Patent US4056626A successfully refreshed from Google Patents.
US4056626A
Expired / Lapsed
US
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Pharmaceutical composition containing benzofuran derivative
Assignee: Kaken Pharmaceutical Co Ltd
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Filing: 1976-02-27
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Granted: 1977-11-01
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Expires: 1996-02-27
Abstract
Abstract A pharmaceutical composition containing as the essential active ingredient a benzofuran derivative of the formula: <IMAGE> wherein A is -COR', <IMAGE> or ethyl group; B is hydrogen atom when A is -COR' <IMAGE> or -COR'' substituted at the 3 or 4 position of the benzofuran nucleus when A is ethyl; R is an alkyl group having 1 to 5 carbon atoms; R' is an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 3 carbon atoms or phenyl group; R'' is an alkyl group having 1 to 4 carbon atoms, phenyl or phenylalkyl group wherein the alkyl moiety has 1 to 2 carbon atoms; and the substituted propoxy group is at the 3, 4, 5, 6 or 7 position of the benzofuran nucleus; or a pharmaceutically acceptable acid addition salt thereof in admixture with a pharmaceutically acceptable carrier. The pharmaceutical composition possesses a superior beta -adrenergic blocking activity and local anesthetic activity, and is useful for the prevention and treatment of heart diseases, hypertension and hyperthyroidism.
Inventors
- 👤 Kiyoshi Ito
- 👤 Masahiko Ikemoto
- 👤 Kazuhiko Kimura
- 👤 Teruo Nakanishi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 18:01
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/78; C07D307/79; C07D307/80; C07D307/81; C07D307/86
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
157 words
A pharmaceutical composition possessing a β-adrenergic blocking activity and local anesthetic activiy which comprises as the essential active ingredient an effective amount a benzofuran derivative of the formula: ##STR14## wherein A is --COR', ##STR15## or ethyl group; B is hydrogen atom when A is --COR' or ##STR16## or --COR" substituted at the 3 or 4 position of the benzofuran nucleus when A is ethyl; R is an alkyl group having 1 to 5 carbon atoms; R' is an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 3 carbon atoms or phenyl group; R" is an alkyl group having 1 to 4 carbon atoms, phenyl or phenylalkyl group wherein the alkyl moiety has 1 to 2 carbon atoms; and the substituted propoxy group is at the 3, 4, 5, 6 or 7 position of the benzofuran nucleus; or a pharmacetuically acceptable acid addition salt thereof in admixture with a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim
157 words
A pharmaceutical composition possessing a β-adrenergic blocking activity and local anesthetic activiy which comprises as the essential active ingredient an effective amount a benzofuran derivative of the formula: ##STR14## wherein A is --COR', ##STR15## or ethyl group; B is hydrogen atom when A is --COR' or ##STR16## or --COR" substituted at the 3 or 4 position of the benzofuran nucleus when A is ethyl; R is an alkyl group having 1 to 5 carbon atoms; R' is an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 3 carbon atoms or phenyl group; R" is an alkyl group having 1 to 4 carbon atoms, phenyl or phenylalkyl group wherein the alkyl moiety has 1 to 2 carbon atoms; and the substituted propoxy group is at the 3, 4, 5, 6 or 7 position of the benzofuran nucleus; or a pharmacetuically acceptable acid addition salt thereof in admixture with a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim
26 words
The pharmaceutical composition of claim 1, which is employed for treating a disease selected from the group consisting of cardiac arrhythmias, angina pectoris, hypertension and hyperthyroidism.
Claim 4
Dependent Claim
29 words
The pharmaceutical composition of claim 1, which is administered in a dose of 10 to 200 mg./day on the basis of the essential active ingredient for treating cardiac arrhythmias.
Claim 5
Dependent Claim
29 words
The pharmaceutiical composition of claim 1, which is administered in a dose of 10 to 200 mg./day on the basis of the essential active ingredient for treating angina pectoris.
Claim 6
Dependent Claim
28 words
The pharmaceutical composition of claim 1, which is administered in a dose of 30 to 800 mg./day on the basis of the essential active ingredient for treating hypertension.
Claim 7
Dependent Claim
28 words
The pharmaceutical composition of claim 1, which is administered in a dose of 10 to 100 mg./day on the basis of the essential active ingredient for treating hyperthyroidism.
Claim 8
Dependent Claim
22 words
The pharmaceutical composition of claim 1, which is in a preparation form selected from the group consisting of tablet, capsule, powder, granule.
Claim 9
Dependent Claim
23 words
The pharmaceutical composition of claim 1, which is in a preparation form selected from the group consisting of solution, suspension, emulsion and syrup.
Claim 10
Dependent Claim
33 words
The pharmaceutical composition of claim 1, wherein the essential active ingredient is a benzofuran derivative of the formula (I) in which R is a branched alkyl group having 3 to 4 carbon atoms.
Claim 11
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
Claim 12
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-7-(2-hydroxy-3-tert.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 13
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-7-(2-hydroxy-3-sec.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 14
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-carbethoxy-7-(2-hydroxy-3-isopropylaminoproxy)benzofuran or its hydrochloride.
Claim 15
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-benzoyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
Claim 16
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-3-(2-hydroxy-3-tert.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 17
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-4-(2-hydroxy-3-tert.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 18
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-5-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
Claim 19
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-acetyl-6-(2-hydroxy-3-tert.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 20
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-(1-isopropyl-iminoethyl)-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
Claim 21
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-(1-isopropyl-iminoethyl)-4-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
Claim 22
Dependent Claim
17 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-(1-sec.- butyliminoethyl)-7-(2-hydroxy-3-sec.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 23
Dependent Claim
17 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-(1-sec.- butyliminoethyl)-4-(2-hydroxy-3-sec.-butylaminopropoxy)benzofuran or its hydrochloride.
Claim 24
Dependent Claim
16 words
The pharmaceutical composition of claim 9, wherein the essential active ingredient is 2-ethyl-4-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran or its hydrochloride.
References Cited (Backward Citations)
US3590084A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-10-31 | 1981-05-02 | 1981-11-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-10-31 | 1985-05-02 | 1985-11-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-10-31 | 1989-05-02 | 1989-11-01 | $7700.00 | Window Closed / Lapsed |