Imidazole derivatives (I), their salts and (R) enantiomers and/or (S) enantiomers are new. Imidazole derivatives of formula (I), their salts and (R) enantiomers and/or (S) enantiomers are new. [Image] R 1, R 2, R 3H, halo, alkyl, alkyloxy, OH, NO 2, NH 2, alkylcarbonylamino, alkylamino or dialkylamino； R 4H, alkyl or alkylaryl； X : CH 2, O or S； n : 1-3； halo : F, Cl, Br or I； alkyl : 1-6C hydrocarbon chains optionally substituted by aryl, alkoxy, halo, alkoxycarbonyl or hydroxycarbonyl； aryl : phenyl or naphthyl optionally substituted by alkyloxy, halo or NO 2； provided that when n is 1, X is not CH 2. Independent claims are also included for: (1) a carbonyl compound of formula (III)； (2) compound (III； n' = 3 and NR 4'R 6= phthalimido) (3) an amine of formula (II)； and (4) preparation of (R) enantiomers and/or (S) enantiomers and salts of (I). [Image] R 1', R 2', R 3'F or H (provided that at least one of R 1', R 2' and R 3' is F)； R 4'H or alkyl； R 5hydroxyl protecting group selected from trialkylsilyl, triphenylsilyl, phenyldialkylsilyl or alkyldiphenylsilyl； R 6amino protecting group selected from an alkyl carbamate or alkylaryl carbamate； and n' : 2. ACTIVITY : Cardiovascular-Gen.； Hypotensive； Cardiant. MECHANISM OF ACTION : Peripheral selective dopamine-beta-hydroxylase inhibitors； Dopamine-beta-hydroxylase inhibitor (claimed). The dopamine-beta-hydroxylase inhibitory activity of compounds (I) was determined in SK-N-SH cells. (R)-5-Aminomethyl-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione hydrochloride (Ia) exhibited a median inhibitory concentration value of 91 nM.
