|Title:|| 8-alkoxyquinolonecarboxylic acid and salts thereof|
|Abstract:||Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group or substituted lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.|
|Inventor(s):|| Masuzawa; Kuniyoshi (Koga, JP), Suzue; Seigo (Kuki, JP), Hirai; Keiji (Kuki, JP), Ishizaki; Takayoshi (Washimiya, JP) |
|Assignee:|| Kyorin Pharmaceutical Co., Ltd. (Tokyo, JP) |
|Filing Date:||Oct 22, 1990|
|Claims:||1. A compound of the formula: ##STR27## wherein R.sup.1 is lower alkyl, X is halogen, R is hydrogen or lower alkyl, n is 0 or 1, R.sup.4 is hydrogen, lower alkyl or substituted lower alkyl and R.sup.5 is hydrogen, lower alkyl, acyl, or alkoxy carbonyl. |
2. The compound of claim 1 which is 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4- oxo-3-quinolinecarboxylic acid.
3. The compound of claim 1 which is 7-(3-aminomethyl-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-meth oxy-4-oxo-3-quinolinecarboxylic acid.
4. The compound of claim 1 which is 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methylaminomethyl-1-pyrr olidinyl)-4-oxo-3-quinolinecarboxylic acid.
5. The compound of claim 1 which is 1-cyclopropyl-7-(3-ethylaminomethyl-1-pyrrolidinyl)-b 6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecaboxylic acid.