US4455422A
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Carbostyril derivatives and pharmaceutical composition containing the same
Assignee: Otsuka Pharmaceutical Co Ltd
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Filing: 1982-04-07
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Granted: 1984-06-19
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Expires: 2002-04-07
Abstract
Abstract Novel carbostyril derivatives and their salts, having antihistaminic effect and central nervous system controlling effect, are represented by the general formula (1), ##STR1## wherein R 1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, a lower alkynyl group; A is a group of the formula ##STR2## (wherein R 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 ##STR3## or l is 0 or 1 when A is a group of the formula ##STR4## Z is a group of the formula >N--R 3 or ##STR5## (wherein R 3 , R 4 and R 5 are as defined herein).
Inventors
- 👤 Kazuo Banno
- 👤 Takafumi Fujioka
- 👤 Masaaki Osaki
- 👤 Kazuyuki Nakagawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 05:38
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/20; C07D215/22; C07D215/227
Claims Analysis
Total Claims: 30
Claim 1
Independent Claim
165 words
A carbostyril derivative or salt thereof represented by the general formula (1), ##STR54## wherein R 1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group or a lower alkynyl group; R 2 is a hydrogen atom or a lower alkyl group; B is a lower alkylene group; l is 0 or 1; R 3 is an unsubstituted or a 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, a lower alkoxy group, a lower alkoxy-carbonyl group, a carboxy group, a lower alkylthio group, a lower alkanoyl group, a hydroxy group, a nitro group, an amino group and a cyano group; or R 3 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent on the phenyl ring, a phenyl-lower alkyl group or 1,2,3,4-tetrahydronaphthyl group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond.
Claim 2
Dependent Claim
165 words
A carbostyril derivative or salt thereof represented by the general formula (1), ##STR54## wherein R 1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group or a lower alkynyl group; R 2 is a hydrogen atom or a lower alkyl group; B is a lower alkylene group; l is 0 or 1; R 3 is an unsubstituted or a 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, a lower alkoxy group, a lower alkoxy-carbonyl group, a carboxy group, a lower alkylthio group, a lower alkanoyl group, a hydroxy group, a nitro group, an amino group and a cyano group; or R 3 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent on the phenyl ring, a phenyl-lower alkyl group or 1,2,3,4-tetrahydronaphthyl group; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond.
Claim 3
Dependent Claim
17 words
The carbostyril derivative or salt thereof according to claim 1, wherein R 1 is a hydrogen atom.
Claim 4
Dependent Claim
29 words
The carbostyril derivative or salt thereof according to claim 2, wherein the substituted position of a group of the formula, ##STR55## is at the 6-position in the carbostyril skeleton.
Claim 5
Dependent Claim
32 words
The carbostyril derivative or salt thereof according to claim 2, wherein the substituted position of a group of the formula, ##STR56## is at the 5-, 7- or 8-position in the carbostyril skeleton.
Claim 6
Dependent Claim
47 words
The carbostyril derivative or salt thereof according to claim 2, wherein R 3 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.
Claim 7
Dependent Claim
60 words
The carbostyril derivative or salt thereof according to claim 2, wherein R 3 is a substituted-phenyl group having 1 to 3 substituents, on the phenyl ring, selected from the group consisting of a lower alkoxy-carbonyl group, a carboxy group, a lower alkylthio group, a lower alkanoyl group, a hydroxy group, a nitro group, an amino group and a cyano group.
Claim 8
Dependent Claim
33 words
The carbostyril derivative or salt thereof according to claim 2, wherein R 3 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent on the phenyl ring or a 1,2,3,4-tetrahydronaphthyl group.
Claim 9
Dependent Claim
18 words
The carbostyril derivative or salt thereof according to claim 2, wherein R 3 is a phenyl-lower alkyl group.
Claim 10
Dependent Claim
29 words
The carbostyril derivative or salt thereof according to claim 5, wherein the substituted position of the group of the formula, ##STR57## is at the 6-position in the carbostyril skeleton.
Claim 11
Dependent Claim
32 words
The carbostyril derivative or salt thereof according to claim 5, wherein the substituted position of the group of the formula, ##STR58## is at the 5-, 7- or 8-position in the carbostyril skeleton.
Claim 12
Dependent Claim
29 words
The carbostyril derivative or salt thereof according to claim 6, wherein the substituted position of the group of the formula, ##STR59## is at the 6-position in the carbostyril skeleton.
Claim 13
Dependent Claim
29 words
The carbostyril derivative or salt thereof according to claim 7, wherein the substituted position of the group of the formula, ##STR60## is at the 6-position in the carbostyril skeleton.
Claim 14
Dependent Claim
29 words
The carbostyril derivative or salt thereof according to claim 8, wherein the substituted position of the group of the formula, ##STR61## is at the 6-position in the carbostyril skeleton.
Claim 15
Dependent Claim
31 words
The carbostyril derivative or salt thereof according to claim 1, wherein R 1 is a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, or a lower alkynyl group.
Claim 16
Dependent Claim
1 words
6-{4-[4-(3-Chlorophenyl)-1-piperazinyl]-1-butenyl}-3,4-dihydrocarbostyril.
Claim 17
Dependent Claim
1 words
6-{4-[4-(3-Chlorophenyl)-1-piperazinyl]-1-butenyl}-3,4-dihydrocarbostyril.
Claim 18
Dependent Claim
1 words
6-{3-[4-(2-Methoxyphenyl)-1-piperazinyl]-1-propenyl}-3,4-dihydrocarbostyril.
Claim 19
Dependent Claim
1 words
6-{3-[4-(2-Methoxyphenyl)-1-piperazinyl]-1-propenyl}-3,4-dihydrocarbostyril.
Claim 20
Dependent Claim
1 words
6-[4-(4-Phenyl-1-piperazinyl)-1-butenyl]-3,4-dihydrocarbostyril.
Claim 21
Dependent Claim
1 words
6-[4-(4-Phenyl-1-piperazinyl)-1-butenyl]-3,4-dihydrocarbostyril.
Claim 22
Dependent Claim
2 words
6- 3-[4-(3-Chlorophenyl)-1-piperazinyl]-1-propenyl-3,4-dihydrocarbostyril.
Claim 23
Dependent Claim
2 words
6- 3-[4-(3-Chlorophenyl)-1-piperazinyl]-1-propenyl-3,4-dihydrocarbostyril.
Claim 24
Dependent Claim
2 words
6- 3-[4-(3-Methylphenyl)-1-piperazinyl]-1-propenyl-3,4-dihydrocarbostyril.
Claim 25
Dependent Claim
2 words
6- 3-[4-(3-Methylphenyl)-1-piperazinyl]-1-propenyl-3,4-dihydrocarbostyril.
Claim 26
Dependent Claim
2 words
6- 4-[4-(2,3-Dimethylphenyl)-1-piperazinyl]-1-butenyl-3,4-dihydrocarbostyril.
Claim 27
Dependent Claim
2 words
6- 4-[4-(2,3-Dimethylphenyl)-1-piperazinyl]-1-butenyl-3,4-dihydrocarbostyril.
Claim 28
Dependent Claim
1 words
6-[3-(4-Phenyl-1-piperazinyl)-1-propenyl]-3,4-dihydrocarbostyril.
Claim 29
Dependent Claim
1 words
6-[3-(4-Phenyl-1-piperazinyl)-1-propenyl]-3,4-dihydrocarbostyril.
Claim 30
Dependent Claim
27 words
A central nervous system controlling agent containing at least one carbostyril derivative represented by the general formula (1) as claimed in claim 1 as the active ingredient.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-06-19 | 1987-12-19 | 1988-06-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-06-19 | 1991-12-19 | 1992-06-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-06-19 | 1995-12-19 | 1996-06-19 | $7700.00 | Window Closed / Lapsed |