US4882348A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-(aminoalkylthio)imidazoles as dopamine-β-hydroxylase inhibitors
Assignee: SmithKline Beecham Corp
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Filing: 1987-12-29
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Granted: 1989-11-21
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Expires: 2007-12-29
Abstract
Abstract Potent dopamine-β-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-β-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-β-hydroxylase activity in mannals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.
Inventors
- 👤 Lawrence I. Kruse
- 👤 Stephen T. Ross
- 👤 Eliot H. Ohlstein
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 07:00
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/66; C07D233/84; A; A61; A61P; A61P9/00; A61P9/12
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
105 words
Compound of the formula: ##STR7## in which: X is H. F, Cl, Br. I,C 1-4 alkyl, CN, NO 2 , SO 2 NH 2 , COOH, OH, CHO, C 1-4 alkoxy, CH 2 OH, CH 2 OC l-4 alkyl, CF 3 , C 2 F 5 , C 3 F 7 , SO 2 CH 3 , SO 2 CF 3 , or CO 2 C a H 2a+1 wherein a is 1-5, or any accessible combination thereof of up to 5 substituents; n is 1-5; m is 2-5; and R 1 and R 2 are H or a pharmaceutically acceptable salt or hydrate thereof.
Claim 2
Dependent Claim
105 words
Compound of the formula: ##STR7## in which: X is H. F, Cl, Br. I,C 1-4 alkyl, CN, NO 2 , SO 2 NH 2 , COOH, OH, CHO, C 1-4 alkoxy, CH 2 OH, CH 2 OC l-4 alkyl, CF 3 , C 2 F 5 , C 3 F 7 , SO 2 CH 3 , SO 2 CF 3 , or CO 2 C a H 2a+1 wherein a is 1-5, or any accessible combination thereof of up to 5 substituents; n is 1-5; m is 2-5; and R 1 and R 2 are H or a pharmaceutically acceptable salt or hydrate thereof.
Claim 3
Dependent Claim
9 words
A compound of claim 1 wherein n is 1.
Claim 4
Dependent Claim
9 words
A compound of claim 2 wherein m is 2.
Claim 5
Dependent Claim
11 words
A compound of claim 1 that is 2-(2-aminoethylthio)-1-(3,5-difluorobenzyl)imidazole or its dihydrochloride.
Claim 6
Dependent Claim
21 words
A pharmaceutical composition having dopamine-β-hydroxylase inhibiting activity comprising a pharmaceutical carrier and an effective amount of a compound of claim 1.
Claim 7
Dependent Claim
11 words
A composition of claim 5 in which the compound is 2-(2-aminoethylthio)-l-(3,5-difluorobenzyl)imidazole.
Claim 8
Dependent Claim
20 words
A method of inhibiting dopamine-β-hydroxylase activity in mammals that comprises administering an effective amount of a compound of claim 1.
Claim 9
Dependent Claim
11 words
The method of claim 7 in which the compound is 2-(2-aminoethylthio)-1-(3,5-difluorobenzyl)imidazole.
Claim 10
Dependent Claim
20 words
A method of reducing blood pressure in mammals that comprises administering an effective amount of a compound of claim 1.
References Cited (Backward Citations)
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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) | 1992-11-20 | 1993-05-22 | 1993-11-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-11-20 | 1997-05-22 | 1997-11-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-11-20 | 2001-05-22 | 2001-11-21 | $7700.00 | Window Closed / Lapsed |