9-substituted-8-unsubstituted-9-deazaguanines

Details 9-substituted-8-unsubstituted-9-deazaguanines 9-substituted-8-unsubstituted-9-deazaguanines

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2047216

The specification discloses the compounds of formula (1), wherein (a) -CH2Ar represents formula .alpha., in which R1 represents hydrogen, halogen, C1-C3-alkyl, C1-C3-alkoxy, benzyloxy, hydroxy, or trifluoromethyl; and R2 represents hydrogen, halogen, C1-C3-alkyl, C1-C3-alkoxy, benzyloxy, hydroxy or trifluoromethyl; provided that R2 represents hydrogen or C1-C3-alkyl if R1 represents trifluoromethyl, or that R1 represents hydrogen or C1-C3-alkyl if R2 represents trifluoromethyl; or (b) -CH2Ar represents formula .beta., in which X represents sulfur or oxygen and in which attachment to the thiophene or furan ring is at the 2- or 3-position; and tautomers thereof; as purine nucleoside phosphorylase inhibitors.

Composés correspondant à la formule (I) où soit (a) -CH2Ar représente alpha où R1 représente hydrogène, halogène, C1-C3 alkyle, C1-C3 alcoxy, benzyloxy, hydroxy ou trifluorométhyle; et R2 représente hydrogène, halogène, C1-C3 alkyle, C1-C3 alcoxy, benzyloxy, hydroxy ou trifluorométhyle; cela à la condition que R2 représente hydrogène ou C1-C3 alkyle si R1 représente trifluorométhyle, ou que R1 représente hydrogène ou C1-C3 alkyle si R2 représente trifluorométhyle; soit (b) -CH2Ar représente beta, où X représente soufre ou oxygène et où la liaison avec l'anneau de tiofène ou de furane se fait en position 2 ou 3. L'invention porte en outre sur des tautomères de ces composés, qui servent d'inhibiteurs de phosphorylase de nucléosides de purine.

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