Virginia Commonwealth University

Allelix Biopharmaceuticals Inc.

Cambridge Neuroscience, Inc.

Richard A Glennon

Bryan Roth

Ho Law

James B Fischer

Richard C Young

Richard Westkaemper

Spiro&lsqb;9,10-dihydroanthracene&rsqb;-9,3&prime;-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.

Selective serotonin receptor antagonists and therapeutic applications thereof

Compounds which have enhanced affinity and selectivity for 5-HT receptors have been identified. These compounds can be used therapeutically in the treatment of mental disorders via administration in a pharmacologically acceptable delivery route to a patient in need thereof, or can be used to identify antagonists of 5-HT receptors by well known screening methodologies which could themselves be used in the treatment of mental disorders.

Selective 5-HT6 receptor ligands

This invention relates compounds having serotonin receptor binding activity, to pharmaceutical compositions containing them and to their medical use, particularly in the treatment of CNS conditions. Described herein are compounds which have the general formula:

Imidazoles with serotonin receptor binding activity

This invention relates compounds having serotonin receptor binding activity, to pharmaceutical compositions containing them and to their medical use, particularly in the treatment of CNS conditions. Described herein are compounds which have the general formula: ##STR1## wherein R.sup.1 is selected from H, C.sub.1-6 alkyl and benzyl;

Sigma receptor ligands and the use thereof

The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.

This invention relates to compounds having serotonin receptor binding activity and to their medical use, particularly in the treatment of CNS conditions such as migraine. Described herein are compounds which have the general formula: ##STR1## wherein R.sup.1 is selected from a group of Formula i and ii: ##STR2## n is 1-3; R.sup.2 is selected from H and C.sub.1-6 alkyl;

Benzylamidine derivatives with serotonin receptor binding activity

This invention relates to compounds having serotonin receptor binding activity, to pharmaceutical compositions containing them and to their medical use, particularly in the treatment of CNS conditions. Described herein are compounds which have the general formula: ##STR1## wherein R.sup.1 is selected from a group of Formula i and ii: ##STR2## n is 1-3; R.sup.2 is selected from H and C.sub.1-6 alkyl;

Methods of using pharmaceutical tetrahydroisoquinoline compounds for learning and/or memory enhancement, and for treatment of dementia, cocaine dependence, depression, eating disorders, anxiety, or attention deficit disorder with hyperactivity (ADHD).

Methods of using pharmaceutical tetrahydroisoquinolines

Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1D.beta. receptor, of the formula: ##STR1## wherein R.sup.1 is a group selected from aryl-C.sub.1-7 alkyl; aryl-C.sub.2-7 alkoxy; aryl-C.sub.2-7 alkanoyl and aryl-C.sub.1-7 alkanoyloxy, wherein said alkyl, alkoxy, alkanoyl and alkanoyloxy groups are optionally substituted by a C.sub.1-4 alkyl substituent and wherein said aryl group is optionally substituted by one or more substituent selected from hydroxyl, halogen, mercapto, linear or branched C.sub.1-4 alkyl, linear or branched C.sub.1-4 alkoxy, linear or branched C.sub.1-4 alkylthio, thiol substituted C.sub.1-4 alkyl and nitro substituted C.sub.1-4 alkyl;

5-HT-1D receptor ligands

Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1D.beta. receptor, of the formula: ##STR1## wherein R.sup.1 represents a chain selected from C.sub.8-11 alkyl, C.sub.7-10 alkoxy, C.sub.8-11 alkanoyl and C.sub.7-10 alkanoyloxy wherein said chain is optionally substituted by hydroxyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and wherein one of the intervening carbons of said chain is optionally replaced with a heteroatom selected from oxygen, nitrogen and sulfur;

Growing community of inventors

Richmond, VA, United States of America

Richard A Glennon