| 主权项 |
1. A compound of Formula (I):
F1-L1-T-L2-F2 (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: F1 and F2 are each independently selected from ring systems A, B, C, D, E, F, G and H where: at least one of the ring systems A, B, C and D is present; each R is independently selected from the group consisting of H, —C1-C20 alkyl, —C2-C6 alkenyl, —C2-C6 alkynyl, halo, deuterium, hydroxyl, alkoxy, —NH2, —NH(C1-C8 alkyl), —N(C1-C8 alkyl)2, —NO2, —C6-C14 aryl and —C6-C14 heteroaryl, wherein two or more R optionally join to form a ring or rings, and wherein said —C6-C14 aryl and —C6-C14 heteroaryl are optionally substituted with 1 to 5 substituents independently selected from —C1-C10 alkyl, —C1-C10 alkoxy, -halo, —C1-C10 alkylthio, -trifluoromethyl, —NH2, —NH(C1-C8 alkyl), —N(C1-C8 alkyl)2, —C1-C10 alkyl-N(C1-C8 alkyl)2, —C1-C3 alkylthio, —NO2 or —C1-C10 heterocyclyl, for each ring system in which R appears; each V1 independently a bond, O, N(R) or S, for each ring system in which V1 appears; each V2 is independently O, N(R) or S, for each ring system in which V2 appears; W1 and W2 are each independently H, —C1-C5 alkyl, -phenyl, —C(O)OR, —C(O)SR, —C(O)NHN(R)2 or —C(O)N(R)2 for each ring system in which W1 and W2 appear; each X is independently —OH, —O-acyl, azido, halo, cyanate, thiocyanate, isocyanate, thioisocyanate, or for each ring system in which X appears; each Y is independently selected from the group consisting of H, —C1-C6 alkyl-RA, —C(O)RA, —C(S)RA, —C(O)ORA, —S(O)2ORA, —C(O)N(RA)2, —C(S)N(RA)2, glycosyl, —NO2, —PO(ORA)2, an amino acid, and a peptide, for each ring system in which Y appears, wherein each RA is independently selected from the group consisting of H, —C1-C20 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl and —C1-C20 alkylN(R)2, wherein said —C1-C20 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl and —C1-C20 alkylN(R)2 are optionally substituted with 1 to 3 substitutents independently selected from R; each Z is independently selected from the group consisting of H, —C1-C8 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, -aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl, —C(O)OC1-C8 alkyl, —C(O)N(C1-C8 alkyl)2, —C(O)OH, —C(O)NHNH2, and —C(O)-halo, and wherein said C1-C8 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, -aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl, —C(O)OC1-C8 alkyl, —C(O)N(C1-C8 alkyl)2, —C(O)OH, —C(O)NHNH2 and —C(O)-halo are each optionally substituted with 1 to 3 substitutents independently selected from R, for each ring system in which Z appears; L1 and L2 are each independently selected from a direct bond, carbonyl, or a carbonyl acyl group bonded to F1 or F2 at the acyl moiety, where the carbonyl acyl group is selected from the group consisting of: wherein U1 is selected from H, —CH3, —OH, —OCH3, —NO2, —NH2, —NHNHAc, —NHNHC(O)CH3, —NHC(O)phenyl or -halo, U2 is H, —OH or —OCH3, U3 is H, —CH3 or —C2H5, U4 is H or CH3S—, U5 and U6 are each independently selected from H, -halo, —C1-C4 alkyl, —C1-C3 alkoxy, —C1-C6 dialkylamino, —NO2, —NHC(O)C1-C10 alkyl, —OH, —NH2, —NHC(O)NH2, —NHC(O)CH3 or —NHC(O)phenyl, Q1 is —O—, —S—, or —NH—, and Q2 and Q3 are each independently —CH— or —N—; T is selected from: —NHC(O)—, —C(O)NH—, —C(O)O—, —OC(O)—, —NRB-T1-NRC— where RB and RC are each independently H or —C1-C8 alkyl, or together RB and RC join to form a ring and together are (CH2)2-3, where T1 is selected from the group consisting of —C(O)—, —C(O)(CH2)nC(O)— where n is an integer from 0 to 50 and —C(O)PhC(O)— where Ph is 1,3- or 1,4-phenylene, and where T1 is optionally substituted with 1-2 R, —C(O)hetC(O)— wherein het is a mono-, bi-, or tricyclic heteroaryl of 5 to 12 members, containing one, two, or three heteroatoms independently selected from O, N, S, P and B, wherein het is optionally substituted with 1 to 8 substituents each independently selected from the group consisting of —C1-C8 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclycl, —NH2, —NHRD and —NO2, and said optional substituents on het are optionally substituted with RE, wherein each RD is independently selected from the group consisting of H, —C1-C8 alkyl, —C(O)—C1-C8 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, -aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl, —C(O)OC1-C8 alkyl, —C(O)N(C1-C8 alkyl)2, and —C(O)-halo, optionally substituted with RE, wherein each RE is independently selected from the group consisting of H, —C1-C8 alkyl, —C1-C8 heteroalkyl, —C6-C14 aryl, -aralkyl, —C1-C10 heterocyclyl, —C3-C8 carbocyclyl, —C(O)OC1-C8 alkyl, —C(O)N(C1-C8 alkyl)2, and —C(O)-halo, and wherein each RE is optionally substituted with 1 to 3 substitutents independently selected from R, —C(A1)X1-T2-X1C(B1)—, where T2 is: wherein each X1 is independently a bond, —NRE—, —O— or —S—, wherein A1 and B1 are each independently ═O or ═S, wherein R1, R2, R3, and R4 are each independently RE or R1 and R2 form a ring system, or R3 and R4 form a ring system, or both R1 and R2, and R3 and R4, each independently form ring systems, or R1 and R3 form a ring system, or R2 and R4 form a ring system, or both R1 and R3, and R2 and R4, each independently form ring systems, where said ring systems are independently selected from —C1-C10 heterocyclyl or —C3-C8 carbocyclycl, or R1, R2, R3 and R4 are each bonds to different carbons on D, wherein g and j are each independently an integer from 0 to 50 and m is an integer from 1 to 50, and wherein D is a bond or is selected from the group consisting of —S—, —C1-C8 alkylene-, —C6-C14 arylene-, —C6-C14 heteroarylene-, —C1-C8 heteroalkylene-, -aralkylene, —C1-C10 heterocyclo and —C3-C8 carbocyclo, where said —C1-C8 alkylene-, —C6-C14 arylene-, —C6-C14 heteroarylene-, —C1-C8 heteroalkylene-, -aralkylene, —C1-C10 heterocyclo and —C3-C8 carbocyclo are optionally substituted with —RE, —C(O)RE, —C(O)ORE, —N(RE)2, —N(R)C(O)RE or —N(R)C(O)ORE, and D is additionally optionally substituted by 1 to 2 R, and -G1-T2-G2-, where G1 and G2 are each independently —S(O)X1— or —S(O)2X1—. |
