Patent ID: 6448373
Filing Date: 2002-09-10
Classification: A61P,B01J,C07B,C07F,C07H

Abstract:
A compound having structure II: wherein:X is H, a phosphate group, an activated phosphate group, an activated phosphite group, a solid support, a conjugate group, or an oligonucleotide; Y is H, a hydroxyl protecting group, a conjugate group or an oligonucleotide; each Em, independently, is O or S; Z and each Zm, independently, are L1, L1â€”G1, L2, L2â€”G2, NR3R4, a nitrogen-containing heterocycle, a phosphate group, a polyether group, or a polyethylene glycol group, provided that at least two of Z and Zm are different moieties, and that if Z or Zm is a purine or pyrimidine nm is 0, then a nitrogen atom of said purine or pyrimidine is directly bound to said CH2 group; L1 is alkyl having 1 to about 20 carbon atoms, alkenyl having 2 to about 20 carbon atoms, or alkynyl having 2 to about 20 carbon atoms; L2 is aryl having 6 to about 14 carbon atoms or aralkyl having 7 to about 15 carbon atoms; G1 is halogen, OR1, SR2, NR3R4, C(&boxH;NH)NR3R4, NHC(&boxH;NH)NR3R4, CH&boxH;O, C(&boxH;O)OR5, CH(NR3R4)(C(&boxH;O)OR5), C(&boxH;O)NR3R4, a metal coordination group, or a phosphate group; G2 is halogen, OH, SH, SCH3, or NR3R4; R1 is H, alkyl having 1 to about 6 carbon atoms, or a hydroxyl protecting group; R2 is H, alkyl having 1 to about 6 carbon atoms, or a thiol protecting group; R3 and R4 are, independently, H, alkyl having 1 to about 6 carbon atoms, or an amine protecting group; R5 is H, alkyl having 1 to about 6 carbon atoms, or an acid protecting group; Q and each Qm, independently, are L1, G3, L1â€”G3 or G3â€”L1â€”G3; G3 is NR3, C(&boxH;O), C(&boxH;S), C(O)â€”O, C(O)â€”NH, C(S)â€”O, C(S)â€”NH, S(O)2, NR3C(&boxH;O), NR3C(&boxH;S), NR3C(O)â€”O, NR3C(O)â€”NH, NR3C(S)â€”O, NR3C(S)â€”NH or NR3S(O)2; n and each nm, independently, are 0 or 1; j and each jm, independently, are 1 to 6; and m is 1 to 50.