Patent US4719223A successfully refreshed from Google Patents.
US4719223A
Expired / Lapsed
US
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Imidazolethiol dopamine-beta-hydroxylase inhibitors
Assignee: SmithKline Beecham Corp
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Filing: 1985-10-31
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Granted: 1988-01-12
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Expires: 2005-10-31
Abstract
Abstract Potent dopamine- beta -hydroxylase inhibitors having the Formula: <IMAGE> which are useful to inhibit dopamine- beta -hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine- beta -hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Inventors
- 👤 Carl Kaiser
- 👤 Lawrence I. Kruse
- 👤 Stephen T. Ross
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 08:32
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/04; C07D233/28; C07D233/30; C07D233/42; C07C; C07C255/00; A; A61; A61P; A61P43/00; A61P9/00; A61P9/08; A61P9/12; C07C335/00; C07C335/04; C07C335/16; C07C335/20; C07D233/54; C07D233/66; C07D233/84
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
43 words
A compound of the Formula: ##STR17## in which: X is hydrogen, bromo, chloro, fluoro, iodo or any combination thereof of up to four substituents; n is 0-5; and R is hydrogen or C 1-4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
Claim 2
Dependent Claim
43 words
A compound of the Formula: ##STR17## in which: X is hydrogen, bromo, chloro, fluoro, iodo or any combination thereof of up to four substituents; n is 0-5; and R is hydrogen or C 1-4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
Claim 3
Dependent Claim
10 words
A compound of claim 1 in which R is hydrogen.
Claim 4
Dependent Claim
10 words
A compound of claim 2 in which n is 1.
Claim 5
Dependent Claim
8 words
A compound of claim 3 that is 1-(4'-amino-3',5'-diclorobenzyl)imidazole-2-thiol.
Claim 6
Dependent Claim
8 words
A compound of claim 3 that is 1-(4'-amino-3',5'-dichlorobenzyl)imidazole-2-thiol.
Claim 7
Dependent Claim
26 words
A pharmaceutical composition for inhibiting dopamine-β-hydroxylase activity, comprising a pharmaceutically acceptable carrier and an amount sufficient to produce said inhibition of a compound of claim 1.
Claim 8
Dependent Claim
12 words
A pharmaceutical composition of claim 6 in which the compound is 1-(4'-amino-3',5'-difluorobenzyl)imidazole-2-thiol.
Claim 9
Dependent Claim
12 words
A pharmaceutical composition of claim 6 in which the compound is 1-(4'-amino-3',5'-dichlorobenzyl)imidazole-2-thiol.
Claim 10
Dependent Claim
14 words
A pharmaceutical composition of claim 6 containing from 1 to 500 mg of compound.
Claim 11
Dependent Claim
29 words
A method of inhibiting dopamine-β-hydroxylase activity in mammals which comprises: administering internally to a subject in need of such inhibition an effective amount of a compound of claim 1.
Claim 12
Dependent Claim
11 words
A method of claim 10 in which the compound is 1-(4'-amino-3',5'-difluorobenzyl)imidazole-2-thiol.
Claim 13
Dependent Claim
11 words
A method of claim 10 in which the compound is 1-(4'-amino-3',5'-dichlorobenzyl)imidazole-2-thiol.
Claim 14
Dependent Claim
23 words
A method of claim 10 that comprises administering an amount selected from the range of 0.1 to 100 mg per kilogram of compound.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-01-11 | 1991-07-13 | 1992-01-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-01-11 | 1995-07-13 | 1996-01-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-01-11 | 1999-07-13 | 2000-01-12 | $7700.00 | Window Closed / Lapsed |