Aromatic Compositions As Inhibitors Of Exoprotein Production In Non-Absorbent Articles

Abstract

Non-absorbent articles are disclosed. The non-absorbent articles include an effective amount of an aromatic inhibitory compound to substantially inhibit the production of exotoxins by Gram positive bacteria. The aromatic inhibitory compounds of the present invention have the general formula: wherein R 1 is selected from the group consisting of H, —OR 5 , —R 6 C(O)H, —R 6 COOH, —OR 6 COOH, —C(O)NH 2 , and NH 2 and salts thereof; R 5 is a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 6 is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 7 is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 8 is a monovalent substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbyl moiety which may or may not be interrupted with hetero atoms; R 2 , R 3 , and R 4 are independently selected from the group consisting of H, OH, COOH, and —C(O)R 9 ; R 9 is hydrogen or a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety.

1 . An exoprotein inhibitor for inhibiting the production of exoproteins from Gram positive bacteria in and around the vagina comprising a non-absorbent substrate for insertion into a vagina being selected from the group consisting of a non-absorbent incontinence device, a barrier birth control device, a tampon applicator, and a douche, the non-absorbent substrate having deposited thereon an effective amount of a first active ingredient having the general formula: 
       
         
           
           
               
               
           
         
       
       wherein R 1  is selected from the group consisting of H, 
       
         
           
           
               
               
           
         
       
       —OR 5 , —R 6 C(O)H, —R 6 COOH, —OR 6 COOH, —C(O)NH 2 , 
       
         
           
           
               
               
           
         
       
       and NH 2  and salts thereof; R 5  is a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 6  is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 7  is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety; R 8  is a monovalent substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbyl moiety which may or may not be interrupted with hetero atoms; R 2 , R 3 , and R 4  are independently selected from the group consisting of H, OH, COOH, and —C(O)R 9 ; R 9  is hydrogen or a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety, wherein the first active ingredient is effective in inhibiting the production of exoprotein from Gram positive bacteria. 
     
     
         2 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is selected from the group consisting of 
       
         
           
           
               
               
           
         
       
       —OR 5 , and salts thereof and wherein R 5  is a monovalent saturated aliphatic hydrocarbyl moiety having from 1 to about 15 carbon atoms. 
     
     
         3 . The exoprotein inhibitor as set forth in  claim 2  wherein R 5  is a monovalent saturated aliphatic hydrocarbyl moiety having from 1 to about 10 carbon atoms. 
     
     
         4 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is selected from the group consisting of —R 6 C(O)H, —R 6 COOH, and —OR 6 COOH and wherein R 6  is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 15 carbon atoms. 
     
     
         5 . The exoprotein inhibitor as set forth in  claim 4  wherein R 6  is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 10 carbon atoms. 
     
     
         6 . The exoprotein inhibitor as set forth in  claim 4  wherein R 6  is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 6 carbon atoms. 
     
     
         7 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is selected from the group consisting of 
       
         
           
           
               
               
           
         
       
       and wherein R 7  is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 15 carbon atoms. 
     
     
         8 . The exoprotein inhibitor as set forth in  claim 7  wherein R 7  is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 10 carbon atoms. 
     
     
         9 . The exoprotein inhibitor as set forth in  claim 7  wherein R 7  is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety having from 1 to about 4 carbon atoms. 
     
     
         10 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is —R 6 COOH, R 6  is a divalent unsaturated aliphatic hydrocarbyl moiety having from 1 to about 6 carbon atoms, and R 2 , R 3 , and R 4  are hydrogen. 
     
     
         11 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is —C(O)NH 2 , R 2  is OH, and R 3  and R 4  are hydrogen. 
     
     
         12 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is 
       
         
           
           
               
               
           
         
       
       and R 5  is a monovalent saturated aliphatic hydrocarbyl group having from 1 to about 4 carbon atoms. 
     
     
         13 . The exoprotein inhibitor as set forth in  claim 1  wherein R 1  is 
       
         
           
           
               
               
           
         
       
       and R 7  is a trivalent saturated aliphatic hydrocarbyl moiety having from 1 to about 4 carbon atoms and R 8  is C(O)CH 3 . 
     
     
         14 . The exoprotein inhibitor as set forth in  claim 1  wherein R 2  is OH and R 3  is COOH. 
     
     
         15 . The exoprotein inhibitor as set forth in  claim 1  wherein the first active ingredient is selected from the group consisting of trans-cinnamic acid, 4-hydroxybenzoic acid, methyl ester, 2-hydroxybenzoic acid, 2-hydroxybenzamide, acetyl tyrosine, 3,4,5-trihydroxybenzoic acid, lauryl 3,4,5-trihydroxybenzoate, 4-hydroxy-3-methoxybenzoic acid, para-aminobenzoic acid, and acetaminophen. 
     
     
         16 . The exoprotein inhibitor as set forth in  claim 1  wherein the first active ingredient is present in an amount of at least about 0.01 micromoles per gram of non-absorbent substrate. 
     
     
         17 . The exoprotein inhibitor as set forth in  claim 1  wherein the first active ingredient is present in an amount from about 0.5 micromoles per gram of non-absorbent substrate to about 100 micromoles per gram of non-absorbent substrate. 
     
     
         18 . The exoprotein inhibitor as set forth in  claim 1  wherein the first active ingredient is present in an amount from about 1.0 micromoles per gram of non-absorbent substrate to about 50 micromoles per gram of non-absorbent substrate. 
     
     
         19 . The exoprotein inhibitor as set forth in  claim 1  further comprising a pharmaceutically active material selected from the group consisting of antimicrobials, antioxidants, anti-parasitic agents, antipruritics, astringents, local anaesthetics and anti-inflammatory agents. 
     
     
         20 . The exoprotein inhibitor as set forth in  claim 1  further comprising an effective amount of a second active ingredient, said second active ingredient comprising a compound with an ether, ester, amide, glycosidic, or amine bond linking a C 8 -C 18  fatty acid to an aliphatic alcohol wherein the second active ingredient is effective in substantially inhibiting the production of exoprotein from Gram positive bacteria. 
     
     
         21 . The exoprotein inhibitor as set forth in  claim 20  wherein the C 8 -C 18  fatty acid is linked to a polyalkoxylated sulfate salt. 
     
     
         22 . The exoprotein inhibitor as set forth in  claim 1  further comprising an effective amount of a second active ingredient having the general formula:
   R 10 —O—R 11      
       wherein R 10  is a straight or branched alkyl or straight or branched alkenyl having from 8 to about 18 carbon atoms and R 11  is selected from the group consisting of an alcohol, a polyalkoxylated sulfate salt and a polyalkoxylated sulfosuccinate salt wherein the second active ingredient is effective in substantially inhibiting the production of exoprotein from Gram positive bacteria. 
     
     
         23 . The exoprotein inhibitor as set forth in  claim 22  wherein R 10  is a straight or branched alkyl group. 
     
     
         24 . The exoprotein inhibitor as set forth in  claim 22  wherein R 10  is a straight or branched alkenyl group. 
     
     
         25 . The exoprotein inhibitor as set forth in  claim 22  wherein R 10  is obtained from the group consisting of caprylic acid, capric acid, lauric acid, myristic acid, palmitic acid and stearic acid. 
     
     
         26 . The exoprotein inhibitor as set forth in  claim 22  wherein R 11  is an aliphatic alcohol. 
     
     
         27 . The exoprotein inhibitor as set forth in  claim 26  wherein R 11  is an aliphatic alcohol selected from the group consisting of glycerol, glycol, sucrose, glucose, sorbitol, and sorbitan. 
     
     
         28 . The exoprotein inhibitor as set forth in  claim 27  wherein R 11  is a glycol selected from the group consisting of ethylene glycol, propylene glycol, polypropylene glycol, and combinations thereof. 
     
     
         29 . The exoprotein inhibitor as set forth in  claim 22  wherein the second active ingredient is selected from the group consisting of laureth-3, laureth-4, laureth-5, PPG-5 lauryl ether, 1-O-dodecyl-rac-glycerol, sodium laureth sulfate, potassium laureth sulfate, disodium laureth (3) sulfosuccinate, dipotassium laureth (3) sulfosuccinate and polyethylene oxide (2) sorbitol ether. 
     
     
         30 . The exoprotein inhibitor as set forth in  claim 22  wherein the second active ingredient is present in an amount of at least about 0.0001 millimoles per gram of non-absorbent substrate. 
     
     
         31 . The exoprotein inhibitor as set forth in  claim 22  wherein the second active ingredient is present in an amount of at least about 0.005 millimoles per gram of non-absorbent substrate. 
     
     
         32 . The exoprotein inhibitor as set forth in  claim 22  wherein the second active ingredient is present in an amount from about 0.005 millimoles per gram of non-absorbent substrate to about 0.2 millimoles per gram of non-absorbent substrate. 
     
     
         33 - 47 . (canceled) 
     
     
         48 . The exoprotein inhibitor as set forth in  claim 1  further comprising an effective amount of a second active ingredient having the general formula: 
       
         
           
           
               
               
           
         
       
       wherein R 17 , inclusive of the carbonyl carbon, is an alkyl group having 8 to 18 carbon atoms, and R 18  and R 19  are independently selected from hydrogen or an alkyl group having from 1 to about 12 carbon atoms which may or may not be substituted with groups selected from ester groups, ether groups, amine groups, hydroxyl groups, carboxyl groups, carboxyl salts, sulfonate groups, sulfonate salts, and mixtures thereof wherein said second active ingredient is effective in substantially inhibiting the production of exoprotein from Gram positive bacteria. 
     
     
         49 . The exoprotein inhibitor as set forth in  claim 48  wherein R 17  is derived from a saturated or unsaturated fatty acid. 
     
     
         50 . The exoprotein inhibitor as set forth in  claim 49  wherein R 17  is derived from an acid selected from the group consisting of caprylic acid, capric acid, lauric acid, myristic acid, palmitic acid, and stearic acid. 
     
     
         51 . The exoprotein inhibitor as set forth in  claim 48  wherein the second active ingredient is selected from the group consisting of sodium lauryl sarcosinate, lauramide monoethanolamide, lauramide diethanolamide, lauramidopropyl dimethylamine, disodium lauramide monoethanolamide sulfosuccinate, and disodium lauroamphodiacetate. 
     
     
         52 . The exoprotein inhibitor as set forth in  claim 48  wherein the second active ingredient is present in an amount of at least about 0.0001 millimoles per gram of non-absorbent substrate. 
     
     
         53 . The exoprotein inhibitor as set forth in  claim 48  wherein the second active ingredient is present in an amount of at least about 0.0005 millimoles per gram of non-absorbent substrate. 
     
     
         54 . The exoprotein inhibitor as set forth in  claim 48  wherein the second active ingredient is present in an amount from about 0.005 millimoles per gram of non-absorbent substrate to about 0.2 millimoles per gram of non-absorbent substrate. 
     
     
         55 . The exoprotein inhibitor as set forth in  claim 48  further comprising a pharmaceutically active material selected from the group consisting of antimicrobials, antioxidants, anti-parasitic agents, antipruritics, astringents, local anaesthetics and anti-inflammatory agents. 
     
     
         56 . The exoprotein inhibitor as set forth in  claim 1  further comprising an effective amount of a second active ingredient having the general formula: 
       
         
           
           
               
               
           
         
       
       wherein R 20  is an alkyl group having from about 8 to about 18 carbon atoms and R 22  and R 22  are independently selected from the group consisting of hydrogen and alkyl groups having from 1 to about 18 carbon atoms and which can have one or more substitutional moieties selected from the group consisting of hydroxyl, carboxyl, carboxyl salts and imidazoline wherein the second active ingredient is effective in substantially inhibiting the production of exoprotein from Gram positive bacteria. 
     
     
         57 . The exoprotein inhibitor article as set forth in  claim 56  wherein R 22  comprises a carboxyl salt, the carboxyl salt having a cationic moiety selected from the group consisting of sodium, potassium and combinations thereof. 
     
     
         58 . The exoprotein inhibitor as set forth in  claim 56  wherein R 22  comprises an amine selected from the group consisting of lauramine, lauramino propionic acid, sodium lauriminodipropionic acid, lauryl hydroxyethyl imidazoline and mixtures thereof. 
     
     
         59 . The exoprotein inhibitor as set forth in  claim 56  wherein the second active ingredient is present in an amount of at least about 0.0001 millimoles per gram of non-absorbent substrate. 
     
     
         60 . The exoprotein inhibitor as set forth in  claim 56  wherein the second active ingredient is present in an amount of at least about 0.005 millimoles per gram of non-absorbent substrate. 
     
     
         61 . The exoprotein inhibitor as set forth in  claim 56  wherein the second active ingredient is present in an amount from about 0.005 millimoles per gram of non-absorbent substrate to about 0.2 millimoles per gram of non-absorbent substrate. 
     
     
         62 . The exoprotein inhibitor as set forth in  claim 56  further comprising a pharmaceutically active material selected from the group consisting of antimicrobials, antioxidants, anti-parasitic agents, antipruritics, astringents, local anaesthetics and anti-inflammatory agents. 
     
     
         63 - 68 . (canceled)