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Title:
THIOFORMAMIDE DERIVATIVE
Document Type and Number:
Japanese Patent JPH0625154
Kind Code:
A
Abstract:

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.


Inventors:
KABASAWA YASUHIRO
OZAKI FUMIHIRO
ISHIBASHI KEIJI
HASEGAWA KOJI
OINUMA HITOSHI
OGAWA TOSHIAKI
ADACHI HIDEYUKI
KATO KOJI
KODAMA KOTARO
OHARA HIDETO
MORI NOBUYUKI
MINAMI NORIO
Application Number:
JP26594892A
Publication Date:
February 01, 1994
Filing Date:
October 05, 1992
Export Citation:
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Assignee:
EISAI CO LTD
International Classes:
A61K31/385; A61K31/41; A61K31/415; A61K31/4166; A61K31/42; A61K31/425; A61K31/44; A61K31/4433; A61K31/495; A61K31/50; A61K31/505; A61P9/08; A61P9/10; A61P9/12; A61P11/00; C07C327/46; A61K31/38; C07D233/60; C07D233/64; C07D233/72; C07D409/04; C07D471/04; (IPC1-7): C07C327/46; A61K31/38; A61K31/385; A61K31/41; A61K31/415; A61K31/42; A61K31/425; A61K31/44; A61K31/495; A61K31/50; A61K31/505; C07D233/60; C07D233/64; C07D233/72; C07D409/04; C07D471/04
Attorney, Agent or Firm:
Kaoru Furuya (3 outside)