Anti-inflammatory pharmaceutical composition comprising benzopyranyl tetracycles
AssigneesSeoul National University R&Db Foundation, Kyungpook National University Industry-Academic Cooperation Foundation, Kyungpook National University Hospital
InventorsSeung Bum Park, Sanghee Lee, Ja Young Koo, Donghyun Lim, Jongmin Park, Kyoungho Suk, Youngpyo Nam
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Abstract
Disclosed herein is an anti-inflammatory pharmaceutical composition comprising a benzopyranyl tetracycle compound represented by Chemical Formula 1 as an active ingredient. The compound exhibits excellent anti-inflammatory activity by perturbing the post-translational modification of the inflammation mediator HMGB, and thus finds applications in pharmaceutical compositions superior in the treatment or prevention of inflammation-related diseases.
Claims6
A method of treating inflammation-related disease, comprising the administration of a therapeutically effective amount of an anti-inflammatory pharmaceutical composition, wherein the anti-inflammatory pharmaceutical composition comprises a compound represented by the following Chemical Formula 1 as an active ingredient:
- wherein,
- n of (R1)n is an integer of 1 to 4, with the proviso that when n is 2 or greater, R1, which is identical or different, each is independently a hydrogen atom;
- hydroxy;
- halogen;
- C1˜C6 linear or branched alkyl;
- C3˜C10 cycloalkyl;
- C1˜C6 linear or branched alkoxy;
- C2˜C20 heterocycloalkyl containing N, O or S as a heteroatom;
- phenyl, unsubstituted or substituted with at least one selected from the group consisting of a halogen atom, amino, nitryl, nitro, C1˜C30 alkyl, C2˜C30 alkenyl, C1˜C30 alkoxy, C3˜C30 cycloalkyl, C3˜C30 heterocycloalkyl containing N, O or S as a heteroatom, C6˜C30 aryl, and C5˜C30 heteroaryl containing N, O or S as a heteroatom;
- benzyl, unsubstituted or substituted with at least one selected from the group consisting of a halogen atom, amino, nitryl, nitro, C1˜C30 alkyl, C2˜C30 alkenyl, C1˜C30 alkoxy, C3˜C30 cycloalkyl, C3˜C30 heterocycloalkyl containing N, O or S as a heteroatom, C6˜C30 aryl, and C5˜C30 heteroaryl containing N, O or S as a heteroatom;
- benzoyl;
- C1˜C30 alkyl amino;
- C2˜C30 dialkyl amino;
- or C1˜C30 alkoxy,
- R2 and R2′, which may be identical or different, are each a hydrogen atom;
- hydroxy;
- halogen;
- C1˜C6 linear or branched alkyl;
- C3˜C10 cycloalkyl;
- C1˜C6 linear or branched alkoxy;
- C2˜C20 heterocycloalkyl containing N, O or S as a heteroatom;
- phenyl, unsubstituted or substituted with at least one selected from the group consisting of a halogen atom, amino, nitryl, nitro, C1˜C30 alkyl, C2˜C30 alkenyl, C1˜C30 alkoxy, C3˜C30 cycloalkyl, C3˜C30 heterocycloalkyl containing N, O or S as a heteroatom, C6˜C30 aryl, and C5˜C30 heteroaryl containing N, O or S as a heteroatom;
- N-acetyl-4′-piperidyl;
- N-propyl-4′-piperidyl;
- or —(CH2)mX wherein m is an integer of 0 to 20, X is C2˜C30 alkylester, C1˜C30 alkylamide, C2˜C30 alkylether, or carboxylic acid;
- or R2 and R2′ may form a ring, together,
- R3 is a hydrogen atom;
- C1˜C6 linear or branched alkyl;
- C3˜C10 cycloalkyl;
- C1˜C6 linear or branched alkoxy;
- phenyl, unsubstituted or substituted with at least one selected from the group consisting of a halogen atom, amino, nitryl, nitro, C1˜C30 alkyl, C2˜C30 alkenyl, C1˜C30 alkoxy, C3˜C30 cycloalkyl, C3˜C30 heterocycloalkyl containing N, O or S as a heteroatom, C6˜C30 aryl, and C5˜C30 heteroaryl containing N, O or S as a heteroatom;
- C2˜C20 heterocycloalkyl containing N, O or S as a heteroatom;
- benzyl, unsubstituted or substituted with at least one selected from the group consisting of a halogen atom, amino, nitryl, nitro, C1˜C30 alkyl, C2˜C30 alkenyl, C1˜C30 alkoxy, C3˜C30 cycloalkyl, C3˜C30 heterocycloalkyl containing N, O or S as a heteroatom, C6˜C30 aryl, and C5˜C30 heteroaryl containing N, O or S as a heteroatom;
- p-methylphenyl, m-methylphenyl, o-methylphenyl;
- p-tert-butylethylphenyl, m-tert-butylethylphenyl, or o-tert-butylethylphenyl;
- p-methoxyphenyl, m-methoxyphenyl, or o-methoxyphenyl;
- p-fluorophenyl, m-fluorophenyl, or o-fluorophenyl;
- p-iodophenyl, m-iodophenyl, or o-iodophenyl;
- p-nitrophenyl, m-nitrophenyl, or o-nitrophenyl;
- p-chlorophenyl;
- m-chlorophenyl, or o-chlorophenyl;
- or p-bromophenyl, m-bromophenyl, or o-bromophenyl.
Dependencies are inferred from the claim text.