Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Wakunaga Pharmaceutical Co., Ltd.

Shinya Okuda

Kohji Kawabata

Kazuo Sakane

Yoshiki Yoshida

Hisashi Takasugi

Jiro Goto

Hideaki Yamanaka

Satoshi Inoue

Hidenori Ohki

Toshio Yamanaka

Kenji Itoh

Takeshi Terasawa

Keiji Misumi

Yoshiteru Eikyu

Hirofumi Yamamoto

Ayako Toda

Kenji Satoh

Keiji Matsuda

Kenji Murano

Hiroshi Sasaki

Masaru Oogaki

Masaru Ohgaki

Kenji Sato

Hitomi Ogino, Legal Representative

Tetsuya Ogino, Legal Representative

Tomomi Takezawa, Legal Representative

Hisashi Akamatsu

The present invention relates to a compound of the formula [I]:  

Cephem compounds

The present invention relates to a compound of the formula [I]: wherein A is lower alkylene or lower alkenylene; Ris lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl or protected amino(lower)alkyl, and Ris hydrogen or amino protecting group, or Rand Rare bonded together and form lower alkylene; Rand Rare independently amino or protected amino; and Ris carboxy or protected carboxy, or a pharmaceutically acceptable salt thereof, a process for preparing a compound of the formula [I], and a pharmaceutical composition comprising a compound of the formula [I] in admixture with a pharmaceutically acceptable carrier.

The present invention relates to a compound of the formula [I]: wherein 

A compound of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,

Cephem compounds and pharmaceutical use thereof

Compounds of the formula: ##STR1## wherein R is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl or R.sup.3 and R.sup.4 are linked together to form C.sub.3 -C.sub.6 alkylene, A is lower alkylene, and R.sup.5 is hydroxy or a protected hydroxy group; or a group of the formula: ##STR3## in which R.sup.6 is lower alkyl, R.sup.7 and R.sup.8 are each hydroxy or a protected hydroxy group, and Y is N or CH, and salts thereof are intermediates for cephem compounds which show antimicrobial activities and which are useful in the treatment of microbial infections.

Intermediates for cephem compounds

Cephem compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,

Cephem compounds having the following formula are disclosed: ##STR1## R.sup.1 =amino or protected amino R.sup.2 =an organic group ##STR2## R.sup.6 =lower alkyl R.sup.7, R.sup.8 .dbd.OH or protected OH

The invention relates to a highly stable antibacterial agent which is crystalline 7.beta.-[2-(5 -amino-1,2,4-thiadiazol-3-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]- 3-[3-amino-2-(2-hydroxyethyl)-1-pyrazolio]methyl-3-cephem-4-carboxylate hydrochloride (syn-isomer).

Cephem compound

Growing community of inventors

Osaka, Japan

Shinya Okuda