Nitrogen-containing cyclic compound and pharmaceutical composition containing the compound
Inactive Publication Date: 2004-11-04
EISIA R&D MANAGEMENT CO LTD
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However, the therapy according to a conventional medicine is the complicate procedures as described in (1) to (6), and cautious judgment by a specialist on the basis of enough knowledge and experience has been required.
Further, the therapeutic effects of the drugs used heretofore are not satisfactory and further there is the danger that bleeding is often accompanied by their pharmacological effect.
Accordingly, there is the problem that it is difficult for those except of skilled medical specialists to use these drugs.
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[0156] 3.00 g (17.9mmol) of 2-naphthylacetonitrile was dissolved in 10 ml of dimethyl sulfoxide, and 2.43 g (19.7 mmol) of 2-bromopropane, 330 mg (0.90 mmol, cat) of tetra-n-butylammonium iodide and 10 ml of 50% potassiumhydroxide were successively added thereto. After completion of the reaction, brine was added, and the mixture was extracted with ether. The organic layer was washed with brine, dried over magnesiumsulfate and evaporated, to give a crude product. The crude product was subjected to 150 g of silica gel (ethyl acetate:hexane=1:10), to give 2.42 g (11.6 mnol, 64.6%) of the title compound as a yellow oil.
[0159] 1.00 g (4.78 mmol) of 3-methyl-2-(2-naphthyl)butyronitrile was dissolved in 20 ml of dimethylformamide, 191 mg (4.78 mmol, 60% by weight) of sodiumhydride was added thereto, and the mixture was heated. After 30 minutes, it was cooled to a room temperature, 0.93 ml (4.00 mmol) of (3-bromopropoxy)-tert-butyldimethylsilane was added thereto. After completion of the reaction, brine was added thereto, and the mixture was extracted with ethyl acetate. The organic layer was washed with brine, dried over magnesiumsulfate and evaporated, to give a crude product. The crude product was subjected to 50 g of silica gel (ethyl acetate:hexane=1:18), to give 1.40 g of a mixture of the objective product, a raw material and an impurity. The mixture was used for the following reaction without purification. Namely, 1.40 g of the abve-mentioned crude 4-cyano-5-methyl-5-(2-naphthyl)hexanoxy-tert-butyldi-methylsilane was dissolved in 20 ml of tetrahy...
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Abstract
The present invention provides a novel compound having a superior calciumantagonism, in particular, a neuron-selective calciumantagonism. Namely, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. 1 In the formula, Ar indicates an optionally substituted 5- to 14-membered aromatic ring etc.; the ring A indicates any one ring selected from a piperazine, a homopiperazine, a piperidine and the like; the ring B indicates an optionally substituted C.sub.3-14 hydrocarbon ring etc.; E indicates a single bond, a group represented by the formula --CO--, etc.; X indicates a single bond, an oxygen atom etc.; R.sup.1 indicates a hydrogen atom, a halogen atom, a hydroxyl group etc.; and D.sup.1, D.sup.2, W.sup.1 and W.sup.2 are the same as or different from each other and each represents a single bond or an optionally substituted C.sub.1-6 alkylene chain.
Description
[0001] The present invention relates to a novel compound useful as a calciumantagonist, a salt thereof, a hydrate of them, a production process thereof, and a pharmaceutical composition thereof; and specifically relates to a neuron-selective calcium antagonist, in particular a novel compound having a P / Q-type calcium channel and / or an N-type calcium channel inhibiting activity, etc.PRIOR ART[0002] In Japan, the number of patients with cerebral apoplexy is about 1.4 million or more per year, and the medical expenses therefor are estimated to be about two billion yen. Cerebral apoplexy is the second cause of death next to malignant tumor and is the biggest cause for bedridden man often suffering from severe secondary diseases. A key to the treatment of cerebral apoplexy is to deal with the acute stage, and the treatment at the acute stage influences the life and function prognosis of the patient and significantly influences secondary diseases.[0003] For the purpose of improving blood...
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