Hoffmann-la Roche Inc.

Roland Reiner

Marc Montavon

Urs Weiss

Peter Angehrn

There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.

Cephalosporin intermediates

There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.

Acyl derivatives

5-Oxo-as-triazines

There is provided cephalosporin derivatives of the formula ##STR1## in which R.sup.1 is carboxy-lower alkyl and

Thiazolylacetamido compounds

There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl- 5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.

Cephalosporin derivatives

There are presented cephalosporin derivatives of the formula ##STR1## wherein X is the group ##STR2## R is hydrogen or a readily hydrolyzable ester or ether group and n stands for 1 or 2, as well as salts of these compounds and hydrates of these compounds and salts.

Cephalosporins represented by the formula

Cephalosporins

Acyl derivatives of the formula ##STR1## wherein R signifies hydrogen or a protective group which can be split off, R.sup.1 signifies lower alkyl and X signifies the group ##STR2## wherein one of the residues R.sup.2 and R.sup.3 represents hydrogen and the other represents alkyl and R.sup.4 represents lower alkyl the easily hydrolyzable esters and ethers thereof, the salts and hydrates of the above compounds, esters, ethers and salts.

Thiazolylacelamide cephalosporins

There is presented cephalosporin derivatives which are the readily hydrolysable esters and ethers of compounds of the general formula ##STR1## wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.1 represents lower alkyl or aminocarbonylmethyl and X represents a group of the formula ##STR2## in which one of the two symbols R.sub.2 and R.sub.3 represents hydrogen and the other represents lower alkyl and R.sub.4 represents lower alkyl, as well as salts of said esters and ethers and hydrates of said esters, ethers and salts.

The acyl derivatives provided by the present invention are compounds of the general formula ##STR1## wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R.sub.1 represents alkyl or aminocarbonylmethyl and X represents a group of the formula ##STR2## in which one of the two symbols R.sub.2 and R.sub.3 or R.sub.4 and R.sub.5 represents hydrogen

Derivatives of 7 [-substituted oxyimins acetamido] cephalosporins

Compounds represented by the following formula ##STR1## wherein R is hydrogen, lower alkanoyloxymethyl, lower alkyl, indanyl or a radical represented by the formula ##STR2## wherein X may be hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or a lower alkoxy-lower alkyl group, Pharmaceutically acceptable salts and hydrates thereof. These compounds are useful as antibiotics.

Growing community of inventors

Basel, Switzerland

Roland Reiner