Patent EA-001517-B1 (EA)
Title: Combinations comprising vx478, zidovudine, ftc and/or 3tc for use in the treatment of hiv
Inventor: ST CLAIR MARTHA HEIDER
IPC: A61K31/34
Filed: 1997-06-23
Abstract: 1. A combination for use in the treatment of an HIV infection beyond central nervous system comprising 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester or a physiologically functional derivative thereof, zidovudine or a physiologically functional derivative thereof and (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one or a physiologically functional derivative thereof wherein the ratio of these three compounds is over the range of 1 to 10: 1 to 10: 1 to 5 by weight. 2. A combination according to claim 1 comprising 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester, zidovudine, and (2R,cis)-4-amino-1-(2-hydroxymethyl-l,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one. 3. A combination according to any claim from 1 to 2 for use in medicine. 4. A combination according to any claim from 1 to 2 for use in the treatment of HIV infections. 5. A combination according to any claim from 1 to 2 for use in the treatment of an HIV infection resistant to nucleoside or non-nucleoside inhibitors. 6. A combination according to any claim from 1 to 2 for use in the treatment of AIDS. 7. A pharmaceutical formulation comprising a combination according to any claim from 1 to 2 in association with one or more pharmaceutically acceptable carriers therefor. 8. A formulation according to claim 7 in unit dosage form. 9. Use of 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester in the manufacture of a medicament for administration either simultaneously or sequentially with zidovudine and (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one for the treatment of an HIV infection beyond central nervous system. 10. Use of zidovudine in the manufacture of a medicament for administration simultaneously or sequentially with 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester and (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one for the treatment of an HIV infection beyond central nervous system. 11. Use of (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the manufacture of a medicament for administration simultaneously or sequentially with 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester and zidovudine for the treatment of an HIV infection beyond central nervous system. 12. Use as claimed in any claim from 9 to 11 for the treatment of an HIV infection resistant to nucleoside or non-nucleoside inhibitors. 13. Use as claimed in any claim from 9 to 11 for the treatment of AIDS related conditions. 14. A patient pack comprising at least one active ingredient selected from 3S-[3R*(1R*,2S*)]-[3-[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-aminoformic acid tetrahydro-3-furanyl ester, zidovudine and (2R,cis)-4-amino-l-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one and an information insert containing directions on the use of all three active ingredients.