PURPOSE: To provide the novel compound having high stability, capable of being readily used, and useful as an excellent antihypertensive or cardiac disease therapeutic agent.
CONSTITUTION: A compound of formula I [Y it O, group of formula II ((n) is 0-2), etc.; R1-R4 are H, lower alkyl, etc.; Z is CH2, O, etc.; A is imidazolyl, imidazopyridyl, aryl, etc.], e.g. 1-(imidazo[1,2-a]pyridin-6-yl)-N-methyl-2- oxocyclohexylcarbothioamide. The compound of formula I is obtained by reacting a compound of formula III with a compound of the formula: R4-N=C=S in the presence of a base (e.g. potassnim t-butoxide) in a solvent (e.g. THF) at -78°C to the refluxing temperature of the solvent. The compound of formula I activates the potassium ions of smooth muscles to relax the vascular smooth muscles, has a coronary blood flow-increasing action and an antihypertensive action, is effective as a potassium channel-opening action agent, and is therefore useful for preventing and treating angina pectoris, hypertension, etc.
OZAKI FUMIHIRO
ISHIBASHI KEIJI
HASEGAWA KOJI
OINUMA HITOSHI
OGAWA TOSHIAKI
ADACHI HIDEYUKI
KATO KOJI
KODAMA KOTARO
OHARA HIDETO
MORI NOBUYUKI
MINAMI NORIO