Takeda Chemical Industries, Inc.

Takuichi Miki

Hirotomo Masuya

Giichi Goto

Kentaro Hiraga

Taisuke Matsuo

Tohru Sugawara

Tsunehiko Asako

Takenobu Soma

Tadatsugu Harukawa

Novel cephem compounds having a group of the formula at the 3-position thereof: ##STR1## wherein X represents oxygen, sulfur or imino, which may be substituted; and B represents hydrogen or a hydroxyl, amino, mercapto or hydrocarbon group, which groups may be substituted, can be prepared by reacting a 3-formylcephem compound with a hydrazine compound of the formula: ##STR2## wherein the symbols have the same meanings as above, and subjecting the thus obtained compound to an oxidative ring-closure reaction. The objective compounds are found to have a broad antimicrobial spectrum and, in particular, are effective against gram-negative bacteria including Escherichia Coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus mirabilis, Proteus rettgerii, as well as gram positive ones, and have low-toxity. Thus, these compounds may be used for antimicrobial agents in therapeutical purpose.

3-Heterocyclic substituted cephem compounds

Novel estradiol derivatives of the formula ##STR1## wherein R.sup.1 means an alkyl group of two or more carbon atoms, and R.sup.2 is hydrogen or an acyl group, have antiestrogen activity and are useful as antiestrogen drugs.

Estradiol derivatives

There is disclosed a process for preparing 17.alpha.-hydroxy corticoid 21-phosphate which comprises reacting a compound selected from the group consisting of 17.alpha.,21-dihydroxy corticoid and 11, 17.alpha.,21-trihydroxy corticoid with pyrophosphoryl tetrachloride, subjecting the reaction mixture to a hydrolyzing agent and recovering the objective 17.alpha.-hydroxy corticoid 21-phosphate or 11, 17.alpha.-dihydroxy corticoid 21-phosphate from the hydrolysis reaction medium.

Production of 21-phosphate corticords having unprotected hydroxyl

6-(1'-CYCLOHEXENYLGLYCINAMIDO)PENICILLANIC ACID AND SALTS THEREOF, WHICH HAVE BOTH A BROAD SPECTRUM ANTIBACTERIAL ACTION AND STRONG ACTIVITY AGAINST Escherichia coli.

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Amagasaki, Japan

Takuichi Miki