Thromboxane synthetase inhibiting 3-(1-alkenyl) pyridines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Silicon containing doai

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514277, 514332, 514333, 514336, 514338, 514340, 514341, 514357, 514358, 546256, 546263, 546270, 546276, 546278, 546284, 546330, 546331, 546333, 546340, 546342, 546343, 546346, 546350, 546 14, C07D21389, C07D21359, C07D21324, A61K 3144

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045634467

ABSTRACT:
Novel compounds of the formula: ##STR1## wherein R.sup.2 is an aromatic or heterocyclic group, which may optionally be substituted, R.sup.2 is a methyl group, a hydroxymethyl group, a nitroxymethyl group, a formyl group, a nitrogen-containing five-membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryloxymethyl group, a cyano group, a carbamoyl group which may optionally be substituted, a carbamoyloxymethyl group which may optionally be substituted, a thiocarbamoyloxymethyl group which may optionally be substituted, and an alkoxycarbonyl group, n is an integer of 1 to 20, and ##STR2## provided that n is an integer of 9 to 20 when ##STR3## and, at the same time, R.sup.2 is a carboxyl group or an alkoxycarbonyl group, or a pharmacologically acceptable salt thereof, have a selective inhibitory action on biosynthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of enhancing the production of prostaglandin I.sub.2 (PGI.sub.2), and can be used for mammals to prevent and treat arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardiac infarction, stroke, occlusion of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).

REFERENCES:
Chemical Abstracts 100:174676y, (1984).
Chemical Abstracts 95:180667r, (1981).
J. Med. Chem. 24 1139--Iizuka--Highly Selective Inhibitors of Thromboxane Synthetase. 1. Imidazole Derivatives.
J. Med. Chem. 24 1149--Tanouchi--Highly Selective Inhibitors of Thromboxane Synthetase. 2. Pyridine Derivatives.

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