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Claims for Patent: 5,447,926

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Claims for Patent: 5,447,926

Title: Quinolone carboxylic acid derivatives
Abstract:A quinolone carboxylic acid derivative having the following formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom, Y is CH.sub.2, O, S, SO, SO.sub.2, or N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, and Z is an oxygen atom or two hydrogen atoms; or a salt thereof; and an antimicrobial agent comprising the same. The compound exhibits a superior antimicrobial activity, especially against gram positive microorganisms, and is thus useful for the treatments and prevention of various infectious diseases in clinics.
Inventor(s): Konno; Fujiko (Tomisato, JP), Shibata; Akihiro (Yachiyo, JP), Matsuda; Hideaki (Abiko, JP), Asaoka; Takemitsu (Narita, JP), Kawahara; Ryuichi (Ichikawa, JP), Taido; Naokata (Funabashi, JP), Kuraishi; Tasdayuki (Chiba, JP), Takeda; Sunao (Ichihara, JP)
Assignee: SS Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:08/305,977
Patent Claims: 1. A compound having the formula (I), ##STR26## wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom; or a salt thereof.

2. The compound of claim 1, wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, R.sup.2 is an amino group, and X is a hydrogen atom or a halogen atom.

3. The compound of claim 1, wherein X is a chlorine atom.

4. The compound of claim 2, wherein X is a chlorine atom.

5. An antimicrobial composition effective against bacteria selected from the group consisting of Gram negative and Gram positive microorganisms, comprising an antimicrobially effective amount of a compound of formula (I), ##STR27## wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom; or a salt thereof, and a pharmaceutically acceptable carrier.

6. The composition of claim 5, wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, R.sup.2 is an amino group, and X is a hydrogen atom or a halogen atom.

7. The composition of claim 5, wherein X is a chlorine atom.

8. The composition of claim 6, wherein X is a chlorine atom.

9. A method for curing an infectious disease caused by a microorganism selected from the group consisting of Gram negative and Gram positive microorganisms, comprising administering to a patient in need thereof an effective amount of a compound of the formula (I), ##STR28## wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, an ester residual group which can be hydrolyzed in living bodies, R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two lower alkyl groups, X is a hydrogen atom or a halogen atom; or a salt thereof.

10. The method of claim 9, wherein Z is two hydrogen atoms, Y is CH.sub.2, S, SO or SO.sub.2, R.sup.1 is a hydrogen atom, R.sup.2 is an amino group, and X is a hydrogen atom or a halogen atom.

11. The method of claim 9, wherein X is a chlorine atom.

12. The method of claim 10, wherein X is a chlorine atom.

13. The composition of claim 5, wherein said Gram positive microorganisms are methicillin-resistant.

14. The method of claim 9, wherein said Gram positive microorganisms are methicillin-resistant.
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