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Serving leading biopharmaceutical companies globally:

Citi
McKesson
US Army
AstraZeneca
Harvard Business School
US Department of Justice
Moodys
Cerilliant
Covington
Argus Health

Generated: November 22, 2017

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Title: 3-aralkyl-2-mercaptoyridines as dopamine-.beta.-hydroxylase inhibitors
Abstract:Disclosed are novel substituted 3-aralkyl-2-mercaptopyridines of the structure: ##STR1## processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy in particular as dopamine-.beta.-hydroxylase inhibitors.
Inventor(s): Kruse; Lawrence I. (Hertfordshire, GB2), Ross; Stephen T. (Berwyn, PA)
Assignee: SmithKline Beckman Corporation (Philadelphia, PA)
Filing Date:Sep 17, 1987
Application Number:07/097,988
Claims:1. A compound of structure (I): ##STR12## in which: X.sup.1 to X.sup.5 are hydrogen, halogen, hydroxy, or C.sub.1-4 alkoxy;

n is 1 to 5; and

R is hydrogen or C.sub.1-4 alkyl; or a pharmaceutically acceptable salt thereof.

2. A compound as claimed in claim 1 in which n is 1 or 3, X.sup.1, X.sup.3, and X.sup.5 are hydrogen and X.sup.2 and X.sup.4 are both halogen.

3. A compound as claimed in claim 1 which is 3-(3,5-difluorobenzyl)-2-mercaptopyridine.

4. A compound as claimed in claim 1 which is:

3-(3-fluorobenzyl)-2-mercaptopyridine;

3-benzyl-2-mercaptopyridine;

3(3,5-difluorophenylpropyl)-2-mercaptopyridine;

3-(3-fluorophenylpropyl)-2-mercaptopyridine; or

3-(phenylpropyl)-2-mercaptopyridine.

5. A pharmaceutical composition for inhibiting dopamine-.beta.-hyroxylase activity comprising an effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

6. A pharmaceutical composition of claim 5 wherein the compound is 3-(3,5-difluorobenzyl)-2-mercaptopyridine.

7. A pharmaceutical composition of claim 5 wherein the compound is:

3-(3-fluorobenzyl)-2-mercaptopyridine;

3-benzyl-2-mercaptopyridine;

3-(3,5-difluorophenylpropyl)-2-mercaptopyridine;

3-(3-fluorophenylpropyl)-2-mercaptopyridine; or

3-(phenylpropyl)-2-mercaptopyridine.

8. A method of inhibiting DBH activity which comprises administering to a mammal in need thereof an effective amount of a compound as claimed in claim 1.

9. A method of claim 8 wherein the compound is 3-(3,5-difluorobenzyl)-2-mercaptopyridine.

10. A method of claim 8 wherein the compound is:

3-(3-fluorobenzyl)-2-mercaptopyridine;

3-benzyl-2-mercaptopyridine;

3-(3,5-difluorophenylpropyl)-2-mercaptopyridine;

3-(3-fluorophenylpropyl)-2-mercaptopyridine; or

3-(phenylpropyl)-2-mercaptopyridine.
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Serving leading biopharmaceutical companies globally:

Moodys
Queensland Health
Cerilliant
Colorcon
QuintilesIMS
Harvard Business School
Farmers Insurance
UBS
US Army
Chubb

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