Trovafloxacin drug precursors (prodrugs) having free amino acid groups these precursors comprising an amino acid residue or a polypeptide chain of two or more amino acid residues which are covalently linked by peptide bonds including alatrofloxacin optionally in the form of a pharmaceutically acceptable salt, in particular the mesylate salt thereof

摘要

Azabicyclo quinolone carboxylic acids of formula (I) and their salts and prodrugs of (I) having free amino gps., are new. In (I) R1 = H, a cation or 1-6C alkyl; Y = ethyl, t-butyl, vinyl-cyclopropyl, 2-fluoroethyl, p-fluorophenyl or o,p-difluorophenyl; W = H, F, Cl, Br, 1-4C alkyl, 1-4C alkoxy, amino or aminomethyl; A = CH, CF, CCl, COCH3, C-CH3, C-CN or N, or A is carbon and is taken together with Y and the C and N to which A and Y are attached to form a 5 or 6 membered ring which may contain O or a double bond and which may have attached R8 which is methyl or methylene; R2 = gp. of formula (i) or (ii) where R3-R7,R9,R10,R25 = H, CH3, CH2NH2, CH2NHCH3 or CH2NHC2H5 and R5-R7 and R9 may also be NH2,NHCH3 or NHC2H5, provided that not more than 3 of R3-R7,R8,R10 and R25 are other than H and if 3 of these substits. are not H, at least one of them is methyl.