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Claims for Patent: 5,006,528

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Claims for Patent: 5,006,528

Title: Carbostyril derivatives
Abstract:A novel carbostyril derivative and salt thereof represented by the formula (1) ##STR1## (wherein R is a group of the formula ##STR2## ((wherein R.sup.1 is a C.sub.1- C.sub.3 alkoxy group)), a group of the formula ##STR3## ((wherein R.sup.2 and R .sup.3 are each, at the same time, a chlorine atom, a bromine atom; and R.sup.4 is a hydrogen atom or a chlorine atom)), 2-methyl-3-nitrophenyl group, 3,5-dichlorophenyl group, or a group of the formula ##STR4## ((wherein R.sup.5 is a chlorine atom or a bromine atom; and R.sup.6 is a methyl group)); the carbon-carbon bond between 3- and 4-position in the carbostyril skeleton is a single or double bond).
Inventor(s): Oshiro; Yasuo (Tokushima, JP), Sato; Seiji (Itano, JP), Kurahashi; Nobuyuki (Tokushima, JP)
Assignee: Otsuka Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:07/424,719
Patent Claims: 1. A carboxtyril compound or salt thereof of the formula, ##STR34## wherein R is a group of the formula ##STR35## wherein R.sup.1 is a C.sub.1 -C.sub.3 alkoxy group; a group of the formula ##STR36## wherein R.sup.2 and R.sup.3 are at the same time, both chlorine atoms, or both bromine atoms and R.sup.4 is a hydrogen atom or a chlorine atom; a 2-methyl-3-nitrophenyl group; a 3,5-dichlorophenyl group; or a group of the formula ##STR37## wherein R.sup.5 is a chlorine atom or a bromine atom and R.sup.6 is a methyl group; the carbon-carbon bond between the 3- and 4-positions in the carboxtyril skeleton being a single or a double bond.

2. The carboxtyril compound or salt thereof of claim 1, wherein R is a group of the formula ##STR38##

3. The carboxtyril compound or salt thereof of claim 2, wherein R.sup.1 is a methoxy group or an ethoxy group.

4. The carboxtyril compound or salt thereof of claim 1, wherein R is a group of the formula ##STR39##

5. The carbostyril compound or salt thereof of claim 4, wherein R.sup.2 and R.sup.3 are chlorine atoms and R.sup.4 is a hydrogen atom.

6. The carbostyril compound or salt thereof of claim 4, wherein R.sup.2 and R.sup.3 are bromine atoms and R.sup.4 is a hydrogen atom.

7. The carbostyril compound or salt thereof of claim 4, wherein R.sup.2, R.sup.3 and R.sup.4 are chlorine atoms.

8. The carbostyril compound or salt thereof of claim 1, wherein R is a 2-methyl-3-nitrophenyl group or a 3,5-dichlorophenyl group.

9. The carbostyril compound or salt thereof of claim 1, wherein R is a group of the formula ##STR40##

10. The carbostyril compound or salt thereof of claim 9, wherein R.sup.5 is a chlorine atom.

11. The carbostyril compound or salt thereof of claim 9, wherein R.sup.5 is a bromine atom.

12. 7-{4-[4-(2,3 -Dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydrocarbostyril.

13. 7-{4-[4-(b 2,3-Dichlorophenyl)-1-piperazinyl]-butoxy}carbostyril.

14. 7-{4-[4-(2-Ethoxyphenyl)-1-piperazinyl]butoxy}-3,4-dihydrocarbostyril.

15. 7-{4-[4-]2-Ethoxyphenyl)-1-piperazinyl]butoxy}-carbostyril.

16. A pharmaceutical composition for treating schizophrenia containing, as the active ingredient, a carbostyril compound or pharmaceutically acceptable salt thereof of claim 1 and a pharmaceutically acceptable carrier.

17. The pharmaceutical composition of claim 16, wherein the carbostyril compound or salt thereof is 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydrocarbostyril.

18. The pharmaceutical composition of claim 16, wherein the carbostyril compound or salt thereof is 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}carbostyril.

19. The pharmaceutical composition of claim 16, wherein the carbostyril compound or salt thereof is 7-{4-[4-(2-ethoxyphenyl)-1-piperazinyl]butoxy}-3,4-dihydrocarbostyril.

20. The pharmaceutical composition of claim 16, wherein the carbostyril compound or salt thereof is 7-{4-[4-(2-ethoxyphenyl)-1-piperazinyl]butoxy}carbostyril.

21. The pharmaceutical composition for treating schizophrenia containing, as the active ingredient, a carbostyril compound or pharmaceutically acceptable salt thereof of claim 3 and a pharmaceutically acceptable carrier.
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