US4011319A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical compositions and methods involving benzazepine derivatives
Assignee: GlaxoSmithKline LLC
•
Filing: 1975-07-02
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Granted: 1977-03-08
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Expires: 1995-07-02
Abstract
Abstract Pharmaceutical compositions and a method of stimulating peripheral dopamine receptors by administering internally a nontoxic effective quantity of a benzazepine derivative to an animal. Renal vasodilator and diuretic methods are also disclosed.
Inventors
- 👤 Carl Kaiser
- 👤 Robert G. Pendleton
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 22:23
CPC Classifications
C; C07; C07D; C07D223/00; C07D223/14; C07D223/16; A; A61; A61P; A61P25/00
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
116 words
A method of stimulating peripheral dopamine receptors in an animal requiring stimulation of said peripheral dopamine receptors which comprises administering internally to said animal a nontoxic amount sufficient to stimulate said peripheral dopamine receptors of a compound of the formula: ##STR3## in which: R is hydrogen, methyl, hydroxyethyl or n-butyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 2 is hydroxy, methoxy, ethoxy or alkanoyloxy, in the 8-or 9-position; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
Claim 2
Independent Claim
116 words
A method of stimulating peripheral dopamine receptors in an animal requiring stimulation of said peripheral dopamine receptors which comprises administering internally to said animal a nontoxic amount sufficient to stimulate said peripheral dopamine receptors of a compound of the formula: ##STR3## in which: R is hydrogen, methyl, hydroxyethyl or n-butyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 2 is hydroxy, methoxy, ethoxy or alkanoyloxy, in the 8-or 9-position; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
Claim 3
Dependent Claim
32 words
The method of claim 1 in which R and R 4 are hydrogen, R 1 and R 2 are hydroxy, and R 3 is hydrogen or a meta-or para-substituent as defined above.
Claim 4
Dependent Claim
19 words
The method of claim 2 in which R 1 and R 2 are 7,8-dihydroxy and R 3 is hydrogen.
Claim 5
Dependent Claim
17 words
The method of claim 3 in which the compound is in the form of a free base.
Claim 6
Dependent Claim
17 words
The method of claim 3 in which the compound is in the form of a hydrobromide salt.
Claim 7
Dependent Claim
20 words
The method of claim 1 in which the active ingredient is administered with a pharmaceutical carrier in dosage unit form.
Claim 8
Dependent Claim
11 words
The method of claim 6 in which the administration is orally.
Claim 9
Dependent Claim
19 words
The method of claim 1 in which the active ingredient is administered with a pharmaceutical carrier by intravenous infusion.
Claim 10
Dependent Claim
27 words
The method of claim 1 in which a daily dosage selected from the range of about 60 mg. to about 3000 mg. of active ingredient is administered.
Claim 11
Dependent Claim
33 words
The method of claim 6 in which dosage units containing an active but nontoxic amount selected from about 20 mg. to about 1000 mg. of active ingredient are administered three times a day.
Claim 12
Dependent Claim
36 words
The method of claim 8 in which a total dose selected from the range of about 0.5 mg. to about 50 mg. of active ingredient is administered over a period of from 10 to 30 minutes.
Claim 13
Independent Claim
98 words
A method of producing renal vasodilator activity in an aminal requiring said activity which comprises administering internally to said animal a nontoxic amount sufficient to produce said activity of a compound of the formula: ##STR4## in which: R is hydrogen, methyl, hydroxyethyl or n-butyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
Claim 14
Independent Claim
98 words
A method of producing renal vasodilator activity in an aminal requiring said activity which comprises administering internally to said animal a nontoxic amount sufficient to produce said activity of a compound of the formula: ##STR4## in which: R is hydrogen, methyl, hydroxyethyl or n-butyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
Claim 15
Independent Claim
120 words
A method of producing diuretic activity in an aminal requiring said activity which comprises administering internally to said animal a nontoxic amount sufficient to produce said activity of a compound of the formula: ##STR5## in which: R is hydrogen, methyl or hydroxyethyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 2 is hydroxy, methoxy, ethoxy or alkanoyloxy, in the 8-or 9-position, provided that R 1 and R 2 are not 8,9-dihydroxy or 8,9-dialkanoyloxy; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
Claim 16
Independent Claim
120 words
A method of producing diuretic activity in an aminal requiring said activity which comprises administering internally to said animal a nontoxic amount sufficient to produce said activity of a compound of the formula: ##STR5## in which: R is hydrogen, methyl or hydroxyethyl; R 1 is hydrogen, hydroxy, methoxy, ethoxy or alkanoyloxy, in the 7-, 8-or 9-position; R 2 is hydroxy, methoxy, ethoxy or alkanoyloxy, in the 8-or 9-position, provided that R 1 and R 2 are not 8,9-dihydroxy or 8,9-dialkanoyloxy; R 3 is hydrogen, chloro, bromo, fluoro, methyl, hydroxy or methoxy; R 4 is hydrogen or methyl; and said alkanoyl moieties have from 2 to 5 carbon atoms, or a pharmaceutically acceptable acid addition or quaternary salt of said compound.
References Cited (Backward Citations)
US3393192A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-03-07 | 1980-09-06 | 1981-03-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-03-07 | 1984-09-06 | 1985-03-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-03-07 | 1988-09-06 | 1989-03-08 | $7700.00 | Window Closed / Lapsed |