Sankyo Company, Limited

Takeo Miyaoka

Toshiyuki Konosu

Sadao Oida

Yawara Tajima

Yasushi Takahashi

Teruo Tanaka

Atsushi Somada

Hiroshi Yasuda

Noriko Takeda

Masanao Kaneko

Teruo Hashimoto

Junichi Nakazawa

Triazole antifungal agent

A triazole compound having the formula: ##STR1## wherein Ar.sup.1 represents an optionally substituted phenyl, Ar.sup.2 represents an optionally substituted phenyl, R.sup.0 represents a hydrogen atom or a lower alkyl; R.sup.1 represents a lower alkyl; R.sup.2 to R.sup.5 represent a hydrogen atom or an unsubstituted or halo substituted alkyl, n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; and A represents a 1,3-dioxan-5-yl. The triazole compound of the present invention exhibits an excellent antifungal activity.

Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; is R.sup.1 is alkyl; R.sup.2 is substituted alkyl, substituted cycloalkyl R.sup.2 or optionally substituted heterocyclic; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.

Anti-fungal triazole derivatives, their uses

Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; R.sup.1 is alkyl; R.sup.2 is substituted alkyl or substituted cycloalkyl; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.

Anti-fungal triazole derivatives

A 7-acylamino (or 7-amino)-3-(substituted thiomethyl)cephalosporin derivative or a carboxyl derivative thereof is prepared by heating the corresponding 7-acylamino (or 7-amino)-3-carbamoyloxymethylcephalosporanic acid or a carboxyl derivative thereof with a thiol corresponding to the group which it is desired to introduce at the 3-position under conditions in which the water present is minimized, specifically, either no water is present or the amount of water is limited to less than 5 times the weight of the 7-acylamino (or 7-amino)-3-carbamoyloxymethylcephalosporanic acid or carboxyl derivative thereof. The compounds thus prepared are useful as pharmaceuticals or as intermediates in the production of pharmaceuticals. One of the compounds thus prepared, namely 7.alpha.-methoxy-3-(1-methyl-1H-tetrazol-5-yl)thiomethyl-7.beta.-(O-5-p-ni trobenzoylamino-5-carboxyvaleramido-3-cephem-4-carboxylic acid, is a new compound and it and its salts and esters also form part of the present invention.

Process for preparing cephalosporin derivatives

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Funabashi, Japan

Takeo Miyaoka