Patent ID: 6828427
Filing Date: 2004-12-07
Classification: B01J,C07D,C07F,C07H,C12Q,C40B

Abstract:
An oligomeric compound comprising a plurality of aminodiol monomer subunits joined by linking groups, wherein each of said aminodiol monomer subunits has one of the structures II, III, IV or VI: wherein:each x is, independently, 0 to 5; R1 is â€”Tâ€”L or a base labile protecting group; T is a single bond, a methylene group or a group having formula: {[CR6R7]mâ€”(R5)â€”[CR8R9]nâ€”[C(R10)]pâ€”(E)â€”}qâ€”wherein:R10 is &boxH;O, &boxH;S, or &boxH;NR11; R5 and E, independently, are a single bond, CH&boxH;CH, Câ‰¡C, O, S, NR11, or C6-C14 aryl; each R6, R7, R8, R9, R11, R12 and R13 are, independently, H, alkyl or haloalkyl having 1 to about 10 carbon atoms, alkenyl having 2 to about 10 carbon atoms, alkenyl having 2 to about 10 carbon atoms, or aryl having 7 to about 14 carbon atoms; m and n, independently, are 0 to 5; p is 0 or 1; q is 1 to about 10; L is H, substituted or unsubstituted C2-C10 alkyl, substituted or unsubstituted C2-C10 alkenyl, substituted or unsubstituted C2-C10 alkynyl, substituted or unsubstituted C4-C7 carbocyclic alkyl, substituted or unsubstituted C4-C7 carbocyclic alkenyl, substituted or unsubstituted C4-C7 carbocyclic alkynyl, substituted or unsubstituted C6-C14 aryl, an ether having 2 to 10 carbon atoms and 1 to 4 oxygen or sulfur atoms, a nitrogen containing heterocycle, a sulfur containing heterocycle, an oxygen containing heterocycle, a metal coordination group, a conjugate group, halogen, hydroxyl (OH), thiol (SH), keto (C&boxH;O), carboxyl (COOH), amide (CONR12), amidine (C(&boxH;NH)NR12R13), guanidine (NHC(&boxH;NH)NR12R13), glutamyl (R12OOCCH(NR12R13)(CH2)2C(&boxH;O), nitrate (ONO2), nitro (NO2), nitrile (CN), trifluoromethyl (CF3), trifluoromethoxy (OCF3), O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aralkyl, S-aralkyl, NH-aralkyl, amino (NH2), azido (N3), hydrazino (NHNH2), hydroxylamino (ONH2), sulfoxide (SO), sulfone (SO2), sulfide (Sâ€”), disulfide (Sâ€”S), silyl, a nucleosidic base, an amino acid side chain, a carbohydrate, a biopharmaceutically active moiety, or group capable of hydrogen bonding where the substituent groups are selected from hydroxyl, amino, alkoxy, alcohol, benzyl, phenyl, nitro, thiol, thioalkoxy, halogen, alkyl, aryl, alkenyl, and alkynyl groups; R2 is hydrogen or C1-C10 alkyl; R3 and R4 are independently hydrogen, an acid labile hydroxyl protecting group, a linking group or a conjugate group, wherein said linking group has the formula: â€ƒwherein: J1 is &boxH;O or &boxH;S; J2 is OH or N(Y0)T0; Y0 is H or (Q2)jâ€”Z2; T0 is (Q1)kâ€”Z1, or together Y0 and T0 are joined in a nitrogen heterocycle; Q1 and Q2 independently are C2-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C4-C7 carbocylo alkyl C4-C7 carbocylo alkenyl, a heterocycle, an ether having 2 to 10 carbon atoms and 1 to 4 oxygen or sulfur atoms, a polyalky glycol, or C7-C14 aralkyl; j and k independently are 0 or 1; Z1 and Z2 independently are H, C1-C2 alkyl, C2-C20 alkenyl, C2-C20 alkynyl, C6-C14 aryl, C7-C15 aralkyl, halogen, CH&boxH;O, OR12, SR12, NR12R13, C(&boxH;NH)NR12R13 CH(NR12R13), NHC(&boxH;NH)NR12R13, CH(NH2)C(&boxH;O)OH, C(&boxH;O)NR12R13, C(&boxH;O)OR12, a metal coordination group, a reporter group, a nitrogen-containing heterocycle, a purine, a pyrimidine, a phosphate group, a polyether group, or a polyethylene glycol group; and provided that at least one of said aminodiol monomer subunits in said oligomeric compound does not have structure III.