Novel pyranosyl cytosines: pharmaceutical formulations and methods

A compound of the formula (I):

• 142
• where R1 is ˜NR8R9 or ˜C(R10)3;
• R2, R3 and R7 each independently are ˜NR11R12, ˜YZ, alkyleno, substituted alkyleno, heteroalkyleno, substituted heteroalkyleno, aryleno, heteroaryleno, alkylenearyleno, arylenealkyleno, alkyleneheteroalkyleno, heteroyleno, halyleno, H radical or;
• where R2 and R3 or R3 and R7, together form a ring including two atoms of the pyrimidine ring and having at least 1 additional ring atom;
• each R5 independently is alkyl, substituted alkyl, heteroalkyl, alkylenheteroyl, aryl, heteroaryl, ˜(CH2)nN(R11R12), ˜(CH2)nG or H radical;
• R6 is an electron pair, alkyleno, heteroalkyleno, aryleno, heteroaryleno or H radical;
• R4, R11, R12, R15 and R16 each independently are alkyleno, heteroalkyleno, aryleno, heteroaryleno or H radical;
• R8 and R9 each independently are alkyleno, heteroalkyleno, substituted heteroalkyleno, aryleno, heteroaryleno, H radical or together join to form an aminocyclic ring radical;
• each R10 independently is alkyleno, heteroalkyleno, aryleno, heteroaryleno, halyleno or H radical;
• R13 and R14 each independently are alkyleno, heteroalkyleno, aryleno, heteroaryleno, halyleno, hydroxyleno or H radical;
• Y is a heteroatom radical with Z a radical selected from the group comprising 1 or more heteroatoms or H, alkyleno, heteroalkyleno, aryleno, heteroaryleno, halyleno, combinations thereof and adapted to fill the valence of Y, said Y being singly or doubly bound to the pyrimidine ring radical;
• Q is a member selected from the group of radicals comprising ˜S(═O)˜, ˜S(O)2˜, ˜C(═O)˜, ˜C(═S)˜, ˜CH2˜, ˜Y(O)˜ and ˜C(Y)n˜;
• where G is a cyclic alkyleno or cyclic heteroalkyleno substituent and n is an integer of at least 0;
• and
• with the proviso that;
• when R2 is ˜NH2 and R9 is ˜H, then;
• R8 is not an amino acid and;
• the ratio of carbon atoms to nitrogen atoms of R5 is greater than or equal to one and;
• R16 is H radical and;
• R15 does not comprise a
• 143
• radical.