1,2,3,6-tetrahydropyrimidine-2-one compositions and therapeutic methods therewith for sexual disfunction

Abstract

A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one sensory nerve receptor agonist in a therapeutically effective amount. The sensory nerve receptor agonist may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 is -hydroxy, -chloro, - fluoro, -alkyl, -acetoxy, -trifluoromethyl ; and R2 is -nitro, -chloro, -fluoro, -alkyl, -trifluoromethyl. Therapeutic compositions of the invention elicit soothing, cooling, and stimulatory effects when formulated for topical delivery to human sexual organs and to anorectal areas of the body and are useful to alleviate dysfunction in sexual response and intercourse for both men and women.

It is claimed:  
     
         1 . A composition for the treatment of sexual dysfunction, comprising: 
 a therapeutically effective amount of a sensory nerve endings receptor agonist having the formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one, wherein R1 is hydroxy, chloro, fluoro, an alkyl of about 2 to about 4 carbon atoms, acetoxy, or trifluoromethyl and R2 is nitro, chloro, fluoro, an alkyl or about 2 to 4 carbon atoms or trifluoromethyl; and    a dermatologically acceptable vehicle in which the a sensory nerve endings receptor agonist is dispersed.    
     
     
         2 . The composition for the treatment of sexual dysfunction as in  claim 1  wherein the sensory nerve endings receptor agonist is in an amount of from about 0.1% w/w to about 15% w/w and is dispersed as a suspension or an emulsion.  
     
     
         3 . An ointment or cream composition comprising: 
 1-[2-hydroxy]-4-[3-nitrophenyl]-1,2,3,6-tetrahydropyridimine-2-one or an analog thereof in an amount of about 0.1 wt. % to about 20 wt. % of the composition; and,    an oleaginous base.    
     
     
         4 . A method of treating sexual dysfunction in a human patient comprising: topically administering a therapeutically effective amount of a sensory nerve endings receptor agonist having the formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one, wherein R1 is hydroxy, chloro, fluoro, an alkyl of about 2 to about 4 carbon atoms, acetoxy, or trifluoromethyl and R2 is nitro, chloro, fluoro, an alkyl of about 2 to 4 carbon atoms or trifluoromethyl, to a sex organ or an anorectal area of the patient.  
     
     
         5 . The method as in  claim 4  wherein the sensory nerve endings receptor agonist is administered as an ointment or cream  
     
     
         6 . The method as in  claim 4  wherein the sensory nerve endings receptor agonist is administered as a lotion, gel, liniment, powder, spray, foam, or in suspension or in emulsified form.  
     
     
         7 . The method as in  claim 4  wherein the amount of the sensory nerve receptor agonist administered is in an amount of from about 1 mg to about 15 mg per application.  
     
     
         8 . A method of treating sexual dysfunction or enhancing sexual pleasure in a man, comprising: 
 topically applying a composition comprising 1-[2-hydroxy]-4-[3-nitrophenyl]-1,2,3,6-tetrahydropyridimine-2-one or an analog to the penis or anorectal area.    
     
     
         9 . A method of treating sexual dysfunction or enhancing sexual pleasure in a woman, comprising: 
 topically applying a composition comprising 1-[2-hydroxy]-4-[3-nitrophenyl]-1,2,3,6-tetrahydropyridimine-2-one or an analog to the gentalia.    
     
     
         10 . A method of treating sexual dysfunction or enhancing sexual pleasure in a human, comprising: 
 topically applying a composition comprising 1-[2-hydroxy]-4-[3-nitrophenyl]-1,2,3,6-tetrahydropyridimine-2-one or an analog to the gentalia or anorectal area, the 1-[2-hydroxy]-4-[3-nitrophenyl]-1,2,3,6-tetrahydropyridimine-2-one or an analog being in an amount of at least about 0.1 wt % of the composition.