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US4760064A
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Carbostyril compounds, compositions containing same and processes for preparing same
Assignee: Otsuka Pharmaceutical Co Ltd
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Filing: 1985-12-13
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Granted: 1988-07-26
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Expires: 2005-12-13
Abstract
Abstract A carbostyril compound of the formula (I): ##STR1## wherein R 1 and R 2 are as defined or its pharmaceutically acceptable salt, composition containing the compound and processes for preparing the same are disclosed. The compound is useful as a cardiotonic agent.
Inventors
- 👤 Michiaki Tominaga
- 👤 Takafumi Fujioka
- 👤 Kazuyoshi Nagami
- 👤 Kazuyuki Nakagawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 03:51
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/38
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
124 words
A carbostyril compound of the formula (I): ##STR56## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenyl-lower alkyl group which has, on the phenyl ring thereof, 1 to 3 substituents selected from among lower alkanoyloxy and hydroxy groups, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, withn 1 to 3 substituents selected from the group consisting of nitro, unsubstituted or lower alkyl-substituted amino, phenyl-lower alkoxy, hydroxy, carboxy, phenyl-lower alkoxycarbonyl-lower alkoxy, lower alkanoyloxy, carboxy-lower alkoxy and lower alkyl-substituted amino-lower alkyl, or a naphthoyl group, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 lower alkoxy groups, and its pharmaceutically acceptable salt.
Claim 2
Dependent Claim
124 words
A carbostyril compound of the formula (I): ##STR56## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenyl-lower alkyl group which has, on the phenyl ring thereof, 1 to 3 substituents selected from among lower alkanoyloxy and hydroxy groups, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, withn 1 to 3 substituents selected from the group consisting of nitro, unsubstituted or lower alkyl-substituted amino, phenyl-lower alkoxy, hydroxy, carboxy, phenyl-lower alkoxycarbonyl-lower alkoxy, lower alkanoyloxy, carboxy-lower alkoxy and lower alkyl-substituted amino-lower alkyl, or a naphthoyl group, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 lower alkoxy groups, and its pharmaceutically acceptable salt.
Claim 3
Dependent Claim
33 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 1, wherein R 2 is a benzoyl group which is substituted with 1 or 2 of a (C 1-6 )alkoxy group.
Claim 4
Dependent Claim
71 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 2, wherein R 1 is a benzoyl group which may optionally be substituted, on the phenyl ring thereof, with 1 to 3 substituents selected from the group consisting of nitro, unsubstituted or (C 1-6 )alkyl-substituted amino, phenyl-(C 1-6 )alkoxy, hydroxy, carboxy, phenyl-(C 1-6 )alkoxycarbonyl-(C 1-6 )alkoxy, (C 1-6 )alkanoyloxy, carboxy-(C 1-6 )alkoxy, and (C 1-6 )alkylsubstituted amino-(C 1-6 )alkyl
Claim 5
Dependent Claim
22 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 2, wherein R 1 is a (C 1-6 )alkanoyl group.
Claim 6
Dependent Claim
58 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 2, wherein R 1 is a (C 1-6 )alkoxycarbonyl group, a (C 1-6 )alkoxycarbonyl-(C 1-6 )alkyl group, a phenyl-(C 1-6 )alkyl group which has, on the phenyl ring thereof, 1 to 3 substitutent selected from among (C 1-6 )alkanoyloxy and hydroxy groups, or a naphthoyl group.
Claim 7
Dependent Claim
57 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 3, wherein R 1 is a benzoyl group which is substituted, on the phenyl ring thereof, with 1 to 3 substituents selected from the group consisting of hydroxy, carboxy, unsubstituted or (C 1-6 )alkyl-substituted amino, carboxy-(C 1-6 )alkoxy, and (C 1-6 )alkyl-substituted amino-(C 1-6 )alkyl.
Claim 8
Dependent Claim
21 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 3, wherein R 1 is an unsubstituted benzoyl group.
Claim 9
Dependent Claim
49 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 6, wherein R 1 is a benzoyl group which is substituted, on the phenyl ring thereof, 1 to 2 substituents selected form the group consisting of unsubstituted or (C 1-6 )alkyl-substituted amino, hydroxy, and carboxy-(C 1-6 )alkoxy.
Claim 10
Dependent Claim
22 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 8, wherein R 2 is a 3,4-di(C 1-6 )alkoxybenzoyl group.
Claim 11
Dependent Claim
45 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 9, wherein R 1 is a benzoyl group which is substituted, on the phenyl ring thereof, with one substituent selected form the group consisting of unsubstituted or (C 1-6 )alkyl-substituted amino, and hydroxy.
Claim 12
Dependent Claim
5 words
1-(4-Aminobenzoyl)-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydrocarbostyril according to claim 10.
Claim 13
Dependent Claim
5 words
1-(4-Hydroxybenzoyl)-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydrocarbostyril according to claim 10.
Claim 14
Dependent Claim
5 words
1-Benzxoyl-6-[4-(3,4-dimethoxybenzxoyl)-1-piperazinyl]-3,4-dihydrocarbostyril according to claim 7.
Claim 15
Dependent Claim
5 words
1-(4-Hydroxy-3-dimethylaminomethylbenzxoyl)-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydrocarbostyril according to claim 9.
Claim 16
Dependent Claim
5 words
1-(3-Hydroxy-5-carboxymethoxybenzoyl)-6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydrocarbostyril according to claim 9.
Claim 17
Dependent Claim
25 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 5, wherein R 1 is a (C 1 -C 6 ) alkoxycarbonyl group.
Claim 18
Dependent Claim
77 words
A carbostyril compound of the formula (I): ##STR57## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, with 1 to 2 substituents selected from the group consisting of unsubstituted amino, hydroxy, and carboxy, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 of a lower alkoxy group, and its pharmaceutically acceptable salt.
Claim 19
Dependent Claim
77 words
A carbostyril compound of the formula (I): ##STR57## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, with 1 to 2 substituents selected from the group consisting of unsubstituted amino, hydroxy, and carboxy, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 of a lower alkoxy group, and its pharmaceutically acceptable salt.
Claim 20
Dependent Claim
43 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 17, wherein R 1 is a benzoyl group which is substituted, on the phenyl ring thereof, 1 to 2 substituents selected from the group consisting of unsubstituted amino, hydroxy, and carboxy.
Claim 21
Dependent Claim
41 words
A carbostyril compound or its pharmaceutically acceptable salt as claimed in claim 18, wherein R 1 is a benzoyl group which is substituted, on the phenyl ring thereof, with one substituent selected from the group consisting of unsubstituted amino and hydroxy.
Claim 22
Dependent Claim
132 words
A cardiotonic composition comprising a cardiotonically effective amount of a compound of the formula (I): ##STR58## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenyl-lower alkyl group which has, on the phenyl ring thereof, 1 to 3 substituents selected from among lower alkanoyloxy and hydroxy groups, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, with 1 to 3 substituents selected from the group consisting of nitro, unsubstituted or lower alkyl-substituted amino, phenyl-lower alkoxy, hydroxy, carboxy, phenyl-lower alkoxycarbonyl-lower alkoxy, lower alkanoyloxy, carboxyl-lower alkoxy, and lower alkyl-substituted amino-lower alkyl, or a naphthoyl group, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 lower alkoxy groups, and its pharmaceutically acceptable salt.
Claim 23
Dependent Claim
132 words
A cardiotonic composition comprising a cardiotonically effective amount of a compound of the formula (I): ##STR58## wherein R 1 is a lower alkanoyl group, a lower alkoxycarbonyl group, a lower alkoxycarbonyl-lower alkyl group, a phenyl-lower alkyl group which has, on the phenyl ring thereof, 1 to 3 substituents selected from among lower alkanoyloxy and hydroxy groups, a benzoyl group which may optionally be substituted, on the phenyl ring thereof, with 1 to 3 substituents selected from the group consisting of nitro, unsubstituted or lower alkyl-substituted amino, phenyl-lower alkoxy, hydroxy, carboxy, phenyl-lower alkoxycarbonyl-lower alkoxy, lower alkanoyloxy, carboxyl-lower alkoxy, and lower alkyl-substituted amino-lower alkyl, or a naphthoyl group, R 2 is a benzoyl group which may optionally have, on the phenyl ring thereof, 1 or 2 lower alkoxy groups, and its pharmaceutically acceptable salt.
References Cited (Backward Citations)
US4415572A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-07-26 | 1992-01-25 | 1992-07-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-07-26 | 1996-01-25 | 1996-07-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-07-26 | 2000-01-25 | 2000-07-26 | $7700.00 | Window Closed / Lapsed |