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Details for Patent: 5,385,900

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Details for Patent: 5,385,900

Title: Quinoline 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 (Chiba, JP), Shibata; Akihiro (Yachiyo, JP), Matsuda; Hideaki (Abiko, JP), Asaoka; Takemitsu (Narita, JP), Kawahara; Ryuichi (Ichikawa, JP), Taido; Naokata (Funabashi, JP), Kuraishi; Tadayuki (Chiba, JP), Takeda; Sunao (Ichihara, JP)
Assignee: SS Pharmaceutical Co., Ltd. (Tokyo, JP)
Filing Date:Nov 08, 1993
Application Number:08/149,134
Claims:1. A quinolone carboxylic acid derivative having the formula (I), ##STR26## wherein Z is an oxygen atom, Y is N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, or 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 and X is a hydrogen atom or a halogen atom; or a salt thereof.

2. The quinolone carboxylic acid derivative of claim 1, wherein Z is an oxygen atom, Y is NH, R.sup.1 is a hydrogen atom, R.sup.2 is hydrogen atom, and X is a hydrogen atom or a halogen atom; or a salt thereof.

3. The quinolone carboxylic acid derivative of claim 1, wherein X is a chlorine atom.

4. The quinolone carboxylic acid derivative of claim 2, wherein X is a chlorine atom.

5. The quinolone carboxylic acid derivative of claim 1, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group.

6. The quinolone carboxylic acid derivative of claim 1, wherein R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.

7. The quinolone carboxylic acid derivative of claim 1, wherein R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies.

8. The quinolone carboxylic acid derivative of claim 1, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group, R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies, and R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.

9. An antimicrobial composition, comprising an antimicrobially effective amount of a quinolone carboxylic acid derivative of formula (I) ##STR27## wherein Z is an oxygen atom, Y is N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, or 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 and X is a hydrogen atom or a halogen atom; or a salt thereof, and a pharmaceutically acceptable carrier.

10. The composition of claim 9, wherein Z is an oxygen atom, Y is NH, R.sup.1 is a hydrogen atom, R.sup.2 is a hydrogen atom, and X is a hydrogen atom or a halogen atom; or a salt thereof.

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

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

13. The composition of claim 9, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group.

14. The composition of claim 9, wherein R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.

15. The composition of claim 9, wherein R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies.

16. The composition of claim 9, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group, R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies, and R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.

17. A method for curing an infectious disease caused by a microorganism, comprising administering to a patient in need thereof an effective amount of a quinolone carboxylic acid derivative of the formula (I) ##STR28## wherein Z is an oxygen atom, Y is N--R.sup.3, wherein R.sup.3 is a hydrogen atom or a lower alkyl group, R.sup.1 is a hydrogen atom, an alkyl group, an aralkyl group, or 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 and X is a hydrogen atom or a halogen atom; or a salt thereof.

18. The method of claim 17, wherein Z is an oxygen atom, Y is NH, R.sup.1 is a hydrogen atom, R.sup.2 is a hydrogen atom, and X is a hydrogen atom or a halogen atom; or a salt thereof.

19. The method of claim 17, wherein X is a chlorine atom.

20. The method of claim 18, wherein X is a chlorine atom.

21. The method of claim 17, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group.

22. The method of claim 17, wherein R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.

23. The method of claim 17, wherein R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies.

24. The method of claim 17, wherein R.sup.3 is a hydrogen atom or a C.sub.1 -C.sub.5 -alkyl group, R.sup.1 is a hydrogen atom; a C.sub.1 -C.sub.12 -alkyl group; an aralkyl group selected from the group consisting of benzyl, phenylethyl, methylbenzyl, and naphthylmethyl; or an ester residual group which can be hydrolyzed in living bodies, and R.sup.2 is a hydrogen atom or an amino group which may be substituted by one or two C.sub.1 -C.sub.5 -alkyl groups.
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