Toyama Chemical Co., Ltd.

Junichi Mitsuyama

Hiroshi Sakai

Hirokazu Narita

Hiroyuki Imaizumi

Kazuya Hayashi

Minako Yotsuji

Keiko Takakura

Akira Yotsuji

Tetsuya Kajita

Katsumi Shimizu

Kenichi Takashima

Katsuji Ojima

Hiroyo Kawafuchi

Hiroshi Kuroda

Kazuto Kunitani

Naokatu Aoki

Tetsumi Yamakawa

Tokunori Kito

Keisuke Tohdo

Noriyuki Okujo

Kozo Hori

Naokatsu Aoki

To provide novel crystals of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N'-(butoxycarbonyl)benzamidine. Means for Solving the Problems The type II crystal, the type III crystal and the type IV crystal of 4-{3-[4-(3-{4-[amino(butoxycarbonylimino)methyl]phenoxy}propyl)-1-piperidinyl]propoxy}-N&#x2032;-(butoxycarbonyl)benzamidine are useful as excellent drug substances of antifungal agents.

4-{3-[4-(3-{4-[amino (butoxycarbonylimino) methyl] phenoxy} propyl)-1-piperidinyl] propoxy}-N'-(butoxycarbonyl) benzamidine crystals

An arylamidine derivative represented by a general formula described below or a salt thereof has an excellent antifungal action and high safety, and it is useful as an antifungal agent with good pharmacokinetics and pharmacodynamic properties wherein X represents an unsubstituted or substituted lower alkylene or alkenylene group; Grepresents an oxygen atom, a sulfur atom, or an imino group; Grepresents a carbon atom or a nitrogen atom; Rrepresents at least one group selected from the group consisting of a hydrogen atom, a halogen atom, and unsubstituted or substituted alkyl, cycloalkyl and alkoxy groups; Rrepresents an unprotected or protected or unsubstituted or substituted amidino group; and Rrepresents a substituted amino or substituted cyclic amino group, or the like.

Arylamidine derivative or salt thereof

Quinolonecarboxylic acid derivatives or salts thereof

The present invention relates to a compound represented by the general formula (1) or its salt, a process for producing the same, and an antifungal agent comprising the same as an effective component: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group bonded through a carbon atom in the ring to the main chain; R.sup.2 presents a hydrogen atom, a fluorine atom or a substituted or unsubstituted alkyl group; and R.sup.3 represents a cyano group, a thioamido group or a group represented by the formula ##STR2## in which R.sup.4 is a hydroxyl group or a group of the formula ##STR3## (R.sup.7 and R.sup.8, which may be the same or different, are hydrogen atoms or substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, amino, alkoxy, hydroxyl or heterocyclic groups, and may form a substituted or unsubstituted heterocyclic group together with the nitrogen atom to which R.sup.7 and R.sup.8 attach), R.sup.5 is a substituted or unsubstituted alkoxy group or a group of the formula ##STR4## (R.sup.7 and R.sup.8 are as defined above), and R.sup.6 is a hydrogen atom or a substituted or unsubstituted alkyl group.

Triazole derivatives and salts thereof, and antifungal agent containing

Triazole derivatives and salts thereof and antifungal agent containing

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Toyama, Japan

Junichi Mitsuyama