Patent ID: 7271154

Claim:
A conjugate of the following formula: wherein T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is an antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative and the conjugate has the formula: wherein X=N(R 7 )—CH 2 CH 2 —N(R 7 )C(═O) C(═NOR 8 ) C(OH)(R 9 ) CH(NR 10 R 11 ) C(═NR 12 ) Y=independently a bond or a linker Z=C(═O) CH(R 16 ) R 1 =H CH 3 (C 2 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl (C 1 -C 4 )alkyliden-NR 18 R 19 Y—R 13 C(═O)—Y—R 15 C(═O)—R 15 R2=H OH SCH 3 ; R 3 =H C(═O)—Y—R 15 C(═O)—R 15 R 4 =H C(═O)—Y—R 15 C(═O)—R 15 R 5 =H or R 4 , R 5 are connected by Z R 6 =H CH 3 R 7 =H CH 3 Y—R 13 C(═O)—Y—R 15 C(═O)—R 15 R 8 =H Y—R 13 C(═O)—R 17 R 9 =H (C 1 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl R 10 ,R 11 =independently, H (C 1 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl (C 1 -C 4 )alkyliden-NR 18 R 19 or R 10 =H and R 11 =Y—R 13 C(═O)—Y—R 15 C(═O)—R 15 R 12 =independently, H (C 1 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl (C 1 -C 4 )alkyliden-NR 18 R 19 Y—R 13 R 13 =independently, an antibiotic therapeutic agent R 15 =independently, an antibiotic therapeutic agent R 16 =independently, H CH 3 (C 2 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl (C 1 -C 4 )alkyliden-NR 18 R 19 Y—R 13 , R 17 =(O—R 20 -aryliden)(C 1 -C 10 )alkyl R 18 , R 19 =independently, H (C 1 -C 10 )alkyl (C 1 -C 10 )alkenyl (C 1 -C 10 )alkynyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkyl (C 1 -C 8 )[(C 1 -C 4 )alkoxy]alkenyl (C 6 -C 10 )aryl-(C 1 -C 5 )alkyl (C 2 -C 9 )heteroaryl-(C 1 -C 5 )alkyl R 20 =independently, Halogen (C 1 -C 3 )alkyl NO 2 CN OCH 3 N(CH 3 ) 2 .