Sankyo Company, Limited

Teruo Tanaka

Yukio Sugimura

Kimio Iino

Toshihiko Hashimoto

Tomoyuki Shibata

Shinichi Sugawara

Tetsuo Miyadera

Yasushi Takahashi

Toshiyuki Konosu

Sadao Oida

Masayuki Iwata

Yawara Tajima

Takeo Miyaoka

Atsushi Somada

Isao Kawamoto

Rokuro Endo

Masao Miyauchi

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 R.sup.a is a group of formula (II): ##STR2## where one of R' is a bond to the remainder of the compound, one more of R' is R.sup.2 and the others of R' are all hydrogen, R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen, optionally substituted alkyl, halogen, hydroxy, alkoxy, amino, alkanoylamino, alkanoyloxy, alkanoyl, carboxy, alkoxycarbonyl, cyano, --S(O).sub.j R.sup.9 where j is 0, 1 or 2 and R.sup.9 is alkyl, or --CONR.sup.6 R.sup.7 which is optionally substituted carbamoyl or heterocyclyl-carbonyl, --NR.sup.3 R.sup.4 is optionally substituted amino or heterocyclic, and --COOR.sup.5 is carboxy, --COO.sup.-, --COOM.sub.x, where M is a cation and x is the reciprocal of the valence of the cation M or protected carboxy and, where --COOR.sup.5 is carboxy, --COOM.sub.x or protected carboxy, the compound of formula (I) also contains an anion; l, m and n are independently 0, 1, 2 or 3, provided that (m+n) is an integer from 2 to 6; p is 0, 1 or 2; Y is a single bond, oxygen, sulfur or ##STR3## wherein R.sup.8 is hydrogen, alkyl or alkanoyl, and pharmaceutically acceptable salts and esters thereof. Such compounds are useful as antibiotics.

2-(heterocyclylthio) carbapenem derivatives, their preparation and their

Compounds of formula (I): ##STR1## in which R.sup.a is a group of formula (II): ##STR2## or a group of formula (III): ##STR3## (where one of R' is a bond to the remainder of the compound, one more of R' is R.sup.2 and the others of R' are all hydrogen), R.sup.1 is hydrogen or methyl, R.sup.2 is hydrogen, optionally substiuted alkyl, halogen, hydroxy, alkoxy, amino, alkanoylamino, alkanoyloxy, alkanoyl, carboxy, alkoxycarbonyl, cyano, --S(O).sub.j R.sup.9 (where j is 0, 1 or 2 and R.sup.9 is alkyl), or --CONR.sup.6 R.sup.7 (which is optionally substituted carbamoyl or heterocyclyl-carbonyl), R.sup.2a is hydrogen, alkyl or alkanoyl, --NR.sup.3 R.sup.4 is optionally substituted amino or heterocyclic, and --COOR.sup.5 is carboxy, --COO.sup.-, --COOM.sub.x (where M is a cation and x is the reciprocal of the valence of the cation M) or protected carboxy and, where --COOR.sup.5 is carboxy, --COOM.sub.x or protected carboxy, the compound of formula (I) also contains an anion; l, m and n are independently 0, 1, 2 or 3, provided that (m+n) is an integer from 2 to 6; p is 0, 1 or 2; Y is a single bond, oxygen, sulfur or R.sup.8 N&lt;(wherein R.sup.8 is hydrogen, alkyl or alkanoyl) and pharmaceutically acceptable salts and esters thereof are potentially valuable antibiotics.

2-(heterocyclylthio)carbapenem derivatives, their preparation and their

Compounds of formula (I): ##STR1## wherein: one or both of R.sup.1 and R.sup.2 are selected from a variety of organic groups;

2-(1-aceti

Compounds of formula (I): ##STR1## (wherein R.sup.1 is carboxy, --CONR.sup.4 R.sup.5, cyano or hydroxymethyl, and R.sup.2 and R.sup.3 are hydrogen, alkyl or substituted alkyl, R.sup.4 and R.sup.5 being hydrogen or a variety of groups) have good antibiotic activity and reduced renal toxicity.

Carbapenem compounds and use

Compounds of formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;

2-penem-3-carboxylic acid derivatives and use

Compounds of formula (I): ##STR1## (wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.3 alpha-hydroxyalkyl group;

Penem derivatives, and composition containing them

Compounds of formula (I): ##STR1## [wherein: R.sup.1 represents a hydrogen atom, an alkyl group, an alkoxy group or various substituted alkyl groups;

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Yokohama, Japan

Teruo Tanaka