E. R. Squibb Sons, Inc.

Sam T Chao

Ravi K Varma

Eric M Gordon

Jeffrey O Saunders

Christopher M Cimarusti

Dinos P Santafianos

##STR1## and pharmaceutically acceptable salts thereof possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula,

Sulfur-substituted mevinic acid derivatives

Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; and R.sup.2 is hydrogen, alkyl, ammonium, or alkali metal.

6-.alpha.-hydroxy derivatives of mevinic acids

Compounds of the formula ##STR1## and pharmaceutically acceptable salts and tautomeric mixtures thereof possess activity as HMg-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula,

Fluorinated derivatives of mevinic acids

Antihypercholesterolemic activity has been discovered in compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein: Z is ##STR2## X is lower alkyl, lower alkenyl, or lower alkenyl; R.sup.1 is hydrogen, alkyl, alkenyl, aryl, alkylaryl, or substituted aryl having one or more substituents; and

2-pyrrolidone substituted dihydroxy alkanoic, alkenoic and alkynoic

7-Oxabicyclo(2.2.1)heptane-based N-hydroxy-N-alkyl (or aryl) ureas, carbamic acids and carbamothioic acids are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, aryl or aralkyl; R.sub.2 is hydrogen, lower alkyl, aralkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is oxygen, sulfur or NH; n is an integer from 1 to 8; and all stereoisomers thereof. These new compounds have been found to simultaneously inhibit the enzymes arachidonic acid cyclooxygenase and arachidonic acid 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.

7-oxabicyclo(2.2.1)heptane-based derivatives useful as antiinflammatory,

Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a 6-dehydro derivative of a 3-oxo-4,5-dehydro steroid intended for radioimmunoassay, said steroid being saturated in the 1,2-position; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4; and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays. The unlabeled analogs can be coupled with an immunogenic carrier and used to induce antibody formation in animals.

Steroid derivatives and their use in radioimmunoassays

Steroidal-17-spiro-dihydrofuranones, i.e., steroid having in the 17-position a group having the partial structural formula ##STR1## wherein R.sub.1 is bromine, chlorine, or fluorine; R.sub.2 is alkyl, aryl, or arylalkyl; R.sub.3 is hydrogen, .alpha.-methyl, .beta.-methyl, hydroxy or a conventional hydrolyzable ester thereof, have topical antiinflammatory activity.

Steroidal-17-spiro-dihydrofuranones

Steroids having the formula ##STR1## wherein X is -S-, ##STR2## R.sub.1 is alkyl, aryl or acyloxyalkyl; R.sub.2 is carbonyl or .beta.-hydroxymethylene; R.sub.3 is hydrogen or halogen; R.sub.4 is hydrogen, fluorine or methyl; R.sub.5 is hydrogen or alkyl; and R.sub.6 and R.sub.7 are the same or different and are hydrogen, halogen, alkyl or alkoxy, or R.sub.6 and R.sub.7 together with the benzene ring to which they are attached form a naphthalene group; can be used as antiinflammatory agents.

17-Alkylthio (and arylthio)

A series of novel steroidal[ 16.alpha., 17-d]cyclohexenes having a 9-fluoro group is disclosed herein for use as anti-inflammatory agents.

Growing community of inventors

East Windsor, NJ, United States of America

Sam T Chao