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T-type calcium channel blockers

A technology of calcium channel blockers and solvates, applied in the field of T-type calcium channel blockers, can solve problems such as decreased quality of life

Inactive Publication Date: 2006-04-26
NISSAN CHEM IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] However, dihydropyridine-5-phosphonate derivatives represented by efodipine (racemate) may become a strong vasodilator based on L-type calcium channel blockade in addition to the treatment of the above-mentioned diseases. The effect and the influence on the heart function are hindering factors, and sometimes it may lead to the decrease of the quality of life (Quality of life) such as headache, fever, dizziness, and edema based on the vasodilation effect

Method used

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  • T-type calcium channel blockers
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  • T-type calcium channel blockers

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0168] Manufacture of granules containing the following ingredients

[0169] The compound shown in component formula (1)

[0170] Pass the compound represented by formula (1) and lactose through a 60-mesh sieve. Pass the cornstarch through a 120-mesh sieve. Mix them with a V-blender. Add low-viscosity hydroxypropyl cellulose (HPC-L) aqueous solution to the mixed powder, knead and granulate (extrusion granulation, pore size 0.5-1 mm), and then dry. The obtained dried granules were sieved through a vibrating sieve (12 / 60 mesh) to obtain granules.

preparation example 2

[0172] The compound shown in component formula (1)

[0173] Pass the compound represented by formula (1) and lactose through a 60-mesh sieve. Pass the cornstarch through a 120-mesh sieve. Blend them with magnesium stearate using a V-blender. Fill 10 times powder 100mg into No. 5 hard gelatin capsules.

preparation example 3

[0175] The compound shown in component formula (1)

[0176] Pass the compound represented by formula (1) and lactose through a 60 sieve. Pass the cornstarch through a 120-mesh sieve. Blend them using a V-blender. A low-viscosity hydroxypropyl cellulose (HPC-L) aqueous solution was added to the mixed powder, kneaded, granulated, and then dried. The obtained dried granules were sieved through a vibrating sieve (12 / 60 mesh) to size the granules, and 150 mg thereof were filled into No. 4 hard gelatin capsules.

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PUM

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Abstract

The invention provides a T-type calcium channel blocker. Specifically, a T-type calcium channel blocker as an optically active 1,4-dihydropyridine compound represented by the following formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof is provided, [wherein, R1 and R2 independently represent a C1-6 alkyl group, or R1 and R2 are combined to represent -CR5R6-CR7R8-, -CR5R6-CR7R8-CR9R10- or -CR5R6-CR7R8-CR9R10-CR11R12-, etc., X1 or X2 are independently Represents O or NR13, Ar represents phenyl that can be substituted, etc., Ra and Rb independently represent C1-6 alkyl, -L2-NR16R17, -CH2O-L2-NR16R17, CN, -L2-N(CH2CH2)2NR16 Or NR16R17, Y represents C1-20 alkyl, -L3-NR18R19 and the above chemical formula (2), represents the absolute configuration].

Description

technical field [0001] The present invention relates to a T-type calcium channel blocker, which is an optically active dihydropyridine-5-phosphonate derivative whose absolute configuration at the 4-position of the dihydropyridine ring is R configuration, and also relates to T-type calcium Therapeutic or preventive agents for diseases for which channel blockers are effective. Background technique [0002] It is known that dihydropyridine-5-phosphonate derivatives (racemate) exhibit oral antihypertensive effects, and are effective in the improvement of circulatory system diseases such as angina pectoris, cerebrovascular disorders, and hypertension (see For example, Patent Documents 1 to 7). [0003] The above-mentioned effect is mainly produced by the vasodilation action based on L-type calcium channel blocking action, and this effect is the same as that of many other L-type calcium antagonists typified by 1,4-dihydropyridine derivatives. [0004] In recent years, it has bee...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/714A61P7/10A61P9/04A61P9/06A61P9/10A61P13/12A61P25/10
Inventor 增田幸则古川泰司
Owner NISSAN CHEM IND LTD