American Home Products Corporation

Wyeth

Edward J Podlesny

Wayne Everett Childers

Michael G Kelly

Yvette L Palmer

Magid A Abou-Gharbia

Gary Paul Stack

Gan Zhang

Wayne E Childers, Jr

Callain Younghee Kim

Jerome C Wu

Bicyclic amide derivatives of formula (I) or tautomers or pharmaceutically acceptable salts thereof or both are provided: Also provided are processes for preparing the bicyclic amide derivatives as well as pharmaceutical compositions containing the same and therapeutic uses. The bicyclic amide derivatives are useful for treating a variety of conditions associated with the abnormal modulation of one or more Kv1.1 voltage-gated potassium channels.

Bicyclic derivatives that modulate voltage-gated potassium channels and methods of use thereof

This invention relates to compounds which have activity as 5-HTagonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; Ris optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; Ris H or alkyl; Ris H, COR, COOR, and CONRR; Ris H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; Rand Rare H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or Rand Rtaken together may form a 5&#x2013;7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR; when Ror Rare chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C&#x2013;Calkyl group;or an optical isomer; or a pharmaceutically acceptable salt thereof.

Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents

N-substituted imide derivatives with serotonergic activity

This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, cyano, nitro, halo or perhaloalkyl, with the proviso that one of R.sup.1 and R.sup.3 is other than hydrogen; R.sub.2 is alkyl; or a pharmaceutically acceptable salt thereof.

Substituted dibenzo[a,d]cycloheptene NMDA antagonists

The compounds ##STR1## in which R.sub.1 is hydroxy, alkoxy of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino where each alkyl substituent contains 1 to 6 carbon atoms, or alkanoylamino of 2 to 6 carbon atoms;

Serotonergic substituted piperazinyl tetralins

Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 --where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of 3 to 5 carbon atoms; Y is alkylene of 1 to 3 carbon atoms or alkenylene of 2 to 3 carbon atoms; n is one of the integers 0 to 1; m is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; or a pharmaceutically acceptable salt thereof.

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New Tripoli, PA, United States of America

Edward J Podlesny