Kaken Pharmaceutical Company, Ltd.

Tadashi Arika

Mamoru Yokoo

Kouji Amemiya

Kazuya Sasaki

Tetsuya Maeda

Toshiyuki Yamamoto

Mituo Takase

Sakae Koshikawa

Rieko Hashimoto

Takanobu Naito

Tokiko Nishida

Hironobu Ogura

Haruhito Kobayashi

Kiyoshi Nagai

Satoko Shusse

Jun Nakano

Hisato Senda

Hideto Fukui

Yoshiyuki Tatsumi

Katuyuki Ohtuka

Kosho Nakamura

Hisamitsu Haigoh

Wakao Iwatani

Yayoi Watanuki

Tetsuro Maejima

Tetsuo Shibata

A novel method for evaluating an effect of an antimicrobial agent which comprises removing the antimicrobial agent remaining in a biological sample or the like to thereby accurately evaluate the effect of the antimicrobial agent without being affected by the remaining antimicrobial agent. A therapeutic agent for onychomycosis which can be obtained according to the evaluation method of the drug effect.

Method for treating onychomycosis

There is disclosed a fungicide containing, as an effective ingredient, a compound having the general formula (I): ##STR1## or an acid addition salt thereof, particularly the compound wherein an absolute configuration of the asymmetric carbon atoms is R,R-configuration or an acid addition salt thereof.

Azolylamine derivative

Quinolinecarboxylic acid derivatives and salts thereof

There is disclosed a fungicide containing, effective ingredient, a compound having the general formula (I): ##STR1## or an acid addition salt thereof, particularly the compound wherein an absolute configuration of the asymmetric carbon atoms is R,R-configuration or an acid addition salt thereof.

Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y. The amine derivatives (I) are useful as fungicides.

Amine derivatives, processes for preparing the same and fungicides

An oxime derivative of the formula: ##STR1## wherein R is a hydrogen atom or a C.sub.1-5 alkyl group, R.sub.1 is a hydrogen atom, a C.sub.1-5 alkyl group or a carboxyl-protecting group, R.sub.2 is a hydrogen atom, a halogen atom, a hydroxyl group or an amino group, R.sub.3 is a C.sub.3-7 cycloalkyl group, R.sub.4 is a hydrogen atom, a halogen atom or a C.sub.1-4 alkoxy group, each of R.sub.5 and R.sub.6 which may be the same or different, is a hydrogen atom or a C.sub.1-5 alkyl group, or R.sub.5 and R.sub.6 together represent a C.sub.2-4 alkylene group which forms together with the adjacent carbon atom a C.sub.3-5 ring, provided that when R.sub.2 is a hydrogen atom, R.sub.4 is a C.sub.1-4 alkoxy group, m is an integer of 0 or 1, and n is an integer of from 1 to 3; or its pharmaceutically acceptable salt.

Oxime derivatives

Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y. The main derivatives (I) are useful as fungicides.

A synergistically active antifungal composition comprising an azole compound and an arylmethylamine compound.

Antifungal composition

Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## Y is selected from the group consisting of ##STR3## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y. The amine derivatives (I) are useful as fungicides.

Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y. The amine derivatives (I) are useful as fungicides.

Amine derivatives and fungicides containing the same

An antifungal and antibacterial imidazole derivative represented by the general formula I or a biologically acceptable acid addition salt thereof: ##STR1## where Ar is a phenyl group which may be substituted by alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 4 carbon atoms, alkylamino having from 1 to 4 carbon atoms, alkoxy carbonyl having from 1 to 4 carbon atoms, phenyl, halogen or hydroxyl; a naphthyl group; a furyl group; or a thienyl group which may be substituted by halogen or alkyl having from 1 to 4 carbon atoms, and R is an alkyl group having from 1 to 10 carbon atoms; an alkenyl group having from 1 to 6 carbon atoms; or a phenylalkyl group which may be substituted by halogen.

Growing community of inventors

Kasukabe, Japan

Tadashi Arika