METHODS AND COMPOSITIONS INVOLVING ESTERS OF AZELAIC ACID AND OTHER DICARBOXYLIC ACIDS

摘要

The present invention relates to formulations of azelaic acid esters and other dicarboxylic acid esters, and their derivatives. In preferred embodiments, the esters have the general Formula (I) wherein R<SUB>1</SUB> and R<SUB>2</SUB> are selected from hydrogen, alkyl groups of up to about 18 carbon atoms and aryl groups of up to about 18 carbon atoms and alkylene group of up to about 18 carbon atoms and an arylene group of up to about 18 carbon atoms. The alkyl, aryl, alkylene and aryl groups may be substituted or unsubstituted, branched or straight chains. In addition, R<SUB>1</SUB> and R<SUB>2</SUB> may contain heteroatoms and may be straight chained or branched, n is an integer from 1-16, and R<SUB>1</SUB> and R<SUB>2</SUB> are not simultaneously hydrogen. R<SUB>2</SUB>OOC-(CH<SUB>2</SUB>)n-COOR<SUB>1 </SUB>(I). The azelaic acid derivatives of Formula I of this invention are certain derivatives of azelaic acid and other alkyl geminal diacids which possess a desirable high lipophilicity and biphasic solubility in comparison to the parent compound, azelaic acid, and which are cleaved enzymatically to azelaic acid. Compounds produced from the compounds of Formula (I) by the enzymatic hydrolysis of the R<SUB>1</SUB> and R<SUB>2</SUB> groups are useful as anti-bacterial agents in mammals in vivo and have been contemplated to be used in the treatment of skin disease.