Moxifloxacin its hydrates and its pharmaceutically acceptable acid addition salts and its alkali metal alkaline earth metal and guanidine m-rate salts as well as the d-riv-s c1-c4-alkyl-and (5-m-thyl -oxo-1,3-dioxol-4-yl) -m-thyhlester of basic carboxylic acids as well as the rac-mates of these products

摘要

7-(1-Pyrrolidinyl)-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid and 7-(1-pyrrolidinyl)-1,4-dihydro-4-oxo-1,8-naphthyridin-3-carboxylic derivs. of formula (I), their hydrates, acid addition salts, as well as their alkali metal, alkaline earth, silver and guanidinium salts are new; X1 = halo; X2 = H, NH2, 1-4C alkylamino, di(1-3C alkyl)amino, OH, 1-4C alkoxy, SH, 1-4C alkylthio, arylthio or halo; R1 = 1-4C alkyl, 2-4C alkenyl, 3-6C cycloalkyl, 2-hydroxyethyl, 2-fluoroethyl, OMe, NH2, MeNH, EtNH or Me2N; or is Ph (opt. mono- or disubstd. by F); R2 = H, 1-4C alkyl or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl; R3 = a gp. of formula (a): R4 = 1-4C alkyl, aryl or 1-4C acyl; R5 = H, 1-4C alkyl, OH or OMe; R6 = H, 1-4C alkyl (opt. substd. by OH), aryl, heteroaryl, benzyl, 1-4C alkoxycarbonyl, 1-4C acyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl or 3-6C cycloalkyl; R7 = H or 1-4C alkyl; R',R'' = H, Me or Ph; R''' = H or Me; Y = O, CH2, CH2CH2 or CH2O (where the bond to N may be via C as well as O); (Note: Y is not otherwise defined in claim 1). Z = O or S; A = N or CR8; R8 = H, halo, Me, CN, NO2 or OH, or R8+R1 = a bridge of type (b)-(d): Cpds. of formula (e) are excluded; R1 = 1-4C alkyl; R2,R3 = H or 1-4C alkyl; R4 = cyclopropyl, Ph, halophenyl, thienyl, opt. substd. by 1-4C alkyl or halo; R5 = halo. Also claimed is the S,S-configuration of a cpd. of formula (f) and its salts:A = CCl, CF or COMe.