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T-type calcium channel inhibitor

A technology of calcium channel blockers and nitrogen heterocycles, applied in the field of pyridine compounds, can solve problems such as the possibility of T-type calcium channel blockers not mentioned

Inactive Publication Date: 2010-06-16
NISSAN CHEM IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] On the other hand, it has been reported that 1,4-dihydropyridine-5-phosphonate derivatives and pyridine-5-phosphonate derivatives have an effect of enhancing the efficacy of anticancer agents (see, for example, Patent Document 13), and Cardioprotective effects against ischemia-reperfusion disorders (see e.g. Patent Document 14), but there is no mention of their potential as T-type calcium channel blockers

Method used

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  • T-type calcium channel inhibitor
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  • T-type calcium channel inhibitor

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0177] Granules containing the following ingredients were manufactured.

[0178] 10 mg of the compound represented by the ingredient formula (1)

[0179] Lactose 700mg

[0180] Corn starch 274mg

[0181] HPC-L 16mg

[0182] 1000mg

[0183] Pass the compound represented by formula (1) and lactose through a 60 sieve. Pass the cornstarch through a 120-mesh sieve. Mix them with a V-blender. A low-viscosity hydroxypropyl cellulose (HPC-L) aqueous solution was added to the mixed powder, followed by kneading and granulation (extrusion granulation: pore size: 0.5 to 1 mm), followed by drying. The obtained dried granules were sieved through a vibrating sieve (12 / 60 mesh) to obtain granules.

preparation example 2

[0185] A powder for capsule filling containing the following ingredients is manufactured.

[0186] 10 mg of the compound represented by the ingredient formula (1)

[0187] Lactose 79mg

[0188] Corn starch 10mg

[0189] Magnesium Stearate 1mg

[0190] 100mg

[0191] Pass the compound represented by formula (1) and lactose through a 60-mesh sieve. Pass the cornstarch through a 120-mesh sieve. These were mixed with magnesium stearate using a V-blender to obtain a powder for capsule filling. 100 mg of the 10-fold powder is filled into No. 5 hard gelatin capsules to prepare capsules.

preparation example 3

[0193] Granules for capsule filling containing the following ingredients were produced.

[0194] 15 mg of the compound shown in the formula (1)

[0195] Lactose 90mg

[0196] Corn starch 42mg

[0197] HPC-L 3mg

[0198] 150mg

[0199] Pass the compound represented by formula (1) and lactose through a 60-mesh 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 with a vibrating sieve (12 / 60 mesh) to size the granules to obtain granules for capsule filling. 150 mg thereof was filled into No. 4 hard gelatin capsules to prepare capsules.

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Abstract

There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof: wherein Ar 1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO 2 R 2 ; R a and R b are independentlyof each other C 1-6 alkyl group, ANR 8 R 9 , CH 2 OANR 8 R 9 , or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R 1 is C 1-6 alkyl group, ANR 8 R 9 ,AN(CH 2 CH 2 ) 2 NR 8 , AN(CH 2 CH 2 ) 2 O, AOR 8 or benzyl group; R 3 is hydrogen atom, C 1-20 alkyl group, ANR 8 R 9 , a group of formula or or the like.

Description

technical field [0001] The present invention relates to a pyridine compound exhibiting selective T-type calcium channel blocking action, a 1,4-dihydropyridine compound having a substituent at the 1-position, and a therapeutic agent for a disease in which T-type calcium channel blocking action is effective or preventive medicine. Background technique [0002] Many 1,4-dihydropyridine compounds are known to exhibit oral antihypertensive effects and are effective in improving circulatory diseases such as angina pectoris, cerebrovascular disorders, and hypertension (see, for example, Patent Documents 1 to 12). The above-mentioned effects exhibited by the compound are realized mainly based on the vasodilator effect of L-type calcium channel blocking effect. [0003] In recent years, among 1,4-dihydropyridine compounds, compounds having T-type calcium channel blocking activity in addition to L-type calcium channel blocking activity have been discovered (see, for example, Non-Pate...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61P7/10A61P9/00A61P9/04A61P9/10A61P13/12A61P25/04A61P25/08A61P29/00A61P35/00A61P43/00
CPCA61K31/675A61P7/10A61P9/00A61P9/04A61P9/06A61P9/10A61P13/12A61P25/04A61P25/08A61P29/00A61P35/00A61P43/00
Inventor 古川泰司山田修松本浩郎山下彻增田幸则
Owner NISSAN CHEM IND LTD