Sankyo Company, Limited

Sadao Oida

Toshiyuki Konosu

Yawara Tajima

Takeo Miyaoka

Noriko Takeda

Hiroshi Yasuda

Yasushi Takahashi

Makoto Mori

Teruo Tanaka

Takuya Uchida

Atsushi Somada

Akira Yoshida

Satoshi Ohya

Akihiko Nakagawa

Kazuo Sato

Shinichi Sugawara

Hideo Takeshiba

Hisaki Kajino

Junzo Tobitsuka

Yukiyoshi Takahi

Hiroshi Ohta

Eiji Ohki

Hiroyuki Itoh

Teruo Hayashi

Triazole derivatives having antifungal activity

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## (wherein R.sup.1 represents hydrogen or a hydroxy-protecting group, R.sup.2 and R.sup.3 represent hydrogen, alkyl or aryl; R.sup.4 represents optionally substituted alkyl, alicyclic heterocyclic, aryl, aromatic heterocyclic, optionally substituted alkenyl or optionally substituted alkynyl; R.sup.5 represents hydrogen or a carboxy-protecting group; and R.sup.6 represents alkoxy, aryloxy, dialkylamino or diarylamino or two or R.sup.6 together represent o-phenylenedioxy or three together represent CH.sup.3 C(--CH.sub.2 O--).sub.3) may be prepared by reacting the corresponding carbonyl compound with a compound of formula P(R.sup.6).sub.3. Compounds (I) may be cyclised to prepare carbopenem derivatives, many of which have valuable antibiotic activity.

Azetidinone derivatives, a process for their preparation and their use

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

Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen or alkyl, or together are cycloalkyl; R.sup.3 and R.sup.4 are hydrogen, alkyl or phenyl, or together are cycloalkyl; or R.sup.1 and R.sup.3 together are cycloalkyl fused to the oxetane ring; Ar is phenyl substituted by R.sup.5, R.sup.6 and R.sup.7, where R.sup.5, R.sup.6 and R.sup.7 are hydrogen, halogen, alkyl, alkoxy, halogenated alkyl or halogenated alkoxy; and R.sup.8 and R.sup.9 are hydrogen or alkyl] and salts thereof have valuable agricultural and pharmaceutical anti-fungal or fungicidal activity. They may be prepared by a variety of processes.

Oxetane derivatives and their use as anti-fungal or fungicidal agents

Penem-3-carboxylic acid derivatives of formula (I): ##STR1## (wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyalkyl group, an acyloxyalkyl group, an alkylsulphonyloxyalkyl group, an arylsulphonyloxyalkyl group or a trialkylsilyloxyalkyl group;

Penem-3-carboxylic acid derivatives

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Yokohama, Japan

Sadao Oida