Lilly Industries, Inc.

Eli Lilly and Company

Roger G Harrison

William J Ross

John Christopher Saunders

William B Jamieson

Acylamino tetrazolyl compounds having anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.

Acylamino derivatives

Acylamino pyrazolyl compounds of the formula: ##STR1## wherein Ar represents an optionally substituted pyrazolyl group, the acylamino group --NR.sup.1 COR.sup.2 being attached to a carbon atom of the pyrazolyl ring, which have anti-allergic activity, methods of making the compounds and pharmaceutical formulations containing the compounds.

Acylaminopyrazoles

Oxazoles having a sulfinyl or sulfonyl substituent at the 2-position are provided. Such compounds readily react with an alkali metal salt of a secondary amide in a method of making 2-acylamino oxazole derivatives having anti-allergic activity.

2-Sulfinyl and 2-sulfonyl oxazoles

1,2,3-triazoles and 1,2,4-triazoles having an N-substituted acylamino substituent are prepared by alkylating N-unsubstituted acylamino triazoles or acylating N-substituted amino triazoles. The N-substituted acylamino triazoles are useful as anti-allergy drugs. Pharmaceutical formulations containing acylamino triazoles and a method of treating allergic conditions utilizing such compounds are provided.

Acylamino triazoles as antiasthmatic agents

An improved method for the preparation of intermediates of formula: ##EQU1## WHERE R.sup.1 and R.sup.2 represent hydrogen, C.sub.1.sub.-4 alkyl, C.sub.1.sub.-4 hydroxyalkyl, C.sub.3.sub.-10 cycloalkyl, C.sub.3.sub.-6 acyloxyalkyl, or phenyl, by mercuric ion assisted hydrolysis of the corresponding dithianes, and novel intermediates thereby produced.

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Farnborough, United Kingdom

Roger G Harrison