摘要 |
Acyl derivatives of the formula <IMAGE> I in which R is an acyl group, excluding those acyl groups of the formula <IMAGE> in which A is a group of the formulae -NHCO-, -NHCONHCO-, -NHCOCH=CH-, <IMAGE> wherein R6 is hydrogen or lower alkyl; R1 and R2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or -OR2, n is 1 or 2, R4 and R5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R4 and R5 both represent hydrogen) or a group of the formula -O-B- (where R4 and R5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene; and wherein R3 is a substituted bicyclic group of the formulae <IMAGE> <IMAGE> <IMAGE> <IMAGE>7 5 NR7NNN+RE wherein R7 and R8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R'' and R''' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R4 and R5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates, as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts. These compounds are useful as antibiotics. |
申请人 |
HOFFMANN-LA ROCHE & CO AG, F. |
发明人 |
FURLENMEIER, ANDRE;GOETSCHI, ERWING;HEBEISEN, PAUL;HOFHEINZ, WERNER;LINK, HELMUT |