Acyl guanidine sodium/proton exchange inhibitors and method

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 207/16 (2006.01) A61K 31/155 (2006.01) A61K 31/165 (2006.01) A61K 31/335 (2006.01) A61K 31/34 (2006.01) A61K 31/36 (2006.01) A61K 31/38 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 31/435 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) C07C 279/02 (2006.01) C07C 279/16 (2006.01) C07C 279/18 (2006.01) C07C 279/20 (2006.01) C07C 279/22 (2006.01) C07C 279/24 (2006.01) C07D 203/10 (2006.01) C07D 203/12 (2

Patent

CA 2316352

Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have 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; and 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 acyl guanidines.

L'invention concerne des acyl guanidines qui sont des inhibiteurs d'échange sodium/proton (NHE), présentant la structure (I), dans laquelle n est compris entre 1 et 5; X désigne N ou C-R?5¿ où R?5¿ désigne H, un halo, un alcényle, un alcynyle, un alcoxy, un alkyle ou un hétéroaryle, et R?1¿, R?2¿, R?3¿ et R?4¿ sont tels que spécifiés dans la description et où X est un N, R?1¿ est de préférence un aryle ou un hétéroaryle. Ces composés sont utilisés comme agents antiangineux et cardio-protecteurs. En outre, l'invention concerne un procédé pour la prévention ou le traitement de l'angine de poitrine, de dysfonctions cardiaques, de nécrose myocardique et d'arythmie, procédé utilisant les acyl guanidines précitées.

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