Merrell Dow Pharmaceuticals

Merrell Pharmaceuticals, Inc.

Ronald C Bernotas

Albert A Carr

Craig E Thomas

George Ku

Jeffrey S Sprouse

Ian A McDonald

Mark W Dudley

Hsien C Cheng

The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Cyclic nitrones

The present invention is directed to a new class of serotonin 5HT.sub.1A agonists.

Serotonin 5HT.sub.1A agonistic method

Cyclic nitrone compounds useful in treating stroke

The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.sub.4 or --NR.sub.4 R.sub.5 in which R.sub.4 and R.sub.5 are each independently hydrogen or C.sub.1-4 alkyl; and the pharmaceutically acceptable addition salts thereof; with the proviso that when n is O or X is --CH=CHX.sub.1, then X.sub.1 is not OH, OR.sub.2, or NR.sub.2 R.sub.3 ; that are serotonin 5HT.sub.1A and 5HT.sub.1D receptor agents.

Serotonin receptor agents

1,4 benzodioxin derivatives and their use as serotonin 5HT.sub.1A

Cyclic nitrones, pharmaceutical compositions thereof and their use in

Serotonin 5HT.sub.1A agonists

Growing community of inventors

Cincinnati, OH, United States of America

Ronald C Bernotas