Claims
- 1. A carbostyril derivative or a pharmaceutically acceptable salt thereof, wherein said carbostyril derivative is represented by thereof, wherein said carbostyril derivative is represented by the general formula (1), ##STR56## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group or a lower alkynyl group; A is a group of the formula, ##STR57## (wherein R.sup.2 is a hydrogen atom or a lower alkyl group); B is a lower alkylene group; l is 1 when A is a group of the formula ##STR58## or l is 0 or 1 when A is a group of the formula ##STR59## R.sup.4 is an unsubstituted or substituted-phenyl group having 1 to 3 substituents, on the phenyl ring, selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; or R.sup.4 is a substituted-phenyl group having a lower alkylene-dioxy group as the substituent, on the phenyl ring, a phenyl-lower alkyl group, 1,2,3,4-tetrahydronaphthyl group or a group of the formula, ##STR60## R.sup.5 is a hydrogen atom, a hydroxy group or a lower alkanoyl group; the carbon-carbon bond between the 3- and 4-positions in the piperidine ring of formula (1) may be a double bond, in which case R.sup.5 does not exist; the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that (a) when R.sup.1 is a hydrogen atom, (b) when the substituted position of a group of the formula ##STR61## is at the 6-position in the carbostyril skeleton (A is a group of the formula ##STR62## B is a group of the formula ##STR63## (wherein R is a hydrogen atom or a lower-alkyl group); R.sup.4 is a phenyl-lower alkyl group or an unsubstituted phenyl group) and (c) when the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single bond, then R.sup.5 should not be a hydrogen atom.
- 2. The carbostyril derivatives and salts thereof according to claim 1, wherein R.sup.4 is an unsubstituted-or substituted-phenyl group having 1 to 3 substituents, on the phenyl ring, selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group.
- 3. The carbostyril derivatives and salts thereof according to claim 1, wherein R.sup.4 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent, on the phenyl ring, or 1,2,3,4-tetrahydronaphthyl group.
- 4. The carbostyril derivatives and salts thereof according to claim 1, wherein R.sup.4 is a phenyl-lower alkyl group.
- 5. The carbostyril derivatives and salts thereof according to claim 1, wherein R.sup.1 is a hydrogen atom.
- 6. The carbostyril derivatives and salts thereof according to claim 1, wherein R.sup.1 is a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, or a lower alkynyl group.
- 7. The carbostyril derivative or pharmaceutically acceptable salt thereof according to any one of claims 1 to 4, wherein the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single bond.
- 8. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 7, wherein B is ethylene, trimethylene, 2-methyltrimethylene, 2,2-dimethyltrimethylene, 1-methyltrimethylene, tetramethylene, pentamethylene or hexamethylene.
- 9. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 8, wherein the substituted position of the group of the formula ##STR64## is the 6-position in the carbostyril skeleton.
- 10. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 9, wherein B is trimethylene or tetramethylene.
- 11. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 10, wherein R.sup.1 is a hydrogen atom.
- 12. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 10, wherein R.sup.1 is a lower alkyl, a phenyl-lower alkyl, a lower alkenyl or a lower alkynyl group.
- 13. The carbostyril derivative or pharmaceutically acceptable salt thereof according to any one of claims 1 to 4, wherein the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a double bond.
- 14. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 13, wherein B is ethylene, trimethylene, 2-methyltrimethylene, 2,2-dimethyltrimethylene, 1-methyltrimethylene, tetramethylene, pentamethylene or hexamethylene.
- 15. The carbostyril derivative or pharmaceutically acceptible salt thereof according to claim 14, wherein the substituted position of the group of the formula ##STR65## is the 6-position in the carbostyril skeleton.
- 16. The carbostyril derivative or pharmaceutically acceptable salt thereof according to claim 15, wherein B is ethylene, trimethylene or tetramethylene.
- 17. The carbostyril derivative or pharmaceutically acceptable salt thereof according to any one of claims 1 to 4, wherein the substituted position of the group of the formula ##STR66## is the 6-position in the carbostyril skeleton and the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single bond.
- 18. The carbostyril derivative or pharmaceutically acceptable salt thereof according to any one of claims 1 to 4, wherein the substituted position of the group of the formula ##STR67## is the 6-position in the carbostyril skeleton and the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a double bond.
- 19. 6-[1-Oxo-3-(4-phenyl-1,2,5,6-tetrahydro-1-pyridyl)propyl]-3,4-dihydrocarbostyril.
- 20.6-{1-Oxo-3-[4-(4-chlorophenyl)-1,2,5,6-tetrahydro-1-pyridyl]propyl}-3,4-dihydrocarbostyril 1/4-hydrate.
- 21. A pharmaceutical composition comprising an antihistaminic agent containing an effective amount of at least one carbostyril derivative represented by the general formula (1) of claim 1, or a pharmaceutically acceptable salt thereof, as the active ingredient.
Priority Claims (2)
Number |
Date |
Country |
Kind |
55-28805 |
Mar 1980 |
JPX |
|
55-115022 |
Aug 1980 |
JPX |
|
Parent Case Info
This is a division of application Ser. No. 240,306, filed Mar. 4, 1981, now abandoned.
US Referenced Citations (7)
Foreign Referenced Citations (4)
Number |
Date |
Country |
0118771 |
Oct 1976 |
JPX |
0118772 |
Oct 1976 |
JPX |
0016478 |
Feb 1979 |
JPX |
0083749 |
Jun 1980 |
JPX |
Non-Patent Literature Citations (3)
Entry |
Schmidle, et al., J. Am. Chem. Soc., vol. 78, pp. 1702-1705 (1956). |
Ariens, et al., Arch. Int. Pharmacodyn., vol. 110, Nos. 2-3, pp. 275-299 (1957). |
van Rossum, Arch. Int. Pharmacodyn., vol. 143, Nos. 3-4, pp. 299-330 (1963). |
Divisions (1)
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Number |
Date |
Country |
Parent |
240306 |
Mar 1981 |
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