Ortho Pharmaceutical Corporation

American Cyanamid Company

Jeffery B Press

Pauline J Sanfilippo

Ramesh M Kanojia

Zoltan G Hajos

Robert Falotico

James J McNally

William B Wright, Jr

Sidney Robert Safir

Ronald K Russell

Maud Urbanski

Andrew S Tomcufcik

Victor T Bandurco

Alfonso J Tobia

Robert A Mallory

Joseph W Marsico, Jr

Corris M Hofmann

O William Lever, Jr

Jerry R Roberts

A process for the preparation of enantiomerically pure thienopyran derivatives of the formula ##STR1## is described. The thienopyran derivatives are relaxants of smooth muscle tone and as such are useful in vascular tissue for the treatment of hypertension disease, angina and other vascular disorders characterized by poor regional perfusion.

Process for the preparation of enantiomerically pure thienopyran

Substituted thienopyrans and processes for preparing the thienopyrans are disclosed. The thienopyrans are useful as antihypertensive agents; antianginals are peripheral antivasoconstrictive agents.

Substituted thienopyrans as antihypertensive agents

Novel 6-substituted purinyl piperazine derivatives are described. The novel derivatives are useful as cardiotonic agents and antiarrhythmic agents.

6-substituted purinyl piperazine derivatives

Novel substituted biphenylalkoxyamines and their synthesis are described. These novel compounds possess antimicrobial activity against yeasts and molds, and also have anticonvulsant and antisecretory properties. The compounds are useful for the treatment of yeast and mold infections in mammals, as well as the treatment of seizures and gastrointestinal diseases in mammals.

Substituted biphenylalkoxyamines

6-substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

##STR1## Novel tetrahydropyrido[4,3-d]pyrimidines and their synthesis are described. These compounds are useful for the treatment of gastrointestinal diseases, and are particularly useful as cytoprotective agents to prevent ulcer formation.

4-phenyl tetrahydropyrido(4,3-d)pyrimidines

Novel substituted imidazole and pyridine derivatives and their synthesis are disclosed. The derivatives inhibit the enzyme, H.sup.+ /K.sup.+ ATPase, and are therefore useful for the treatment of gastrointestinal diseases.

Substituted imidazole and pyridine derivatives

Substituted thienopyrans

6-Substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

4-Substituted pyrazolo[3,4-d]pyrimidine derivatives and a method of synthesis for the derivatives are described. The 4-substituted pyrazolopyrimidine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

4-substituted pyrazolo[3,4-d]pyrimidine derivatives

4-Substituted pyrazolo[3,4-d]pyrimidine derivatives and a method of synthesis for the derivatives are described. The 4-substituted pyrazolopyrimidine derivatives are useful as cardiotonic agents and antiarryhythmic agents.

4-Substituted pyrazolo[3,4-D]pyrimidine derivatives

O-functional derivatives of substituted isoquinolin-3-ol compounds of the general formula ##STR1## that exhibit cardiotonic and/or phosphodiesterase fraction III inhibiting properties and/or renal vasodilating are pharmacologically active in the treatment of cardiac conditions. Methods for synthesizing and using the compounds are described.

O-functionalized derivatives of substituted isoquinolin-3-ols having

Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.

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Rocky Hill, NJ, United States of America

Jeffery B Press