Smithkline Beckman Corporation

Smithkline Beecham Corporation

Thomas B Leonard

Lawrence I Kruse

Joseph A Finkelstein

Carl Kaiser

Stephen T Ross

James S Frazee

Potent DBH inhibitors having the formula ##STR1## can be used to inhibit DBH activity in mammals.

Dopamine-.beta.-hydroxylase inhibitors

Disclosed are novel substituted 3-aralkylimidazolines 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.

1-aralkyl-2-mercaptoimidazolines as DBH inhibitors

Potent dopamine-.beta.-hydroxylase inhibitors having the formula ##STR1## that 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.

2-(N-Phenylakyl-N-formyl)amino-3-hydroxy-2-propenoic acids are intermediates for mercaptoimidazolecarboxylic acids which are dopamine-.beta.-hydroxylase inhibitors.

Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that 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.

Growing community of inventors

Haverford, PA, United States of America

Thomas B Leonard