NEW CLASS OF COMPOUNDS HAVING A VARIABLE SPECTRUM OF ACTIVITIES FOR CAPSAICIN-LIKE RESPONSES, COMPOSITIONS AND USES THEREOF

摘要

The present invention relates to a new class of compounds having a variable spectrum of activities for capsaicin-like responses, compositions thereof, processes for preparing the same, and uses thereof. Compounds of the invention are prepared by combining phorbol related diterpenes and homovanillic acid analogs via esterification at the exocyclic hydroxy group for the diterpene. Examples of these compounds include 20- homovanillyl-mezerein and 20-homovanillyl-12- deoxyphorbol-13-phenyl-acetate. These compounds having a variable spectrum of activities for capsaicin-like responses are represented by the following formulas I to IV: (see formula I, II, III) (see formula IV,) wherein R1 in formulas (I)-(IV) represents (see formula V,VI) with the proviso that in formula (II), R' is not (see formula VII) R3 and R4 are not H at the same time. The compounds are useful in therapeutic compositions for desensitizing a subject animal.