. Obtained solution is concentrated under reduced pressure to give 1.28 g of 1-pyrimidin-5-yl-(E)-ethanone oxime(yield 78 %).
식 중, R 1 은 탄소 원자수 1 내지 4의 저급 알킬기, 할로겐으로 치환된 탄소 원자수 1 내지 4의 저급 알킬기 또는 할로겐으로 치환된 페닐기이고, X는 N, CH 또는 CY이고, Y는 할로겐 또는 탄소 원자수 1 내지 4의 저급 알콕시이거나, 또는 R 1 및 X는 함께 -COCH 2 CH(CH 3 )-를 형성하고, R 5 는 H 또는 아미노기이고, R 2 및 R 3 은 각각 H, 탄소 원자수 1 내지 4의 저급 알킬기, 또는 할로겐으로 치환된 저급 알킬기이고, n은 0 또는 1이다.