초록 ▼

The present invention relates to the formulations of ester derivatives of sandalwood oil and santalol. These derivatives are capable of reverting to the active parent compound following enzymatic or chemical hydrolysis. These derivatives have a higher lipophilicity, lipid solubility and less irritat

The present invention relates to the formulations of ester derivatives of sandalwood oil and santalol. These derivatives are capable of reverting to the active parent compound following enzymatic or chemical hydrolysis. These derivatives have a higher lipophilicity, lipid solubility and less irritation to the skin than the parent compound, and hence are better able to be incorporated into certain pharmaceutical formulations, including cream and ointment pharmaceutical formulations. The compounds of the present invention are set forth by the following formula: The present invention generally pertains to a compound of formula (I): R—CO—SWO  (I) wherein SWO refers to collectively the alcohols, including santalol, present in the sandalwood oil; wherein R is selected from alkyl groups of up to about 22 carbon atoms and aryl groups of up to about 22 carbon atoms and alkylene group of up to about 22 carbon atoms and an arylene group of up to about 22 carbon atoms. The alkyl, aryl and alkylene groups may be substituted or unsubstituted, branched or straight chains. In addition, R may contain heteroatoms and may be straight chained or branched. Compounds of formula I are useful as anti-bacterial and anti-viral in mammals in vivo and have been contemplated to be used in the treatment of skin disease.

대표청구항 ▼

We claim: 1. A method for treating cold sores and genital herpes induced by the infection of herpes simplex viruses (HSV-1 and HSV-2) in a mammal, said method comprising application to said mammal of a therapeutically effective amount of a pharmaceutical composition containing an ester of sandalwoo

We claim: 1. A method for treating cold sores and genital herpes induced by the infection of herpes simplex viruses (HSV-1 and HSV-2) in a mammal, said method comprising application to said mammal of a therapeutically effective amount of a pharmaceutical composition containing an ester of sandalwood oil of formula (I): R—CO—SWO  (I) wherein SWO refers to collectively the alcohols, including santalol, present in the sandalwood oil; wherein R is selected from alkyl groups of up to about 22 carbon atoms and aryl groups of up to about 22 carbon atoms and alkylene group of up to about 22 carbon atoms and an arylene group of up to about 22 carbon atoms, wherein all of said alcohols in said oil are fully esterified. 2. The ester of sandalwood oil of claim 1 wherein R is a methyl group. 3. The method of claim 1, wherein the pharmaceutical composition is comprised in a topical formulation. 4. The method of claim 3, wherein the topical formulation is a cream. 5. The method of claim 1, wherein the pharmaceutical composition comprises one or more additional pharmaceutical agents. 6. The method of claim 5, wherein the one or more additional pharmaceutical agents is one or more fungicidal or fungistatic agents. 7. The method of claim 5, wherein the one or more additional pharmaceutical agents is one or more bacteriocidal or bacteriostatic agents. 8. The method of claim 5, wherein the one or more additional pharmaceutical agents is one or more viricidal or viristatic agents. 9. The method of claim 5, wherein the one or more additional pharmaceutical agents is one or more cytotoxic agents. 10. The method of claim 1, wherein the composition is a pharmaceutical composition further comprising one or more pharmaceutically acceptable excipients. 11. The method of claim 10, wherein the excipients include one or more pharmaceutically acceptable antioxidants. 12. The method of claim 11, wherein the antioxidant is selected from the group consisting of ascorbic acid, sodium ascorbate, sodium bisulfite, sodium metabisulfate, curcumin, curcumin derivatives, ursolic acid, resveratrol, resveratrol derivatives, alpha-lipoic acid and monothioglycerol. 13. The method of claim 10, wherein the excipients are selected from the group consisting of pharmaceutically acceptable preservatives and buffering agents. 14. The method of claim 13, wherein the buffering agent is selected from the group consisting of monobasic sodium phosphate, dibasic sodium phosphate, sodium benzoate, potassium benzoate, sodium citrate, sodium acetate and sodium tartrate. 15. The method of claim 13, wherein the preservative is selected from the group consisting of methylparaben, methylparaben sodium, propylparaben, propylparaben sodium, benzalkonium chloride and benzthonium chloride. 16. The method of claim 1, wherein the composition comprises one or more pharmaceutically acceptable polysaccharides. 17. The method of claim 16, wherein the polysaccharide is selected from the group consisting of dextran sulfate, pectin, modified pectin, insoluble 1,3-β-D glucan, micronized 1,3-β-D glucan, soluble 1,3-β-D glucan, phosphorylated 1,3-β-D glucan, aminated 1,3-β-D glucan and carboxymethylated 1,3-β-D glucan, sulfated 1,3-β-D glucan, insoluble 1,3/1,6-β-D glucan, micronized 1,3/1,6-β-D glucan, soluble 1,3/1,6-β-D glucan, phosphorylated 1,3/1,6-β-D glucan, aminated 1,3/1,6-β-D glucan and carboxymethylated 1,3/1,6-β-D glucan or sulfated 1,3/1,6-β-D glucan. 18. The method of claim 1 wherein the mammal is a human. 19. The method of claim 1, wherein the composition is administered orally, nasally, topically, rectally or vaginally. 20. The method of claim 1 where the alkyl, aryl and alkylene groups may be substituted. 21. The method of claim 1 where the alkyl, aryl and alkylene groups may be unsubstituted. 22. The method of claim 1 where the alkyl, aryl and alkylene groups may be branched chains. 23. The method of claim 1 where the alkyl, aryl and alkylene groups may be straight chains. 24. The method of claim 1 where the R may contain heteroatoms such as O, N, Cl, F, Br, I and S. 25. The method of claim 1 where the R may be a straight chain. 26. The method of claim 1 where the R may be a branched chain.