Patent ID: 6369040
Filing Date: 2002-04-09
Classification: A61K,C07H,C07J,C07K,C12N,C12Q,C12Y,Y02P

Abstract:
A pharmaceutical composition comprising a compound having the following formula: wherein:R5 is H or CH3; one of R2 and R4 is &boxH;O, &boxH;NH, or &boxH;NH2+; and the other of R2 and R4 is Q, &boxH;C(RA)â€”Q, C(RA)(RB)â€”C(RC)(RD)â€”Q, C(RA)&boxH;C(RC)â€”Q or Câ‰¡Câ€”Q; each RA, RB, RC and RD is, independently [are] H, SH, OH, NH2, or C1-C20 alkyl, or one of (RA) and (RB) or (RC) and (RD) is combined to give &boxH;O and each of the other of (RA) and (RB) or (RC) and (RD) is, independently H, SH, OH, NH2, or C1-C20 alkyl; Q is halogen, hydrogen, C1-C20 alkyl, C1-C20 alkylamine, C1-C20 alkyl-N-phthalimide, C1-C20 alkylimidazole, C1-C20 alkylbis-imidazole, NH2, C2-C20 alkenyl, C2-C20 alkynyl, hydroxyl, thiol, keto, carboxyl, nitrates, nitro, nitroso, nitrile, trifluoromethyl, trifluoromethoxy, O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aralkyl, S-aralkyl, NH-aralkyl, azido, hydrazino, hydroxylamino, isocyanato, sulfoxide, sulfone, sulfide, disulfide, silyl, O-(hydroxyl protecting group), a leaving group, a heterocycle, a polyamine, a polyamide, a polyether, or a depurination enhancing group; T3 and T5 independently are H, phosphate, an activated phosphate, a hydroxyl protecting group, a nucleoside, a nucleotide, an oligonucleotide comprising up to 50 nucleosides joined together by 3â€²-5â€² internucleoside linkages, or an oligonucleoside comprising up to 50 nucleosides joined together by 3â€²-5â€² internucleoside linkages; X1 and X2 independently are hydrogen, halogen, hydroxyl, O-(hydroxyl protecting group), thiol, carboxyl, nitrate, nitro, nitroso, nitrile, trifluoromethyl, trifluoromethoxy, O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aralkyl, S-aralkyl, NH-aralkyl, amino, azido, hydrazino, hydroxylamino, isocyanato, sulfoxide, sulfone, sulfide, disulfide, silyl, heterocyclic, alicyclic, carbocyclic, polyamines, polyamides, or polyethers; or T3 and one of X1 or X2, together, form a hydroxyl protecting group; and provided that when T5 is a hydroxyl protecting group or together T3 and one of X1 or X2 is a hydroxyl protecting group, then R2 is not CH3; and that when T3 and T5 are OH or O-benzoyl, then R2 is not CH2OC6H5; and that when R4 is Q, then Q is not hydrogen, hydroxyl, thiol, amino or hydrogen.