Merck + Co., Inc.

William A Bolhofer

Jacob M Hoffman, Jr

Edward J Cragoe, Jr

John D Prugh

John J Baldwin

William C Lumma, Jr

Adolph M Pietruszkiewicz

Novel amino-phenyl-thiadiazoledioxides and related compounds and processes for preparing such compounds are disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.

Amino-phenyl-thiadiazoledioxides as gastric secretion inhibitors

There are disclosed novel compounds described as aminoalkyl pyridine derivatives in which the aminoalkyl pyridine is connected to a guanidine moiety or a functional equivalent thereof, either directly or through a linear connecting group. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastirc acid secretions in mammals and compositions for such uses are also disclosed.

Aminoalkyl pyridine derivatives

There are disclosed novel substituted pyridopyrimidine compounds and processes for preparing such compounds. These compounds are useful as gastric secretion inhibitors in mammals.

Substituted pyridopyrimidines as gastric secretion inhibitors

Heterocyclic carbamates are disclosed which have potent gastric secretion inhibitory properties. The heterocyclic substituent is a pyridyl group or a 6-membered heterocycle with two nitrogen heteroatoms, which may be optionally substituted. Further substituents on the carbamate nitrogen and oxygen atoms are also disclosed. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Suppression of gastric acid secretion using pyrimidylcarbamates

Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a heterocyclic ring which may be substituted with one or more loweralkyl groups. The urea is also substituted with loweralkyl and a lower-alkylamino loweralkyl group. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Imidazole or imidazoline substituted ureas

Substituted ureas and processes for their preparation

Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Substituted naphthyridinones and processes for their preparations

Heterocyclic carbamates

There are disclosed novel compounds described as imidazole cyanoguanidines in which the imidazole moiety is connected to the cyanoguanidine moiety through a cyclic group which may optionally contain one or two alkylene linkages. The cyclic groups may be phenyl, cyclohexyl, thienyl and the like. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretion in mammals, and compositions for such uses are also disclosed.

Cyclic imidazole cyanoguanidines

Organic chemical compounds based upon the urea molecule are disclosed which have potent gastric secretion inhibitory properties. The urea is substituted with a 6 membered heterocyclic substituent containing 2 or 3 heteroatoms, and also with a substituted amino alkyl group. Further substitution is also possible. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.

Pyrazine substituted ureas

Compounds of the formula ##STR1## have been found to inhibit gastric secretion in mammalian species.

Pyridinyl ureas and pharmaceutical use

N-pyrimidinyl-N-dialkylaminoalkyl ureas

Substituted naphthyridinones

N-(Sulfo-lower alkyl)amides of (3-trifluoromethylphenoxy)-(4-chlorophenyl)acetic acid which are useful in the treatment of atherosclerosis. The N-(sulfo-lower alkyl)amides of (3-trifluoromethylphenoxy) (4-chlorophenyl)-acetic acid are prepared by reacting a (3-trifluoromethylphenoxy) (4-chlorophenyl)acetyl halide with an amino-lower alkanesulfonic acid.

N-(Sulfo-lower alkyl) amides of (3-trifluoromethylphenoxy)

[.alpha.-(3-Trifluoromethylphenoxy)-4-chlorobenzyl heterocycles which are prepared by the cyclization of an appropriately substituted [.alpha.(3-trifluoromethylphenoxy)-4-chlorobenzyl]compound. The products reduce the concentration of cholesterol, trigylcerides and other lipids in blood serum and are therefore useful in the treatment of atherosclerosis.

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Frederick, PA, United States of America

William A Bolhofer