E. R. Squibb Sons, Inc.

Peter C Wade

B Richard Vogt

Berthold Richard Vogt

Thomas P Kissick

John Krapcho

Rudiger D Haugwitz

Miguel A Ondetti

Frank L Weisenborn

Jack Bernstein

Barbara V Maurer

Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.

Imido, amido and amino derivatives of mercaptoacyl prolines and

Carbinolamine esters of 1,2,4-triazoles are provided having the structure ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 are as defined herein. These compounds are useful as antiinflammatory agents.

Antiinflammatory carbinolamine esters of 1,2,4-triazoles

Phenylguanidine derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, phenyl, phenylalkyl, phenoxy, phenylalkoxy, lower alkoxyalkyl, phenoxyalkyl, alkylamino, dialkylaminoalkyl, alkylthio, phenylthio, phenylthioalkyl, and alkylthioalkyl; R.sup.1 is lower alkyl or benzyl; R.sup.2 is hydrogen, lower alkoxy carbonyl, and lower alkanoyl; R.sup.3 is lower alkyl, cycloalkylalkyl, lower alkenyl, lower alkynyl or benzyl; and n is 0 or 1. These compounds are useful as anthelmintic agents.

Substituted phenylguanindines and method

New indolylalkyl esters of mercaptoalkanoic acids, and salts thereof, which have the general formula ##STR1## are useful as hypotensive agents.

Indolylalkyl esters of mercaptoalkanoic acids

Imidazolo-pyridine derivatives are provided having the structure ##STR1## wherein R is lower alkyl, lower alkenylalkyl, lower alkynylalkyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl or phenylalkyl and R.sup.1 is lower alkyl, phenylalkyl or di-lower alkylaminoalkyl and n is 0, 1 or 2. These compounds are useful as anthelmintic agents administered orally or parenterally.

Substituted imidazolo-pyridines and method

Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.

Substituted hydrazino derivatives of benzisothiazole-1,1-dioxides

Substituted 2,3-naphthimidazole carbamates are provided having the structure ##STR1## wherein R is lower alkyl, R.sup.1 is hydrogen, halogen or ##STR2## and R.sup.2 is lower alkyl, CH.sub.2 -lower alkenyl, CH.sub.2 -lower alkynyl, phenyl or phenyl substituted with halogen, lower alkoxy, cyano, lower alkyl or trifluoromethyl, and n is 0, 1 or 2. These compounds are useful as anthelmintics. In addition, intermediates and a method of use are also provided.

Substituted 2,3-naphthimidazole carbamates and method

Compounds of the following formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio, nitro, cyano, and trifluoromethyl, and R is selected from a triacetyl substituted pentose, pentose, a tetraacetyl substituted hexose, hexose, a hydroxy substituted cycloalkyl of 5 to 7 carbons, ##STR2## wherein n is 1 or 2 and R.sup.3 is hydrogen, an alkali metal or alkaline earth metal ion; are disclosed. These compounds possess useful anti-inflammatory activity.

2-Substituted-1H-benz[de]-isoquinoline-1,3(2H)-diones

Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, alkyl, alkoxy or nitro; R.sub.2 is hydrogen, halogen or alkoxy; and R.sub.3 is alkoxycarbonyl, ##STR2## pyridinylcarbonyl, pyrimidinylcarbonyl, or pyrazinylcarbonyl; have antiinflammatory activity.

3-(Substituted hydrazino)benzisothiazole-1,1-dioxides

Benzisothiazolines having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkoxy, halogen or nitro;

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Pennington, NJ, United States of America

Peter C Wade