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US 5,496,935 AGranted
2',3'-dideoxynucleoside pyrimidine compounds and carbocyclic analogs
AssigneeMax-Delbru/ ck-Centrum
InventorsEckart Matthes, Martin von Janta-Lipinski, Dieter Scholz, Klaus Gaertner, Juergen Schildt, Christine Lehmann, Peter Langen, Hans A. Rosenthal
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Abstract
2',3'-dideoxynucleoside pyrimidine compounds and 2-thiothymidine carbocyclic derivatives with antiviral activity are disclosed. These compounds are expected to exhibit antiviral activity recognized for 2',3'-dideoxynucleoside compounds and analogs thereof.
Claims1
A substituted pyrimidine nucleoside selected from the group consisting of:
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-5-methyl-pyrimidine-2-one,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-thiothymine,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-hydroxylamino-5-methyl-(1 H)-pyrimidine-2-one,
- 5-chloro-1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-thiouracil,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-(1H)-pyrimidine-2-one,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-thiouracil,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-hydroxylamino-(1H)-pyrimi dine-2-one,
- 1-(2,3-dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)-4-thiothymine,
- 1-(2,3-dideoxy-.beta.D-glycero-pent-2-enofuranosyl)-5-methyl-(1H)-pyrimidin e-2-one,
- 1-(2,3-dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)-4-hydroxylamino-(1H)-p yrimidine-2-one,
- 1-(2,3-dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)-4-dimethylamino-(1H)-p yrimidine-2-one,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-5-methyl-pyrimidine-2-one,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-pyrimidine-2-one,
- 2',3'-dideoxy-2',3'-didehydro-4-thiothymidine,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-2-thiothymine,
- 1-(5-O-acetyl-2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-2-thiothymine,
- 1-(5-O-acetyl-2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-2,4-dithiothymin e,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-2,4-dithiothymine,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-5-ethyl-4-thiouracil,
- (.+-.)-1-[1.beta.,3,4.beta.)-3-fluoro-4-(trityloxymethyl)-cyclopentyl]-2-th iothymine,
- (.+-.)-1-[1.beta.,3.alpha.,4.beta.)-3-fluoro-4-(hydroxymethyl)-cyclopentyl] -2-thiothymine,
- 3'-deoxy-4-thiothymidine,
- 1-(5-O-acetyl-2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-thiothymine,
- 1-(5-O-acetyl-2,3-dideoxy-3-fluoro-.beta.-D-glycero-ribofuranosyl)-4-hydrox ylamino-(1H) pyrimidine-2-one,
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-glycero-ribofuranosyl)-4-hydroxylamino-(1H )-pyrimidine-2-one,
- 1-(5-O-acetyl-2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-hydroxylamino- 5-methyl-(1H)-pyrimidine-2-one,
- 1-(5-O-acetyl-2,3-dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)-4-thiothymi ne, and
- 1-(2,3-dideoxy-3-fluoro-.beta.-D-ribofuranosyl)-4-thiothymine-5'-triphospha te.
25 more elements
Dependencies are inferred from the claim text.