4-MERCAPTOBENZOYLGUANIDINE DERIVATIVE

Japanese Patent JP3770947

B2

PROBLEM TO BE SOLVED: To obtain a new compound useful for the treatment and prevention of arrhythmia, angina pectoris and infarction, having antiarrythmic properties and active as an inhibitor of the cellular Na+/H+ antiporter.
SOLUTION: This compound is expressed by formula I (R1 is A, CF3, CH2F or the like; R2 is H, A, a 3-7C cycloalkyl, Ph or the like; A is a 1-6C alkyl; Hal is a halogen), e.g. N-diaminomethylene-2-methyl-4(pyridylthio)-5- methylsulfonylbenzamide. The compound of formula I is obtained by reaction of a compound of formula II (Q is Cl, Br, OA, O-C-OA or the like) with guanidine. The compound of formula I can treat etiological hypoxic disorders and ischemic disorders of all types and is useful as a therapeutic agent e.g. for arterial sclerosis due to cellular proliferation, diabetic complications, tumor, fibrosis, organic hypertrophy. The compound of formula I can also be used for diagnostic tests of disorders related to enhanced activity of Na+/H+ antiporters, e.g. the antiporters in erythrocytes, platelets and leukocytes.

Rolf Gerricke
Manfred Baumgart
Claus-Otto Mink
Norbert Bayer

JP3584896A

April 26, 2006

January 31, 1996

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Merck Patent Gesellschaft mit beschraenkter Haftung

C07C279/22; A61K31/10; C07C323/65; A61K31/155; A61K31/18; A61K31/41; A61K31/425; A61K31/426; A61K31/44; A61K31/505; A61P9/06; A61P9/08; A61P9/10; A61P35/00; A61P43/00; C07C319/20; C07D213/70; C07D239/10; C07D239/38; C07D249/10; C07D249/12; C07D277/16; C07D521/00; (IPC1-7): C07C323/65; A61K31/18; A61K31/18; A61K31/18; A61K31/18; A61K31/18; A61K31/41; A61K31/425; C07C319/20; C07D213/70; C07D239/10; C07D239/38; C07D249/12; C07D277/16; C07D521/00

JP6239828A
JP6228082A
JP6009545A

Kiyoji Kuzuwa

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