Anti-hypertension compound, and preparation, pharmaceutical composition and use thereof

A kind of compound and mixture technology, applied in the field of antihypertensive compound and preparation thereof

A kind of compound and mixture technology, applied in the field of antihypertensive compound and preparation thereof

CN101475565AInactive Publication Date: 2009-07-08王建民
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  • Anti-hypertension compound, and preparation, pharmaceutical composition and use thereof
  • Anti-hypertension compound, and preparation, pharmaceutical composition and use thereof
  • Anti-hypertension compound, and preparation, pharmaceutical composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0247] 105) 2-aminopropionic acid (S)-1-[2′-(1H-tetrazol-5-yl)-1′,1-biphenyl-4-yl]methyl-2-n-butyl-4 -Climidazol-5-ylmethyl ester

[0248] At room temperature, 1-[2'-(1H-tetrazol-5-yl)-1',1-biphenyl-4-yl]methyl-2-n-butyl-4-chloroimidazol-5- Dimethylmethanol (422mg, 1.0mmol) was dissolved in anhydrous dimethylformamide (8mL), the solution was placed in an ice bath at 0°C, and N-tert-butoxycarbonyl-L-alanine (378mg , 2.0mmol), 1-(3-dimethylamino)propyl-3-ethylcarbodiimide hydrochloride (383mg, 2.0mmol), N-hydroxybenzotriazole (270mg, 2.0mmol) and N - Methylmorpholine (202 mg, 2.0 mmol). The reaction mixture was stirred at 0°C for 30 minutes and at room temperature for 24 hours. The above reaction mixture was diluted with water (150 mL), and extracted with ethyl acetate (200 mL). The organic extract was washed successively with aqueous citric acid (10%), water and saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated to obtain a crude produc...

Embodiment 2

[0251] 103) 2-Amino-4-methylpentanoic acid (S)-1-[2′-(1H-tetrazol-5-yl)-1′, 1-biphenyl-4-yl]methyl-2- n-Butyl-4-chloroimidazol-5-ylmethyl ester

[0252] Prepared as described in Example 1 except that N-tert-butoxycarbonyl-L-leucine was used in place of N-tert-butoxycarbonyl-L-alanine. The resulting compound is C 28 h 34 ClN 7 o 2 , the calculated value of MS-ESI (m / z) is 535.2; the measured value is 534.1 (100, MH - ).

Embodiment 3

[0254] 101) 2-Aminoacetic acid (S)-1-[2′-(1H-tetrazol-5-yl)-1′, 1-biphenyl-4-yl]methyl-2-n-butyl-4- Clomidazol-5-ylmethyl ester

[0255] Prepared as described in Example 1 except that N-tert-butoxycarbonyl-L-glycine was used in place of N-tert-butoxycarbonyl-L-alanine. The resulting compound is C 24 h 26 ClN 7 o 2 , the calculated value of MS-ESI (m / z) is 479.2; the measured value is 478.7 (100, MH - ).

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Abstract

The invention provides antihypertensive compounds, methods for preparing the same, the pharmaceutical compositions of the same and the uses of the same. The antihypertensive compounds are compounds of a general formula (I) or pharmaceutically acceptable salts, solvates, polycrystals, antipodes or a racemic mixture of the same, wherein R1, R2, R3, and R4 are H, substituted alkyls, substituted cyclohexyls, substituted alkylthios, substituted alkoxyls, substituted aryls, substituted aralkyls independently, or R1 and R2 form substituted cyclohexyls together, or R2 and R3 form substituted heterocyclyls. The compounds are absorbed by gastrointestinal tracts through the active transportation of a PepT1 transporter, and decomposed by enzymes in intestinal tracts and the liver to form iosartan slowly, so the iosartan is kept in the blood for a longer time and stable blood concentration contributes to the improvement of curative effects and reduction of side reactions.

Description

technical field [0001] The invention relates to a class of antihypertensive compounds and a preparation method thereof, as well as pharmaceutical compositions containing the antihypertensive compounds and the use of the antihypertensive compounds in preparing antihypertensive drugs. Background technique [0002] Hypertension is a common disease, frequently-occurring disease, and one of the most important risk factors for cardiovascular and cerebrovascular diseases. The main complications of hypertension—stroke, heart disease, and kidney disease—seriously endanger human health, with a high rate of death and disability, and a heavy burden on individuals, families, and society. Due to social and economic development and changes in people's lifestyles, the prevalence of hypertension among Chinese residents has continued to increase. The results of the 2002 National Survey on Nutrition and Health Status of Residents showed that the prevalence of hypertension among adults in my co...

Claims

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Application Information

Patent Timeline
08 Jul 2009
Publication
CN101475565A
IPC
C07D403/10; C07D403/14; A61K31/4178; A61K31/454; A61K31/55; A61P9/12; A61P9/00; A61P25/06
CPC
C07D403/10; A61K31/4164; C07D233/90; A61P9/00; A61P9/10; A61P9/12; A61P25/06
Inventors
王建民