Myocardial protection using benzothiazepinones

A - Human Necessities – 61 – K

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A61K 31/55 (2006.01) A61K 31/554 (2006.01) C07D 281/10 (2006.01)

Patent

CA 2198862

Myocardial protection is achieved by administering to a patient an effective amount of a benzothiazepin derivative. The benzothiazepin derivatives have general chemical formula (I), wherein R1 represents hydrogen or methyl, R2 represents hydrogen or acetyl, R3 represents hydrogen or methyl, and R4 represents hydrogen or a halogen, with the proviso that R1 cannot be methyl when R2 = acetyl, R3 = methyl and R4 = hydrogen. The above compounds may also be used in other clinical conditions such as treatment of stable and unstable angina, non-Q-wave myocardial infarction, cerebral trauma ischemia and reperfusion, organ graft preservation, etc.

On obtient une protection du myocarde en administrant à un patient une quantité efficace d'un dérivé de la benzothiazépine. Ce type de dérivés de la benzothiazépine présente la formule chimique générale (I), où R¿1? représente hydrogène ou méthyle, R¿2? représente hydrogène ou acétyle, R¿3? représente hydrogène ou méthyle et R¿4? représente hydrogène ou un halogène, à condition que R¿1? ne puisse représenter méthyle quand R¿2? représente acétyle, R¿3? méthyle et R¿4? hydrogène. Ces composés se prêtent aussi au traitement d'autres états cliniques, tel que l'angor stable et instable, les infarctus du myocarde ne produisant pas d'onde Q, les ischémies et reperfusions suivant un traumatisme cérébral, ainsi qu'à la préservation d'organe greffés, etc.

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