US4070470A
Expired / Lapsed
US
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Platelet aggregation inhibiting carbostyrils, their compositions and method of use
Assignee: Otsuka Pharmaceutical Co Ltd
•
Filing: 1975-06-19
•
Granted: 1978-01-24
•
Expires: 1995-06-19
Abstract
Abstract Novel benzcycloamide derivatives represented by the general formula, <IMAGE> (I) wherein R1 is hydrogen, C1-4 alkyl, C2-4 alkenyl or aralkyl; B is -CH2-, -CH2-CH2- or -CH=CH-; A is <IMAGE> (wherein R2 and R3 may be the same or different and are respectively hydrogen or C1-4 alkyl) or -CH=CH-; R4 is -OR5 (wherein R5 is hydrogen, C1-8 alkyl, cycloalkyl or aralkyl) or <IMAGE> (wherein R6 and R7 may be the same or different and are respectively hydrogen, C1-4 alkyl or aralkyl or may form together with the nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a nitrogen, oxygen or sulfur atom); and m and n each are zero or a positive integer and m + n is no more than 11.
Inventors
- 👤 Kazuyukip Nakagawa
- 👤 Minoru Uchida
- 👤 Kimiaki Oka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 23:18
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/16; C07D215/20; C07D215/22; C07D215/227; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/32; C07D209/34; C07D215/24; C07D215/26
Claims Analysis
Total Claims: 46
Claim 1
Independent Claim
159 words
A compound of the formula: ##STR131## where R 1 is selected from the group consisting of hydrogen, C 1-4 alkyl, C 2-4 alkenyl, benzyl and phenethyl; B is --CH 2 --CH 2 -- or --CH═CH--; A is --CH═CH-- or ##STR132## wherein R 2 or R 3 may be the same or different and are selected from the group consisting of hydrogen and C 1-4 alkyl; R 4 is --OR 5 , wherein R 5 is selected from the group consisting of hydrogen, C 1-8 alkyl, cyclohexyl, benzyl and phenethyl, or ##STR133## wherein R 6 and R 7 may be the same or different and are selected from the group consisting of hydrogen, C 1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m + n being no more than 11.
Claim 2
Dependent Claim
159 words
A compound of the formula: ##STR131## where R 1 is selected from the group consisting of hydrogen, C 1-4 alkyl, C 2-4 alkenyl, benzyl and phenethyl; B is --CH 2 --CH 2 -- or --CH═CH--; A is --CH═CH-- or ##STR132## wherein R 2 or R 3 may be the same or different and are selected from the group consisting of hydrogen and C 1-4 alkyl; R 4 is --OR 5 , wherein R 5 is selected from the group consisting of hydrogen, C 1-8 alkyl, cyclohexyl, benzyl and phenethyl, or ##STR133## wherein R 6 and R 7 may be the same or different and are selected from the group consisting of hydrogen, C 1-4 alkyl, benzyl, phenethyl and together with the nitrogen atom, a heterocyclic group selected from the group consisting of a piperidino, morpholino, piperazino or thiazolino group; and m and n each are zero or a positive integer with m + n being no more than 11.
Claim 3
Dependent Claim
10 words
A compound according to claim 1 wherein A is ##STR134##
Claim 4
Dependent Claim
13 words
A compound according to claim 2 wherein R 4 is --OR 5 .
Claim 5
Dependent Claim
11 words
A compound according to claim 2 wherein R 4 is ##STR135##
Claim 6
Dependent Claim
10 words
A compound according to claim 1 wherein A is --CH═CH--.
Claim 7
Dependent Claim
13 words
A compound according to claim 5 wherein R 4 is --OR 5 .
Claim 8
Dependent Claim
11 words
A compound according to claim 5 wherein R 4 is ##STR136##
Claim 9
Dependent Claim
21 words
A pharmaceutical composition for inhibiting platelet aggregation which comprises a compound as claimed in claim 1 and a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
56 words
A method for inhibiting platelet aggregation in the blood of a subject which comprises administering to the subject a pharmaceutical composition containing the compound of claim 1 and a pharmaceutically acceptable carrier in a dosage equivalent to about 0.1 mg. to about 100 mg. of said compound per day per kg. of weight of the subject.
Claim 11
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 12
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 13
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl)propoxycarbostyril.
Claim 14
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl)propoxycarbostyril.
Claim 15
Dependent Claim
1 words
5-(3'-Ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 16
Dependent Claim
1 words
5-(3'-Ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 17
Dependent Claim
1 words
5-(3'-Ethoxycarbonyl)propoxycarbostyril.
Claim 18
Dependent Claim
1 words
5-(3'-Ethoxycarbonyl)propoxycarbostyril.
Claim 19
Dependent Claim
1 words
N-Methyl-6-(3'-ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 20
Dependent Claim
1 words
N-Methyl-6-(3'-ethoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 21
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl-2'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 22
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl-2'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 23
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl-3'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 24
Dependent Claim
1 words
6-(3'-Ethoxycarbonyl-3'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 25
Dependent Claim
1 words
6-(2'-Ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 26
Dependent Claim
1 words
6-(2'-Ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 27
Dependent Claim
1 words
6-(4'-n-Pentoxycarbonyl)butoxy-3,4-dihydrocarbostyril.
Claim 28
Dependent Claim
1 words
6-(4'-n-Pentoxycarbonyl)butoxy-3,4-dihydrocarbostyril.
Claim 29
Dependent Claim
1 words
5-(1'-Ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 30
Dependent Claim
1 words
5-(1'-Ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 31
Dependent Claim
1 words
N-Allyl-5-(1'-ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 32
Dependent Claim
1 words
N-Allyl-5-(1'-ethoxycarbonyl)ethoxy-3,4-dihydrocarbostyril.
Claim 33
Dependent Claim
1 words
6-(3'-Carboxy)propoxy-3,4-dihydrocarbostyril.
Claim 34
Dependent Claim
1 words
6-(3'-Carboxy)propoxy-3,4-dihydrocarbostyril.
Claim 35
Dependent Claim
1 words
6-(3'-Isopropoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 36
Dependent Claim
1 words
6-(3'-Isopropoxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 37
Dependent Claim
1 words
5-(3'-Cyclohexyloxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 38
Dependent Claim
1 words
5-(3'-Cyclohexyloxycarbonyl)propoxy-3,4-dihydrocarbostyril.
Claim 39
Dependent Claim
1 words
6-[(3'-Ethoxycarboxy)-2'-]propenyloxy-3,4-dihydrocarbostyril.
Claim 40
Dependent Claim
1 words
6-[(3'-Ethoxycarboxy)-2'-]propenyloxy-3,4-dihydrocarbostyril.
Claim 41
Dependent Claim
1 words
6-(3'-n-Propylcarbamoyl-2'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 42
Dependent Claim
1 words
6-(3'-n-Propylcarbamoyl-2'-methyl)propoxy-3,4-dihydrocarbostyril.
Claim 43
Dependent Claim
1 words
6-(Carbamoyl)methoxy-3,4-dihydrocarbostyril.
Claim 44
Dependent Claim
1 words
6-(Carbamoyl)methoxy-3,4-dihydrocarbostyril.
Claim 45
Dependent Claim
1 words
6-(1'-Carbamoyl)ethoxy-3,4-dihydrocarbostyril.
Claim 46
Dependent Claim
1 words
6-(1'-Carbamoyl)ethoxy-3,4-dihydrocarbostyril.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-01-23 | 1981-07-25 | 1982-01-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-01-23 | 1985-07-25 | 1986-01-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-01-23 | 1989-07-25 | 1990-01-24 | $7700.00 | Window Closed / Lapsed |