Claims
- 1) A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human an effective amount of a dihydro-alkyloxy-benzyl-oxopyrimidine of formula (A):
- 2) The method of claim 1 wherein the composition is applied to the vaginal endothelium, the rectal endothelium, or the male genetalia.
- 3) The method of claim 1 wherein the composition is in the form of a cream, lotion, gel, or foam.
- 4) The method of claim 1 wherein the composition is in the form of an intra-vaginal pill, an intra-rectal pill, or a suppository.
- 5) The method of claim 1 wherein the composition is topically applied by release from an intravaginal device selected from a vaginal ring, a vaginal sponge, a diaphram, or a cervical cap.
- 6) The method of claim 1 wherein the composition is topically applied from the exterior surface of a condom or vaginal applicator.
- 7) The method of claim 1 wherein the composition further comprises a second anti-HIV agent, a viruside effective against viral infections other than HIV, and/or a spermicide.
- 8) The method of claim 1 wherein the composition further comprises a lubricant.
- 9) The method of claim 1 wherein, in formula (A), Y is —C1-4alkyl, and Z is —C1-4alkyl.
- 10) The method of claim 1 wherein, in formula (A), R1 and R5 are halogen.
- 11) The method of claim 1 wherein, in formula (A), Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 12) The method of claim 1 wherein, in formula (A), —X—R is —N-Me2, Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 13) The method of claim 1 wherein, in formula (A), —X—R is —NH-cPe, Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 14) The method of claim 1 wherein, in formula (A), —X—R is —N═O, Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 15) The method of claim 1 wherein, in formula (A), —X—R is —S-Me, Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 16) The method of claim 1 wherein, in formula (A), —X—R is —S-MeSMe, Y is methyl, Z is methyl, R1 and R5 are fluorine, and R2, R3, and R4 are hydrogen.
- 17) A topical composition in the form of a cream, lotion, gel, or foam, comprising a dihydro-alkyloxy-benzyl-oxopyrimidine of formula (A):
- 18) The composition of claim 17 further comprising a second anti-HIV agent.
- 19) The composition of claim 17 further comprising a viruside effective against viral infections other than HIV.
- 20) The composition of claim 17 further comprising a spermicide.
- 21) The composition of claim 17 further comprising a lubricant.
- 22) A composition in the form of an intra-vaginal or intra-rectal pill or suppository comprising a dihydro-alkyloxy-benzyl-oxopyrimidine of formula (A):
- 23) The composition of claim 22 further comprising a second anti-HIV agent.
- 24) The composition of claim 22 further comprising a viruside effective against viral infections other than HIV.
- 25) The composition of claim 22 further comprising a spermicide.
- 26) A device for inhibiting the sexual transmission of HIV comprising:
a) a barrier structure for insertion into the vaginal cavity, and b) a composition comprising a dihydro-alkyloxy-benzyl-oxopyrimidine of formula (A): 11wherein: X is —O, —CH2, —CHK1 (wherein K1 is —H, —C1-4 alkyl, —C3-6Cycloalkyl), —S, —NK2 (wherein K2 is —H, —C1-4alkyl, —C3-6cycloalkyl, or a bond when X—R is nitro), -aryl, or -arylalkyl; R is —H, —C1-4alkyl (optionally containing one or more of heteroatoms selected from O, S, and N), —C3-6 cycloalkyl (optionally containing one or more of heteroatoms selected from O, S, N), -aryl, -arylakl, heterocycle, oxo, thio, or a primary amine; Y is —H, —C1-4alkyl, or —C3-6cycloalkyl; Z is —H, —C1-4alkyl, or —C3-6cycloalkyl; R1 is —H, —C1-4alkyl, -halogen, —NO2, —OW (wherein W is —H, —CH3, aryl), or —SW (wherein W is —H, —CH3, -aryl); R2 is —H, —C1-4alkyl, -halogen, —NO2, —OW (wherein W is —H, —CH3, -aryl); or —SW (wherein W is —H, —CH3, -aryl); R3 is —H, —C1-4alkyl, -halogen, —NO2, —OW (wherein W is —H, —CH3, -aryl); or —SW (wherein W is —H, —CH3, -aryl); R4 is —H, —C1-4alkyl, -halogen, —NO2, —OW (wherein W is —H, —CH3, -aryl); or —SW (wherein W is —H, —CH3,-aryl); and R5 is —H, —C1-4-alkyl, -halogen, —NO2, —OW (wherein W is —H, —CH3, -aryl), or —SW (wherein W is —H, —CH3, -aryl).
- 27) The device of claim 26 wherein the barrier structure is a vaginal sponge, diaphram, cervical cap, or condom.
- 28) The device of claim 26 wherein the composition further comprises a second anti-HIV agent, a viruside effective against viral infections other than HIV, and/or a spermicide.
- 29) A compound of formula (A):
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority to provisional application serial No. 60/249,532, filed Nov. 17, 2000.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60249532 |
Nov 2000 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
10001868 |
Nov 2001 |
US |
Child |
10350772 |
Jan 2003 |
US |