Merrell Dow Pharmaceuticals

Thomas M Bargar

James R McCarthy

Robert J Broersma

Lawrence C Creemer

Donald Paul Matthews

Charlotte L Barney

Robert Broersma, Jr

James R Mccarthy

John K Daniel

Robert J Borersma

The present invention relates to allenyl amines, more specifically, .beta.-ethenylidene(substituted) ethanamines, possessing antihypertensive activity, and having the general formula ##STR1## wherein n is the integer 0, 1 or 2; each X independently is a substituent selected from the group consisting of loweralkyl, halo, --O--(loweralkyl), --S--(loweralkyl), --SO--(loweralkyl), --SO.sub.2 --(loweralkyl), CO.sub.2 R and CH.sub.2 OR, wherein R is loweralkyl and each loweralkyl group is from 1 to about 6 carbon atoms, or the pharmaceutically-acceptable addition salts thereof. These compounds are prepared by a novel reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.

Allenyl amines

This invention relates to novel aminoalkyl substituted heterocyclic sulfur compounds which are useful as antihypertensive agents.

Novel aminoalkyl-substituted heterocyclic sulfur compounds

The invention relates to novel aminoalkyl substituted heterocyclic sulfur compounds which are useful as antihypertensive agents.

The present invention relates to compounds which are allenyl amines, more specifically, .beta.-ethenylidene-(substituted)ethanamines, possessing antihypertensive activity. They are prepared by a noval reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.

This invention relates to novel .beta.-methylenethiophenethanamines which are mechanism-based inhibitors of dopamine beta-hydroxylase useful as antihypertensive agents.

Novel allylic amines

This invention relates to novel heterocyclyl-2-propyn-1-amines which are useful as dopamine beta hydroxylase inhibitors in the treatment of hypertension.

Heterocyclyl-2-propyn-1-amines

This invention relates to novel .beta.-methylenefuranethanamines which are mechanism-based inhibitors of dopamine beta-hydroxylase useful as antihypertensive agents.

.beta.-methylene furanethanamines and use as anti-hypertensive agents

2-Phenylpyrano[2,3-b]pyridines are described herein. These compounds are active against a variety of viruses. A number of procedures can be used to prepare the compounds of this invention but, at some point, they would all make use of the cyclization of a (phenyl) (pyridyl)propanol or (phenyl) (pyridyl)propenol.

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Clayton, CA, United States of America

Thomas M Bargar