Meiji Seika Kaisha, Ltd.

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Other

Meiji Seika Kabushiki Kaisha

Toshiaki Kudo

Seiji Shibahara

Shinichi Kondo

Atsushi Tamura

Masaki Tsushima

Tomio Takeuchi

Takao Abe

Yasushi Murai

Daishiro Ikeda

Tsuneo Okonogi

Shuichi Gomi

Ken Nishihata

Akihiro Morinaka

Kenji Asai

Takayuki Usui

Yoko Ikeda

Yukiko Hiraiwa

Naoko Miike

Ken Chikauchi

Kaori Tadauchi

Mizuyo Ida

Takashi Yoshida

Katsuyoshi Iwamatsu

Kunio Atsumi

Yuko Kano

Sohjiro Shiokawa

Masako Imai

Eijiro Umemura

A new metallo-&#x3b2;-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of &#x3b2;-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-&#x3b2;-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of &#x3b2;-lactam antibiotics against metallo-&#x3b2;-lactamase producing bacteria by combining the compound of the general formula (I) with &#x3b2;-lactam antibiotics. 

Metallo-&#x3b2;-lactamase inhibitors

A medicament useful for preventive and/or therapeutic treatment of nerve system diseases which comprises, as an active ingredient, a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof:wherein, X represents a group represented by the following general formula (II), (III), (IV), (V), or (VI),'A' represents a saturated or unsaturated 3- to 6-membered carbocyclic group and the like, 'B' represents CHand the like, &#x201c;n&#x201d; represents 0 to 2, Rrepresents a hydrogen atom, a halogen atom and the like, R, R, and Rto Rrepresent a hydrogen atom, a lower alkyl group which may be substituted and the like, Rrepresents a hydrogen atom, a lower alkyl group which may be substituted and the like, Rrepresents a hydrogen atom, a halogen atom and the like, Rrepresents a saturated or unsaturated monocyclic or bicyclic carbocyclic group and the like, and Rand R, Rand R, Rand R, or Rand Rmay bind to each other to form a cyclic structure.

Phenoxyalkylamine derivatives useful as opioid &#x3b4; receptor agonists

Diphenylalkylamine derivatives useful as opioid receptor agonists

Cephem derivatives

As new dibekacin derivatives and new arbekacin derivatives are now provided 2'-amino-2'-deoxydibekacin, 2'-amino-5,2'-dideoxydibekacin, 2'-amino-2'-deoxyarbekacin, 2'-amino-5,2'-dideoxyarbekacin, 2'-amino-5,2'-dideoxy-5-epi-fluoroarbekacin and 2'-amino-5,2'-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Dibekacin derivatives and arbekacin derivatives active against resistant

New cephalosporin derivatives of a general formula (I) and non-toxic salts and non-toxic esters thereof are provided: ##STR1## (wherein R represents an acyclic or cyclic lower alkyl group having 1-6 carbon atoms, which may optionally be substituted by a halogen atom; the steric configuration as asterisked (*) includes an optical-active (R)-form or (S)-form or an optical-inactive (RS)-form; n is 0 or 1, n.sup.1 is 0 to 3, n.sup.2 is 0 to 3; and when n.sup.1 is 0, n.sup.2 is 3; when n.sup.1 is 1, n.sup.2 is 2; when n.sup.1 is 2, n.sup.2 is 1; when n.sup.1 is 3, n.sup.2 is 0). The new derivatives of the formula (I) and non-toxic salts and esters thereof have high bactericidal activity with broad antibacterial spectra, and these are useful as active ingredients in bactericides.

Cephalosporin derivatives and antibiotics containing the same

Cephalosporin compounds having 2-(2-aminothiazol-4-yl)-2{(1S)-carboxyethoxyimino}acetyl group on the side chain at the 7-position thereof and 1-ethylpyridinium-4-ylthiomethyl group on the side chain at the 3-position thereof or non-toxic salts thereof are excellent antibacterial agents for mammals including human. The cephalosporin derivatives have low toxicity.

Antibacterial agent for mammal use comprising cephalosporin derivatives

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Yokohama, Japan

Toshiaki Kudo