Banyu Pharmaceutical Co. Ltd

Merck + Co., Inc.

Eiichi Mano

Susumu Nakagawa

Ryosuke Ushijima

Koji Yamada

Fumio Nakano

Paul N Devine

David M Tschaen

Zhiguo Jake Song

Mangzu Zhao

Minoru Sanada

Norikazu Ban

The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##

Oxidation process using tempo

The present invention relates to stable crystalline (6R,7R)-7-(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxylimino)ac etamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carbox ylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino) acetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carb oxylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.

Crystalline cephalosporin compounds

A compound having the formula: ##STR1## wherein R is a hydrogen atom, a lower alkyl group, an alkanoyl group, an aralkyl group, an alkylsulfonyl group or an arylsulfonyl group, and R.sup.1 is a hydrogen atom or a protecting group for a hydroxyl group, or a salt thereof.

Isoindoline derivatives and processes for their preparation

The present invention relates to stable cyrstalline (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)ac etamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)-3-cephem-4-carboxylate sulfate or its hydrate, a process for production of the compound and (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxyl-1-methylethoxyimino)a cetamido]-3-(5,6-dihydroxy-2-methyl-2-isoindolinium)methyl-3-cephem-4-carbo xylate hydrochloride or its hydrate which is a starting material useful for the production of the desired compound of the present invention.

A compound having the formula: ##STR1## wherein R.sup.1 is an amino group or a protected amino group, R.sup.2 is a hydrogen atom or a protecting group for a hydroxyl group, R.sup.3 represents negative charge, a hydrogen atom or a protecting group for a carboxyl group, and n is 0 or 1, and a salt thereof.

7-amino-3-(substituted isoindolinium)methyl-3-cephem derivatives

The invention relates to an antibiotic comprising a compound having the formula: ##STR1## wherein R.sup.1 is a straight chain, branched chain, or cyclic lower alkyl group which may be substituted by a carboxyl group, and R.sup.2 designates vicinal dihydroxyl groups or diacetoxy groups; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

3-Isoquinoliniomethyl cephalosporin derivatives

A compound having the formula: ##STR1## wherein R.sup.1 is a straight chain, branched chain or cyclic lower alkyl group which may be substituted by a carboxyl group, and each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom, a hydroxyl group, a methoxy group or an acetoxy group, and R.sup.4 is a hydroxyl group, a methoxy group or an acetoxy group; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.

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Kariya, Japan

Eiichi Mano