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Preparation method of medicine for curing urteriosclerosis by using CS-866, losartan and candisartan

A 1.CS-866, arteriosclerosis technology, applied in the direction of drug combination, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve the limitations of treatment, can not reduce serum lipids, can not completely Explain the prevention and treatment of arteriosclerosis and other issues

Inactive Publication Date: 2005-10-05
SANKYO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, renin-angiotensin inhibitors cannot reduce serum lipids [J. Cardiovasc. Pharmacol., 15, S65-S72 (1990)], and single-dose administration has limitations for treatment
[0006] In addition, even if troglitazone, glibenclamide and captopril are given to diabetic patients at the same time, it cannot be fully explained that it is related to the prevention and treatment of arteriosclerosis [J. Clinical Therapeutic & Medicines, 9 (Supp. 3), 39- 60(1993)]

Method used

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  • Preparation method of medicine for curing urteriosclerosis by using CS-866, losartan and candisartan
  • Preparation method of medicine for curing urteriosclerosis by using CS-866, losartan and candisartan
  • Preparation method of medicine for curing urteriosclerosis by using CS-866, losartan and candisartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Suppresses the deterioration of arteriosclerosis

[0093] Using 2-3 months old WHHL rabbits [Watanabe hereditary hyperlipidemia rabbits: the above (Biochimica et Biophysica Acta) etc.] as a group of 4 to 7, a certain amount of drug was orally administered for 32 weeks. In addition, the food intake of each animal is limited to 120g / day. Take blood immediately before taking the medicine and at 4, 8, 12, 16, 20, 24, 28 and 32 weeks after the start of taking the medicine, and measure the total cholesterol value (mg / dl). There was no change in ratio. In addition, the test animals were dissected at 32 weeks, and the lesion area rate (%) of the aorta and the yellowing incidence rate (%) of the knuckles were investigated. The results are shown in Table 1 and Table 2.

[0094] [Table 1]

[0095] Experiment number

test compound

Dosage

(mg / kg)

animal

number

Lesion area rate (%)

bow

Chest

the ...

Embodiment 2

[0099] Suppresses the deterioration of arteriosclerosis

[0100] Using 2-3 months old WHHL rabbits [Watanabe hereditary hyperlipidemia rabbits: the above (Biochimica et Biophysica Acta) etc.] as a group of 5 to 7, a certain amount of the drug was orally administered for 31 weeks. In addition, the food intake of each animal is limited to 100g / day. Blood was taken immediately before taking the medicine and at 8, 16, 24, and 31 weeks after the start of taking the medicine, and the total cholesterol value (mg / dl) was measured. It was considered that there was no change in any taking group compared with the non-taking control group. In addition, the test animals were dissected at 31 weeks, and the lesion area rate (%) of the aorta and the yellowing incidence rate (%) of the knuckles were investigated. The results are shown in Table 3 and Table 4.

[0101] [table 3]

[0102] Experiment number Test compound

Dosage

(mg / kg)

animal

number

Lesion area ...

preparation example 1

[0106] tablet

[0107] CS-866 4.0mg

[0108] Troglitazone 100.0

[0109] Lactose 244.0

[0110] Corn starch 50.0

[0111] Magnesium stearate 2.0

[0112] 400mg

[0113] The above-mentioned powders were mixed, and tableted with a tablet machine to make tablets of 400 mg each.

[0114] The tablets may be coated with sugar if necessary.

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PUM

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Abstract

Compound CS-866, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-Ä2'-(1H-tetrazol-5-yl)biphenyl- 4-ylmethylÜimidazole-5-carboxylate, is useful in the preparation of a medicament for use in the prophylaxis or treatment of arteriosclerosis.

Description

[0001] This application is a divisional application based on application number 97197939.1 and application date 1997 / 7 / 11 (the pharmaceutical composition for preventing and treating arteriosclerosis is its invention title) [Field of invention] [0002] The present invention relates to: a pharmaceutical composition containing one or more drugs selected from angiotensin II receptor antagonists and angiotensin-converting enzyme inhibitors, together with insulin resistance improving agents One or two or more drugs selected as active ingredients (compositions especially for preventing or treating arteriosclerosis); in the manufacture of pharmaceutical compositions (compositions especially for preventing or treating arteriosclerosis) from angiotensin The application of one or more drugs selected from II receptor antagonists and angiotensin-converting enzyme inhibitors and one or more drugs selected from insulin resistance improvers, or the application of drugs from angiotensin II On...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/41A61K31/33A61K31/39A61K31/4178A61K31/425A61K31/427A61K31/44A61K31/55A61K45/06A61P9/10A61P43/00
CPCA61K31/427A61K31/425Y10S514/824A61K31/4178A61K45/06A61K31/55A61K31/44A61P3/10A61P43/00A61P9/00A61P9/10A61K31/415A61K2300/00
Inventor 辻田代史雄藤原俊彦佐田登志夫前田尚之
Owner SANKYO CO LTD