Sankyo Company, Limited

Akiko Ando

Hiroaki Yanagisawa

Hideo Nakao

Masami Fukushima

Hiroyuki Koike

Sadao Ishihara

Yasuteru Iijima

Takuro Kanazaki

Norio Nakamura

Yoshio Tsujita

Hachio Miyazawa

Masafumi Yoshimoto

Takuzo Nishimura

Compounds of formula (I): ##STR1## (wherein A is an alkylene group substituted by an optionally substituted amino or heterocyclic group and optionally interrupted by an oxygen or sulfur atom, R.sup.2 is various organic groups, B is C.sub.1 -C.sub.2 alkylene and Y is sulfur or methylene) and pharmaceutically acceptable salts and esters thereof are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group in place of the group A--CH(COOH)--NH--.

Perhydrothiazepine and perhydroazepine derivatives and their therapeutic

Compounds of formula (I): ##STR1## (wherein R.sup.1 and R.sup.3 are organic groups, A is a direct bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CO--CH.sub.2, --O--CH.sub.2 -- or --S--CH.sub.2 --, B is lower alkylene and n is 1-3) are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group at the 3-position.

Lactam derivatives and their use as hypotensive agents

Compounds of formula (I): ##STR1## (wherein: R.sup.1 represents an optionally substituted alkyl, cycloalkyl, aryl, partially hydrogenated aryl or heterocyclic group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent hydrogen or an optionally substituted alkyl, cycloalkyl, aralkyl, aryl, heterocyclic or heterocyclic-alkyl group or any adjacent pair thereof form a cyclic structure, at least one not being hydrogen; A represents a bond, or a methylene, ethylene, oxymethyl or thiomethyl group; B represents an alkylene, alkylidene, cycloalkylene or cycloalkylidene group; and n is 0, 1 or 2) and salts and esters thereof are hypotensive agents.

Perhydrothiazepine derivatives, their preparation and their therapeutic

7.alpha.-Methoxycephalosporin derivatives of general formula (I): ##STR1## wherein: R.sup.1 represents a hydroxy group; a C.sub.1 -C.sub.4 alkoxy group; a C.sub.2 -C.sub.5 aliphatic acyloxy group; a benzoyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or halogen substituents; a benzenesulphonyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.4 alkyl substituents; or a C.sub.1 -C.sub.3 alkanesulphonyloxy group which is unsubstituted or has one or more C.sub.1 -C.sub.3 alkoxy, cyano, nitro, halogen or C.sub.2 -C.sub.4 alkoxycarbonyl substituents;

7.alpha.-Methoxycephalosporin derivatives and their pharmaceutical

Process for preparing .beta.-lactam antibiotic substances useful as intermediate for various cephalosporin or penicillin derivatives, which comprises oxidation of 7-benzylideneaminocephem or 6-benzylideneaminopenam compounds capable of being converted to their quinoid forms by oxidation followed by reaction with lower alkanols.

Process for preparing beta-lactam antibiotic substances

Process for preparing 7-alkoxy cephalosporins useful as intermediates for various cephalosporin or penicillin derivatives which comprises reacting 7-benzylideneaminocephem or 6-benzylideneaminopenam compounds with a halide cation-producing compound in the presence of an alcohol and a base capable of forming a salt with a phenolic hydroxyl group or converting a phenolic hydroxyl group to phenolate ion.

Process for preparing alkoxylated derivatives of cephalosporin compounds

A process for introducing an alkoxy group into the 7.alpha.-position of a 7-amino-3-cephem-4-carboxylic acid derivative which comprises oxidizing a salt of 7-benzylideneamino-3-cephem-4-carboxylic acid derivative and reacting the product with an alkanol. The 7.alpha.-alkoxy-3-cephem-4-carboxylic acid derivatives obtained by the present invention are useful as intermediates for the synthesis of antibacterial agents.

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Tokyo, Japan

Akiko Ando