A. H. Robins Company, Incorporated

Bruce E Tomczuk

Deborah S Sutherland

Chandler R Taylor, Jr

Harold F Stauffer, Jr

This invention provides a 2-arylpyrazolo[1,5-a]pyrimidine-3-acetic acid corresponding to the formula: ##STR1## where X is hydrogen or a halogen, hydroxy, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituent; Y is hydrogen or a halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituent; Z is a hydroxy, C.sub.1 -C.sub.4 alkoxy or --NRR substituent; and R is hydrogen or a C.sub.1 -C.sub.4 alkyl substituent; or a pharmaceutically acceptable salt thereof which is useful as a therapeutic agent which exhibits anxiolytic, anticonvulsant and muscle relaxant effects in a warm blooded animal.

2-phenylpyrazolo[1,5-a]pyrimidine-3-acetic acid derivatives exhibiting

This invention provides novel pyrazole-4-acetic acid derivatives which have utility as therapeutic agents which exhibit anxiolytic, anticonvulsant and muscle relaxant effects in warm blooded animals. Illustrative of an invention compound is 3-(dimethylamino)-5-(4-methylphenyl)-1H-pyrazole-4-acetamide: ##STR1##

3-amino-5-arylpyrazole-4-acetic acid derivatives exhibiting therapeutic

Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar is phenyl, pyrido, thienyl or furanyl; and W forms a wide combination of groups with B, including acids, esters, alcohols, amides and ketones. The compounds have CNS activity in a method for treating a living animal body as muscle relaxants, anticonvulsants and antianxiety agents.

Pharmaceutical method using fused imidazoheterocyclic compounds

Method of treating animals using fused imidazoheterocyclic compounds

Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, di-loweralkylamino or nitro; Ar is phenyl, pyrido, thienyl or furanyl; and W forms a wide combination of groups with B, including acids, esters, alcohols, amides and ketones. The compounds have CNS activity in a method for treating a living animal body as muscle relaxants, anticonvulsants and antianxiety agents.

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Richmond, VA, United States of America

Bruce E Tomczuk