PURPOSE: To obtain the medicine containing a (+)-antipode, etc., of a specific aminopyridine derivative as an active ingredient, having triglyceride(TG) or TG-rich lipoprotein-lowering action, low in toxicity and useful for preventing and treating arterial sclerosis.
CONSTITUTION: An aminopyridine compound expressed by formula I (R1 and R2 are H, 1-6C alkyl or protecting group of amino group) (e.g. 2,5- diaminopyridine) is made to react with a compound of the formula R-NCS {R is formula II [R3 is H or 1-6C alkyl; (m) is 1 or 2]} (e.g. optically active- end-2-norbornylisothiocyanate) in a solvent and as necessary, the reactinal product is oxidized with an antioxidant such as peracid to provide an (+)-antipode (salt) of an aminopyridine derivative expressed by formula III [Z is S or NCN; (n) is 0 or 1]. Then, this compound, which is used as an active ingredient, is blended with a carrier, vehicles, a diluent and the blend is prepared to provide the lipid metabolism improver for preventing and treating hyperlipemia, ischemic heart diseases, cerebrovascular diseases, pulpy arteriosclerosis, etc.
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AIDA MASAKI
EBISU HAJIME
NAKAMURA NORIFUMI
