Ortho-mcneil Pharmaceutical Corp.

Mcneil Ab

Other

Ortho Pharmaceutical Corporation

Samuel O Nortey

Bruce E Maryanoff

Allen B Reitz

David F McComsey

James J McNally

Pauline J Sanfilippo

Malcolm K Scott

Winston Z Ho

Ellen W Baxter

Michael J Costenzo

Benzamidine derivativesare useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Benzamidine derivatives

C-6 ring-substituted pyrido&lsqb;1,2-a&rsqb;benzimidazole derivatives useful in treating central nervous system disorders

This invention relates to a series of substituted 3-oxo-pyrrolo[1,2-a]imidazopyridine derivatives of the formula 1 ##STR1## where X.sub.1 -X.sub.4, R.sub.1, R.sub.2 and Ar are defined herein. In addition the invention relates to pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are ligands for the benzodiazepine site on the GABA-A receptor and display anxiolytic and anticonvulsant activity in animal models.

Heterocyclic derivatives useful in treating central nervous system

A compound of the general formula I; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.

2-oxo-pyrrolo[1,2-A]benzimidazole-3-carboxyl derivatives useful in

A compound of the general formula I: ##STR1## is disclosed as a potent anticonvulsant drug. Pharmaceutical compositions and methods of treatment are also disclosed.

Anticonvulsant pseudofructopyranose sulfamates

Sulfamates of the following formula (I) are anticonvulsants and are useful in the treatment of epilepsy: ##STR1## wherein R is one or more substituents such as alkyl, halo, alkoxy, CH.sub.3 or nitro; and

Anticonvulsant phenethyl sulfamates

Sulfamates of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.

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LaMott, PA, United States of America

Samuel O Nortey