Warner-lambert Company

David M Lustgarten

Richard E Brown

Donald E Butler

Walter H Moos

Anthony J Thomas

Certain tetrasubstituted alkyl, aryl, pyridinyl, piperidinyl, and piperazinyl urea compounds stimulate the release of acetylcholine and are thus useful analgesic agents for alleviating pain or as cholinergic agents which are useful for the amelioration of the symptoms of cognitive decline in the elderly. These compounds have the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are phenyl or substituted phenyl, and R.sub.3 is pyridinyl. Pharmaceutical compositions including these compounds as well as methods for the preparation of the compounds are also disclosed.

Tetrasubstituted urea cholinergic agents

This invention relates to substituted 2-amino chromones of the general structure I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 may be hydrogen, hydroxy, lower alkyl or lower alkoxy of 1-6 carbon atoms, halogen such as chloro or bromo, or aryl such as phenyl, and X may be cyano or carboxamido. Two novel procedures for preparing substituted 2-amino chromones having the Formula I, starting with salicylic acid or substituted salicylic acid, are described. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.

Substituted 2-amino chromones and process for the preparation thereof

This invention relates to substituted 2-aminothiochromones of the general structure I: ##STR1## wherein R.sub.1 and R.sub.2 may be hydrogen; lower alkyl or lower alkoxy of 1 to 6 carbon atoms; or halogen such as chloro or bromo; and X may be cyano or carboxamido. The compounds are prepared using a thiosalicylic acid or a substituted thiosalicylic acid as starting material. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.

Substituted 2-aminothiochromones

This invention relates to substituted 2-amino chromones of the general structure I: ##SPC1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 may be hydrogen, hydroxy, lower alkyl or lower alkoxy of 1-6 carbon atoms, halogen such as chloro or bromo, or aryl such as phenyl, and X may be cyano or carboxamido. Two novel procedures for preparing substituted 2-amino chromones having the Formula I, starting with salicylic acid or substituted salicylic acid, are described. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.

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Dover, NJ, United States of America

David M Lustgarten