4-AMINOBENZOYLGUANIDINE DERIVATIVE

Japanese Patent JP3770946

B2

PROBLEM TO BE SOLVED: To obtain the subject novel compound, useful as an antiarrhythmic agent to treat the disordess of cellular Na+/H+ exchanging mechanisms, a show ing a good heart protective effect, and useful for treatment and prevention of heart infarction and also for treatment of angina pectoris.
SOLUTION: This compound is shown by formula I (A is a 1-6C alkyl; R1 is A, CF3 or the like; and R2 and R3 are each H, a 3-7C cycloalkyl or the like) or its salt, e.g. diaminomethylene-2-ethyl-4-piperidino-5-methylsulfonylbenzamide. It is obtained by, e.g. reacting a compound shown by formula II (Q is Cl, OH or the like) with guanidine, preferably in an organic solvent, or by reacting a compound shown by formula III (R4 is F, I or the like) with a compound shown by the formula R3R2N-D (D is H, a trialkylsilyl or the like). The compound shown by formula II is obtained by nucleophilic substitution of a benzonic acid derivative with the corresponding amine.

Rolf Gerricke
Manfred Baumgart
Norbert Bayer
Claus-Otto Mink

JP3122196A

April 26, 2006

January 26, 1996

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Merck Patent Gesellschaft mit beschraenkter Haftung

C07C317/48; A61K31/155; C07D295/14; A61K31/415; A61K31/425; A61K31/426; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/505; A61P9/00; A61P9/06; A61P9/10; C07C279/22; C07C315/04; C07D213/74; C07D233/88; C07D239/42; C07D277/20; C07D277/42; C07D295/155; (IPC1-7): C07C317/48; A61K31/425; A61K31/44; C07C315/04; C07D213/74; C07D233/88; C07D239/42; C07D277/42; C07D295/14

JP6228082A
JP6009545A

Kiyoji Kuzuwa

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