Heterocyclic sodium/proton exchange inhibitors and method

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 405/08 (2006.01) A61K 31/506 (2006.01) A61P 9/00 (2006.01) C07D 233/54 (2006.01) C07D 233/88 (2006.01) C07D 239/48 (2006.01) C07D 277/20 (2006.01) C07D 277/40 (2006.01) C07D 401/04 (2006.01) C07D 401/14 (2006.01) C07D 403/04 (2006.01) C07D 403/06 (2006.01) C07D 403/08 (2006.01) C07D 405/14 (2006.01) C07D 409/04 (2006.01) C07D 409/14 (2006.01) C07D 413/08 (2006.01) C07D 417/04 (2006.01) C07D 417/08 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2388813

Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure (I) wherein n is 1 to 5; X is N or C-R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl group, R1, R2, R3 and R4 are as defined herein, and where X is N, R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.

La présente invention concerne des hétérocycles inhibiteurs de l'échange sodium/protons représentés par la formule générale (I) et convenant particulièrement comme antiangoreux et comme cardioprotecteur. Dans cette formule, n vaut 1 à 5; X est N ou C-R?5¿ auquel cas R?5¿ est H, halo, alcényle, alkynyle, alcoxy, alkyle, aryle ou hétéroaryle; Z est un groupe hétéroaryle, R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que définis dans les revendications, et en outre, lorsque X est N, R?1¿ est de préférence aryle ou hétéroaryle. L'invention concerne également une procédure utilisant les dérivés hétérocycliques de l'invention pour la prévention et le traitement de l'angine de poitrine, de la dysfonction cardiaque, de la nécrose myocardique et de l'arythmie.

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