Patent US4320134A successfully refreshed from Google Patents.
US4320134A
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Inhibiton of thromboxane synthetase with 1-substituted imidazole compounds
Assignee: Kissei Pharmaceutical Co Ltd
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Filing: 1979-02-21
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Granted: 1982-03-16
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Expires: 1999-02-21
Abstract
Abstract The imidazole compounds of the general formula (I): ##STR1## wherein Y is a carboxyl group, a hydroxymethyl group, an N-di or -mono alkyl substituted or unsubstituted carbamoyl group, a cyano group, or an N-di or -mono alkyl substituted or unsubstituted aminomethyl group, and n is an integer of 3 to 20; and pharmaceutically acceptable salts thereof. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.
Inventors
- 👤 Kinji Iizuka
- 👤 Kenji Akahane
- 👤 Yukio Kamijo
- 👤 Denichi Momose
- 👤 Yukiyoshi Ajisawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 04:24
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
25 words
A compound of the formula: ##STR13## wherein Y is carboxyl, and n is an integer of 6 to 9 or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
25 words
A compound of the formula: ##STR13## wherein Y is carboxyl, and n is an integer of 6 to 9 or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
9 words
The compound of claim 1, wherein n is 6.
Claim 4
Dependent Claim
9 words
The compound of claim 1, wherein n is 7.
Claim 5
Dependent Claim
9 words
The compound of claim 1, wherein n is 8.
Claim 6
Dependent Claim
9 words
The compound of claim 1, wherein n is 9.
Claim 7
Dependent Claim
35 words
A pharmaceutical composition comprising a compound of claim 1 as an active ingredient in an amount effective for the treatment of a disease caused by thromboxane A 2 and a pharmaceutically acceptable carrier or diluent.
Claim 8
Dependent Claim
29 words
The pharmaceutical composition of claim 6 wherein the compound of claim 1 is present in an amount effective for the treatment of inflammation, hypertension, thrombus, cerebral apoplexy or asthma.
Claim 9
Dependent Claim
14 words
The pharmaceutical composition of claim 6 or 7 wherein said active ingredient is 1-(7-carboxyheptyl)-imidazole.
Claim 10
Independent Claim
79 words
A method for treating inflammation comprising administering a therapeutically effective amount of a compound of the formula: ##STR14## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 11
Independent Claim
79 words
A method for treating inflammation comprising administering a therapeutically effective amount of a compound of the formula: ##STR14## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 12
Independent Claim
79 words
A method for treating hypertension comprising administering a therapeutically effective amount of a compound of the formula: ##STR15## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 13
Independent Claim
79 words
A method for treating hypertension comprising administering a therapeutically effective amount of a compound of the formula: ##STR15## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 14
Independent Claim
79 words
A method for treating thrombus comprising administering a therapeutically effective amount of a compound of the formula: ##STR16## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 15
Independent Claim
79 words
A method for treating thrombus comprising administering a therapeutically effective amount of a compound of the formula: ##STR16## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 16
Independent Claim
80 words
A method for treating cerebral apoplexy comprising administering a therapeutically effective amount of a compound of the formula: ##STR17## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 17
Independent Claim
80 words
A method for treating cerebral apoplexy comprising administering a therapeutically effective amount of a compound of the formula: ##STR17## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 18
Independent Claim
79 words
A method for treating asthma comprising administering a therapeutically effective amount of a compound of the formula: ##STR18## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 19
Independent Claim
79 words
A method for treating asthma comprising administering a therapeutically effective amount of a compound of the formula: ##STR18## to a subject afflicted with the same, wherein Y is carboxyl, hydroxymethyl, N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted carbamoyl, cyano or N-di or -mono straight or branched chain C 1 -C 4 alkyl substituted or unsubstituted aminomethyl, and n is an integer of 3 to 20, or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
15 words
The method of claim 9, 10, 11, 12 or 13 wherein said compound is 1-(7-carboxyheptyl)-imidazole.
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) | 1985-03-15 | 1985-09-14 | 1986-03-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-03-15 | 1989-09-14 | 1990-03-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-03-15 | 1993-09-14 | 1994-03-16 | $7700.00 | Window Closed / Lapsed |