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US4882348A Expired / Lapsed US ⏱️ 0.0 years remaining

2-(aminoalkylthio)imidazoles as dopamine-β-hydroxylase inhibitors

Assignee: SmithKline Beecham Corp
•
Filing: 1987-12-29
•
Granted: 1989-11-21
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Expires: 2007-12-29
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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 07:14
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)

US3334112A Cited
GB1155580A Cited
US3488423A Cited
EP0125033A1 Cited
US4532331A Cited
US4600430A Cited

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

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