Smithkline Beecham Corporation

Smithkline Corporation

Smithkline Beckman Corporation

Smith Kline & French Laboratories Limited

John J Lafferty

Robert M DeMarinis

Carl Kaiser

William Edward Bondinell

Joseph W Venslavsky

Dinubhai H Shah

Charles L Zirkle

Harlan F Hill

Maxwell Gordon

Alpha-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mammals.

.alpha.-adrenergic receptor antagonists and methods of use thereas

.alpha.-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mannals.

.alpha.-adrenergic receptor antagonists

Alpha-andrenergic receptor antagonists and use thereas

.alpha.-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonist to produce .alpha.-adrenoceptor antagonism in mammals.

N-Substituted pyrrolidineacetic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an esters of an N-unsubstituted pyrrolidineacetic acid followed by hydrolysis of the ester.

N-Substituted pyrrolidineacetic acids and their esters

N-Substituted azaheterocyclic carboxylic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.

Inhibition of GABA uptake by N-substituted azaheterocyclic carboxylic

Tricyclic quinolizidine derivatives administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.

Antipsychotically useful quinolizidylidene derivatives of xanthenes,

Novel piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and dibenzoxepins administered internally to an animal host, in therapeutically effective amounts, produce antipsychotic activity essentially free of extrapyramidal symptoms.

Piperidylidene derivatives of benzo-fused xanthenes, thioxanthenes and

N-Allyl-benzmorphan compounds having structures distinguished by having either a 4,5 or 6 carbon containing allyl group at the 2- or N-position or various ether derivatives of the 2'-hydroxy group. The compounds are prepared by alkylation of appropriate N-nor bases and have analgetic antagonist activity particularly pronounced in countering the effects of overdosing. Certain N-acyl-2'-hydroxy-5,9-dimethyl-6,7-benzmorphan intermediates are also disclosed.

Novel N-allyl and N-propargyl benzmorphan derivatives

.beta.-Naphthylmethyl piperazinyl derivates having anti-Parkinsonism activity prepared by condensation of .beta.-chloromethylnaphthalene with the appropriate substituted piperazine.

Growing community of inventors

Levittown, PA, United States of America

John J Lafferty