| 摘要 |
Quinoline derivs. of formula (I) and their pharmaceutically acceptable salts are new. - In (I), R1 = OH, 1-6C alkoxy or NR4R5; R4 and R5 = H or 1-6C alkyl; R2 = H, OH, 1-6C alkanoylamino, morpholine, halo, CN, 1-6C hydroxyalkyl, COOR6, 1-6C alkoxy or NR7R8; R6 = H or 1-6C alkyl; R7 and R8 = H, 1-6C alkyl, 2-6C aminoalkyl, 2-6C alkylamin-(2-6C)alkyl or di(1-6C alkyl)amino-(1-6C)alkyl; R3 = H, 1-6C alkyl or phenyl (opt. substd. by 1-2 of 1-6C alkyl, NO2, NH2, halo, 1-2C alkyl substd. by 1-5 halo, OH, or 1-6C alkoxy. Pref. R1 = NH2 or esp. OH; R2 = H, NH2, OH, acetylamino, CH2OH or COOR6 (esp. H, NH2 or OH); R6 = H; R3 = H or phenyl; and salt = alkali(ne earth) metal salt. - 6 Cpds. (I) viz. 1-cyclopropyl- 6-fluoro-1,4-dihydro-7-Q-4-oxo-3- quinolinecarboxylic acid (Q = 1-azetidinyl, 3-hydroxy-1-azetidinylm 3-amino-1-azetidinyl, 3-acetyl amino-1-azetidinyl, 2-methyl-3-methyl-1-azetidinyl or 2-phenyl-3-amino-1-azetidinyl are specifically claimed. |
