Merrell Dow Pharmaceuticals

Aventis Pharma Limited

Charlotte L Barney

Donald Paul Matthews

James R McCarthy

James R Mccarthy

Eugene R Wagner

Robert J Broersma

Thomas M Bargar

Marion W Wannamaker

Philippe Bey

The present invention relates to certain novel piperidyl ethers and thioethers which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.

Piperidyl ethers and thioethers as inhibitors of cholesterol biosynthesis

The present invention relates to a group of compounds which are novel substituted alkyl piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.

Substituted alkyl piperidines

This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.

Inhibitors of lysyl oxidase

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 3-aryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.

Pharmaceutically active 3-aryl-2-fluoro-1-olefins

This invention relates to novel 3-heteroaryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.

Pharmaceutically active 3-heteroaryl-2-fluoro-1-olefins

N-(3-Dialkylamino-2-propenylidene)-N-alkylalkanaminium salts substituted in the 2-position with an ether or thioether and having the formula ##STR1## are active as hypoglycemic agents.

Hypoglycemic

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.

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Cincinnati, OH, United States of America

Charlotte L Barney