Novel arylamidine derivative, salt thereof, and antifungal...

Details Novel arylamidine derivative, salt thereof, and antifungal... Novel arylamidine derivative, salt thereof, and antifungal...

C - Chemistry, Metallurgy

07

D

C07D 211/22 (2006.01) A61K 31/445 (2006.01) A61P 31/10 (2006.01)

Patent

CA 2572161

An arylamidine derivative represented by the general formula (wherein R1 represents optionally protected or substituted amidino; and R2 and R3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.

Dérivé d~arylamidine représenté par la formule générale (dans laquelle R1 représente un groupe amidine éventuellement protégé ou substitué ; et R2 et R3 sont identiques ou différents et représentent chacun un atome d~hydrogène ou d~halogène) ou sel du dérivé. Le dérivé et le sel ont une activité puissante contre les champignons y compris ceux ayant une tolérance aux médicaments du type azole et ont en outre une innocuité élevée et d~excellentes propriétés dans un test de toxicité avec des doses répétées. Ils sont donc utiles en tant qu~excellents antifongiques.

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