Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Yasuhiro Nishitani

Wataru Nagata

Tadashi Irie

Mitsuru Yoshioka

Teruji Tsuji

Toshiaki Aoki

Tsutomu Aoki

Yutaka Nishino

Yoshio Hamashima

Masayuki Narisada

Kenji Yamawaki

Koji Ishikura

Hiroshi Onoue

Yoshinori Yamano

Hikaru Itani

Jun Sato

Osamu Yoshida

Tsutomu Iwaki

Toshiro Konoike

Tadatoshi Kubota

Masayuki Sano

Kanji Tokuyama

Hisao Sato

Hideki Sugimoto

Mamoru Tanaka

Yuji Sendo

Shinya Hisakawa

Katsuki Yokoo

Makoto Kii

Issei Kato

Yusuke Takeoka

The present invention provides a novel compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria. Specifically, the present invention provides a compound of the formula (I): wherein each symbol is as defined in the specification, or an amino-protected compound when the amino group is present on the ring in the 7-side chain, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same.

Cephem compound having catechol or pseudo-catechol structure

The present invention provides a novel compound which has a broad antibacterial spectrum and particularly exhibits a high antibacterial activity on &#x3b2;-lactamase-producing gram-negative bacteria. Specifically provided are: a compound represented by formula (I) wherein the meaning of each symbol is as defined in the description, an amino-group-protected form of a type of the compound which has the amino group on a ring in a position-7 side chain, or a pharmaceutically acceptable salt of the compound or the amino-group-protected form; and a pharmaceutical composition containing the compound, the amino-group-protected form or the pharmaceutically acceptable salt.

Cephem compound having pyridinium group

The present disclosure describes Cephem compounds of the formula: wherein,

Cephalosporin having catechol group

The present invention provides a novel glycopeptide antibiotic derivative. These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof,whereinRis&#x2014;X&#x2014;Ar&#x2014;X&#x2014;Y&#x2014;X&#x2014;Ar

Glycopeptide antibiotic derivative

Cephem compounds having broad antibacterial spectrum

Broad spectrum cephem compounds

Imidazo&lsqb;4,5-b&rsqb;-pyridiniummethyl-containing cephem compounds having broad antibacterial spectrum activity

Imidazo&lsqb;4,5-b&rsqb;pyridiniummethyl-containing cephem compounds having broad antibacterial spectrum

A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Compounds and pharmaceutical compositions containing the same

A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R,is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Cephem compounds and pharmaceutical compositions containing the same

A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.

Intermediates for pyrrolidylthiocarbapenem derivative

The method for producing a sulfamide according to the present invention includes the step of reacting an alcohol and an oxycarbonylsulfamide compound in the presence of a trivalent phosphorus compound and an azodicarboxylic acid derivative. In one embodiment, the sulfamide is represented by Formula I, the alcohol is represented by Formula II, and the oxycarbonylsulfamide compound is represented by Formula III:

Production method for sulfamide

Pyrrolidylthiocarbapenem derivative

A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or a protecting group; R.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sup.3 is hydrogen, hydroxy, or amino; R.sup.4 is halogen; R.sup.5 and R.sup.6 each is identically or differently hydrogen or C.sub.1 -C.sub.3 alkyl; W is C.sub.1 -C.sub.3 alkylidene; X is N or C-Y; Y is hydrogen or halogen; or a pharmaceutically acceptable salt thereof, having a more potent antibacterial activity against G(+) and G(-) bacteria than known analogues, useful as antibacterial agents.

Pyridonecarboxylic acids and their anti-bacterial compositions

An antibacterial cephalosporin hydroxamic acid derivative represented by the following formula (I), processes for its preparation, compositions containing the same as an active ingredient, and a method for killing bacteria by contacting with said compound. ##STR1## (wherein, R is acyl; R.sup.1 is hydrogen or methoxy; R.sup.2 is alkylene; R.sup.3 is hydrogen, aliphatic group or a hydroxy-protecting group; R.sup.4 is hydrogen or amino-protecting group; R.sup.5 is hydrogen, light metal atom or carboxy-protecting group; and X is oxygen, sulfur, or sulfinyl).

1-oxadethia cephalosporin hydroxamic acid derivatives

Growing community of inventors

Osaka, Japan

Yasuhiro Nishitani