| 摘要 |
Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hapatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. |
| 主权项 |
1. 1,3-Dioxoindene derivatives expressed by Formula 1, pharmaceutically-acceptable salt thereof or optical isomer thereof: where, A1, A2, A3 and A4 are, either independently or optionally, any one selected from a group consisting of —H, halogen, —OH, —CN, —N3, C1˜C10 alkoxy, C1˜C10 straight- or side-chain alkyl, C6˜C12 aryl, —O(C═O)R1, —(C═O)R1, —(C═O)OR1, —O(C═O)OR1, —O(C═O)NR1R2, —NO2, —NR1R2, —NR1 (C═O)R2, —NR1(C═S)R2, —NR1(C═O)OR2, —NR1(C═O)—NR2R3 and —NR1(C═S)—NR2R3, or two or more neighboring substituents of A1, A2, A3 and A4 may form a ring together, wherein a ring formed by two or more neighboring substituents of D1, D2, D3 and D4 may include one or more hetero atom, and the hetero atom is N, O or S; G is —H, halogen, —OH, —CN, —N3, C1˜C10 alkoxy, —O(C═O)R1, —(C═O)R1, —(C═O)OR1, —O(C═O)OR1, —O(C═O)NR1R2, —NO2, —NR1R2, —NR1(C═O)R2, —NR1(C═S)R2, —NR1(C═O)OR2, —NR1(C═O)—NR2R3, —NR1(C═S)—NR2R3 or D1, D2, D3 and D4 are, either independently or optionally, any one selected from a group consisting of —H, halogen, —OH, —CN, C1˜C10 alkoxy, C1˜C10 straight- or side-chain alkyl, C6˜C12 aryl, —(CH2)n—(C═O)OR1, —O(C═O)R1, —(C═O)R1, —(C═O)OR1, —O(C═O)OR1, —O(C═O)NR1R2, —NO2, —NR1R2, —NR1(C═O)R2, —NR1(C═S)R2, —NR1(C═O)OR2, —NR1(C═O)—NR2R3, —SR1 and —NR1(C═S)—NR2R3, or two or more neighboring substituents of D1, D2, D3 and D4 may for a ring together, a ring formed by two or more neighboring substituent of D1, D2, D3 and D4 may include one or more hetero atom, and the hetero atom is N, O or S; E is —H, —OH, —OR1, —O(C═O)R1, —(C═O)R1, —(C═O)OR1, —O(C═O)OR1, —O(C═O)NR1R2, —NO2, —NR1R2, —NR1 (C═O)R2, —NR1(C═S)R2, —NR1(C═O)OR2, —NR1(C═O)—NR2R3 or —NR1(C═S)—NR2R3; R1, R2 and R3 are, each independently, hydrogen, nonsubstituted or phenyl-substituted C1˜C10 straight- or side-chain alkyl, C1˜C10 alkoxy, nonsubstituted or phenyl-substituted C1˜C10 straight- or side-chain alkenyl, C3˜C7 cycloalkyl or nonsubstituted or phenyl-substituted C6˜C12 aryl; X and Y are, each independently, hydrogen, oxygen, hydroxy or sulfur; Z1, Z2 and Z3 are carbon or nitrogen; n is integer between 1˜10; and ‘’ denotes single or double bond. |
