E. R. Squibb Sons, Inc.

Squibb & Sons, Inc.

Zahler, Robert

Jacobs, Glenn A.

Breuer, Hermann

Glenn A Jacobs

Robert Zahler

Frederic P Hauck

Rudiger D Haugwitz

Venkatachala L Narayanan

Hermann Breuer

Gregory S Bisacchi

William H Koster

Antiviral activity is exhibited by compounds having the formula ##STR1## its pharmaceutically acceptable salts thereof wherein R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## and R.sub.1 is either a purine, pyrimidine or an analog thereof.

Purinyl and pyrimidinyl cyclobutanes and their use as antiviral agents

Disclosed are compounds having the formula ##STR1## wherein Prot is a hydroxyl protecting group. The compounds are useful as intermediates in the preparation of compounds of the formula ##STR2## which in turn are useful as antiviral agents.

Purinyl cyclobutanes

Antibacterial activity is exhibited by 2-azetidinones having an acylamino substituent in the 3-position and having an activating group in the 1-position of the formula ##STR1##

1-(substituted phosphorous)-azetidinone antibacterials

Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.3 H group and having in the 3-position an acylamino group of the formula ##STR1##

3-acylamino-2-oxo-1-azetidinesulfonic acids

Acetamide derivatives are provided having the structure ##STR1## wherein X is a single bond, --CH.sub.2 -- or --O--, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, phenyl-lower alkoxy-lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2## may be taken together to form a 5- to 7-membered heterocyclic ring optionally containing one other hetero atom, such as nitrogen, sulfur or oxygen; Y is hydroxyl, OR wherein R is lower alkyl, lower alkenyl or lower alkanoyl, or ##STR3## wherein R.sup.1 and R.sup.2, and R.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached are as defined above, and n is 1 to 6. These compounds are useful as anti-arrhythmia agents and have been found to be effective in the treatment of acute myocardial infarction.

Anti-arrhythmia agents

Morpholinyl acetamide derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl or lower alkanoyl, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2## may be taken together to form a 5- to 7-membered heterocyclic ring optionally containing one other hetero atom, such as nitrogen, sulfur or oxygen; Y is hydroxyl, OR wherein R is as defined above, or ##STR3## wherein R.sup.1 and R.sup.2 and R.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached are as defined above, and n is 1 to 6.

Morpholinyl acetamide derivatives and use thereof

6-[(Aryloxy)methyl]-2-morpholinemethanol derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, or lower alkenyl, and Ar represents a monocyclic or polycyclic aromatic group including tetraindiols and their analogs. These compounds are useful as adrenergic modifiers, particularly in treating arrhythmia.

6-[(Aryloxy)methyl]-2-morpholinemethanol derivatives and use thereof

Isothiocyanobenzoxazoles having the structure ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkoxy, or halogen; X is O or S; R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiamorpholinyl, 4-alkyl-1-piperazinyl, 4-alkyl-1-piperidinyl or 3-alkyl-1-pyrrolidinyl, are useful anthelmintic agents.

Isothiocyanobenzoxazoles

Isothiocyanobenzoxazoles having the structure ##SPC1## Wherein R.sub.1 is hydrogen, alkyl, alkoxy, or halogen; X is O or S; R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiamorpholinyl, 4-alkyl-1-piperazinyl, 4-akyl-1-piperidinyl or 3-alkyl-1-pyrrolidinyl, are useful anthelmintic agents.

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Glenn A Jacobs