Claims
- 1. A carbostyril derivative or a pharmaceutically acceptable salt thereof, said carbostyril derivative being represented by the general formula (1), ##STR15## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s) then R.sup.4 should be neither a hydroxyl group nor a lower alkanoyl group, or a quaternary salt represented by the general formula (1e), ##STR16## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y, n and the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton are the same as defined above, R.sup.6 is a lower alkyl group and Q is a halogen atom.
- 2. The carbostyril derivative or salt thereof or quaternary salt according to claim 1, wherein R.sup.4 is a hydrogen atom.
- 3. The carbostyril derivative or salt thereof or quaternary salt according to claim 2, wherein R.sup.3 is a phenyl group or a lower alkyl group having phenyl group(s) as the substituted group(s).
- 4. The carbostyril derivative or salt thereof or quaternary salt according to claim 3, wherein R.sup.1 is a hydrogen atom.
- 5. The carbostyril derivative or salt thereof or quaternary salt according to claim 3, wherein R.sup.1 is a lower alkyl group which may have phenyl group(s) as the substituted group(s).
- 6. The carbostyril derivative or salt thereof or quaternary salt according to claim 3, wherein R.sup.1 is a lower alkenyl group or a lower alkynyl group.
- 7. The carbostyril derivative or salt thereof or quaternary salt according to claim 2, wherein R.sup.3 is a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups.
- 8. The carbostyril derivative or salt thereof or quaternary salt according to claim 7, wherein R.sup.1 is a hydrogen atom.
- 9. The carbostyril derivative or salt thereof or quaternary salt according to claim 7, wherein R.sup.1 is a lower alkyl group which may have phenyl group(s) as the substituted group(s).
- 10. The carbostyril derivative or salt thereof or quaternary salt according to claim 7, wherein R.sup.1 is a lower alkenyl group or a lower alkynyl group.
- 11. The carbostyril derivative or salt thereof or quaternary salt according to claim 1, wherein R.sup.4 is a hydroxyl group or a lower alkanoyl group.
- 12. The carbostyril derivative or salt thereof or quaternary salt according to claim 11, wherein R.sup.1 is a hydrogen atom.
- 13. The carbostyril derivative or salt thereof or quaternary salt according to claim 11, wherein R.sup.1 is a lower alkyl group which may have phenyl group(s) as the substituted group(s).
- 14. The carbostyril derivative or salt thereof or quaternary salt according to claim 11, wherein R.sup.1 is a lower alkenyl group or a lower alkynyl group.
- 15. The carbostyril derivative or salt thereof or quaternary salt according to claim 3, claim 7 or claim 11, wherein Y is a lower alkylene group.
- 16. The carbostyril derivative or salt thereof or quaternary salt according to claim 3, claim 7 or claim 11, wherein Y is a lower alkylene group having hydroxyl group(s) as the substituted group(s).
- 17. 1-Methyl-5-[3-(4-benzyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 18. 7-[3-(4-Benzyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 19. 7-[3-(4-Phenyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 20. 1-Benzyl-5-[2-hydroxy-3-(4-benzyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 21. 1-Ethyl-5-[2-hydroxy-3-(4-benzyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 22. 7-[2-Hydroxy-3-(4-phenyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 23. 1-(3-Phenylpropyl)-7-[3-(4-phenyl-1-piperidyl)propoxy]-3,4-dihydrocarbostyril.
- 24. An antihistaminic agent containing an antihistaminically effective amount of at least one carbostyril derivative or pharmaceutically acceptable salt thereof or quaternary salt of claim 1 as the active ingredient.
Priority Claims (2)
Number |
Date |
Country |
Kind |
54-120452 |
Sep 1979 |
JPX |
|
54-125565 |
Sep 1979 |
JPX |
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CROSS-REFERENCE TO RELATED APPLICATION
This application is a continuation-in-part of application Ser. No. 327,460 filed on Dec. 4, 1981 which is in turn a continuation application of U.S. Ser. No. 186,340 filed on Sept. 11, 1980 both now abandoned.
US Referenced Citations (7)
Foreign Referenced Citations (10)
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2912105 |
Oct 1979 |
DEX |
0106977 |
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Continuations (1)
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Number |
Date |
Country |
Parent |
186340 |
Sep 1980 |
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Continuation in Parts (1)
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Number |
Date |
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Parent |
327460 |
Dec 1981 |
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