AZOLYLAMINE DERIVATIVE

Japanese Patent JP3437695

B

PROBLEM TO BE SOLVED: To obtain the subject new compound which is a specific azolylamine derivative containing an azolyl group and an amine ring in the molecule, has strongly antimicrobial activity, low toxicity and is effective for preventing and treating human and animal fungal diseases.
SOLUTION: This azolylamine derivative is shown by formula I [Ar is a (substituted) phenyl; R1 and R2 are each H, a lower alkyl, a (substituted) aryl, an alkenyl, an alkynyl or an aralkyl; (m) is 2 or 3; (n) is 1 or 2; X is N or CN; * is an asymmetric carbon atom]. The azolylamine derivative has strongly antifungal activity, low toxicity and is effective for preventing and treating human and animal fungal diseases. The compound is obtained by reacting an azolyl group-containing epoxy compound of formula II {e.g. (2R,3S)-2-(2,4- difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methylloxirane, etc.} with a cyclic amine of formula III (e.g. 4-methylpiperidine, etc.).

Naito, Takanobu
Kobayashi, Haruhito
Ogura, Hironobu
Nagai, Motomi
Nishida, Tokiko
Ariyoshi, Tadashi
Yokoo, Mamoru
Izuse, Satoko

JP1995000341201

June 06, 2003

December 27, 1995

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KAKEN PHARMACEUT CO LTD

C07D401/06; A01N43/50; A01N43/653; A61K31/41; A61K31/415; A61K31/4196; A61K31/4427; A61K31/445; A61K31/454; A61K31/55; A61P31/04; A61P31/10; C07D403/06; C07D401/00; A01N43/48; A01N43/64; A61K31/41; A61K31/415; A61K31/4196; A61K31/4427; A61K31/445; A61K31/4523; A61K31/55; A61P31/00; C07D403/00; (IPC1-7): C07D401/06; A01N43/50; A01N43/653; A61K31/4196; A61K31/454; A61P31/04; C07D403/06

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