Meiji Seika Kaisha, Ltd.

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Meiji Seika Kabushiki Kaisha

Drug Delivery System Institute, Ltd.

Meiji Saika Kaisha, Ltd.

Satoru Nakabayashi

Shinichi Kondo

Shunzo Fukatsu

Takashi Tsuruoka

Shigeo Seki

Shigeharu Inouye

Haruo Yamamoto

Toshinori Saito

Katsuyoshi Iwamatsu

Kiyoaki Katano

Ken Nishihata

Hiroko Ogino

Harumi Fukuyasu

Shokichi Nakajima

Tsutomu Tsuruoka

Nobuo Itoh

Yuuko Ishii

Hiroshi Watanabe

Hitoshi Ikeda

Takashi Yoshida

Seiji Shibahara

Hideaki Takahashi

Yasushi Murai

Masaji Sezaki

Tsuneo Okonogi

Shiro Miyoshi

Shigeharu Inoue

Hitoshi Yamauchi

Masahiro Onodera

Toshiyasu Ishimaru

Yuji Matsuhashi

Kunio Higashi

Takashi Ando

Chikako Udagawa

Takashi Tsuroka

Kumi Taniguchi

Lipid double-chain derivative containing polyoxyethylene

Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc., and new derivatives thereof which inhibit metastasis of cancer cells.

Cancer cell metastasis inhibitor methods

Sialic acid-containing glycolipid derivatives

Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are a hydrogen atom or a lower alkyl group of 1-5 carbon atoms and A is a hydrogen atom or a nucleophilic compound residue or pharmacologically acceptable salts thereof have excellent antibacterial activity against Gram positive and Gram negative microorganisms.

Cephalosporin compounds and antibacterial agents

Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc. and new derivatives thereof which markedly inhibit metastasis of cancer cells.

Cancer cell metastasis inhibitors and novel compounds

A therapeutic and/or prophylactic agent for viral infection, particularly human immunodeficiency virus (HIV) infection, which comprises as an active ingredient a lactam compound represented by formula (I) ##STR1## wherein X represents --COOR, wherein R represents a hydrogen atom or a straight-chain or branched-chain alkyl group having from 1 to 8 carbon atoms, or ##STR2## wherein n represents an integer of 2 or 3 and A represents methine when n is 2 or a quarternary carbon atom when n is 3, or a pharmaceutically acceptable salt or ester derivative thereof.

Antiviral agent containing lactam compound

This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.

Cephalosporin derivatives

A novel ester of a cephem compound having a carboxyl group at the 4-position in the nucleus; a process for preparing the same by reacting a cephem carboxylic acid or its salt with a halogenide; and a method for removing the protective group for the carboxyl group in the nucleus of a cephem compound by contacting it with an alcohol, or with an organic solvent in the presence of a Lewis acid.

Polychalcogen ester of cephem compound, process for preparing the same

A 9,3'-di-acyl derivative of a macrolide antibiotic can be readily produced by reacting a macrolide antibiotic or an acyl derivative thereof with an organic acid halide, particularly an alkanoic acid halide, in a solvent and in the presence of a molecular sieve consisting of a synthetic zeolite and then de-acylating partially the resultant acylation products by a partial hydrolysis in an aqueous alcohol to give the 9,3'-di-acyl derivative of the macrolide antibiotic.

Process for the production of a 9,3'-di-acyl derivative of a macrolide

A process for preparing a cephalosporanic acid derivative or a 7-acylaminocephalosporanic acid derivative which comprises subjecting an esterifying agent to reaction in liquid sulfur dioxide in the presence of a base with an N-protected-cephalosporin C to obtain a diester, subjecting the diester to reaction in an inert solvent with an iminohalide forming agent to produce an iminohalide, subjecting the iminohalide with a lower alcohol to produce an iminoether, subjecting the product produced, after subjecting the iminoether to reaction with a reactive derivative of an organic acid, to hydrolysis and further eliminating the ester group of the carboxylic acid.

Process for preparing cephalosporanic acid derivatives

A process for preparing a cephalosporin ester which comprises subjecting an organic halide or an alcohol to reaction with a cephalosporin acid, a cephalosporin acid halide or a salt thereof in the presence of liquid sulfur dioxide.

Process for preparing cephalosporin esters in the presence of liquid

Growing community of inventors

Yokohama, Japan

Satoru Nakabayashi