Composition for the prevention or treatment of TNF-related diseases containing a novel derivative as an active ingredient, and method for inhibiting TNF activity using the same.

JP7893838B2Active Publication Date: 2026-07-22アイラブ カンパニー リミテッド
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
アイラブ カンパニー リミテッド
Filing Date
2024-07-04
Publication Date
2026-07-22

AI Technical Summary

Benefits of technology

【0008】 本願発明は、4-ベンゾピラノン誘導体化合物を有効成分として含むTNF-関連疾患の予防または治療用の組成物に関し、既存のタンパク質TNF-阻害バイオ医薬品は、他の化合物治療剤と併用投与するのに不都合であり、複合剤の開発も不可能であったが、本願発明が提供するTNF-阻害化合物は、既存の他の化合物治療剤との併用投与または複合剤の開発が非常に容易であり、さらには、優れた効能、低費用、非侵襲的な経口投与、非免疫原性、冷蔵保管の不要などの長所を有するため、TNF-関連疾患の予防または治療用の組成物として有用に活用できる。

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Patent Text Reader

Abstract

To provide a composition for preventing, alleviating or treating TNF-related diseases, containing a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate or stereoisomer thereof as an active ingredient; and a method for treating TNF-related diseases using the composition, a reagent composition for inhibiting TNF, and a method for inhibiting TNF.SOLUTION: The invention relates to: a composition for preventing, alleviating or treating TNF-related diseases, containing a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate or stereoisomer thereof as an active ingredient; and a method for treating TNF-related diseases using the composition, a reagent composition for inhibiting TNF, and a method for inhibiting TNF. The composition can be orally administered so as not to cause injection side effects and immunological tolerance, and can effectively inhibit TNF activity by directly binding to TNF while facilitating co-administering with a conventional oral preparation and dosage control.SELECTED DRAWING: Figure 5a
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Claims

1. A pharmaceutical composition for the prevention or treatment of TNF-overexpression disease, wherein the TNF-overexpression disease is rheumatoid arthritis, and the pharmaceutical composition is characterized by comprising 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone or a pharmaceutically acceptable salt thereof.

2. The pharmaceutical composition for the prevention or treatment of TNF-overexpression disease according to claim 1, further comprising a drug.

3. The aforementioned drugs include methotrexate, hydroxychloroquine, sulfasalazine, leflunomide, bucillamine, cyclosporine, tacrolimus, azathioprine, cyclophosphamide, mizoribine, penicillamine, oral gold preparations, antimalarial agents, 6-mercaptopurine, indomethacin, naproxen, sulindac, diclofenac, aceclofenac, mefenamic acid, aspirin, fenoprofen, sarsalate, piroxicam, etodolac, flurbiprofen, ibuprofen, loxoprofen, nabumetone, lonazolac, meloxicam, and fenbufen. Indoprofen, ketrolactromethamine, indoprofen, ketoprofen, suprofen, carprofen, tiaprofenic acid, flufenamic acid, ebuselene, felbinac, tolmetin, flunixin, celecoxib, lofecoxib, hydrocortisone, cortisone, prednisolone, methylprednisolone, triamcinolone, betamethasone, dexamethasone, fludrocortisone, entocort, 5-aminosalicylic acid, 6-thioguanine, cytarabine, 5-fluorouracil, dacarbazine, mechloretamine, thiotepa, chlorambucil, melfa Lan, Carmustine, Lomustine, Busulfan, Sestrin 2, Withaferin A, Cerastrol, Quercetin, Luteolin, Curcumin, Metformin, Dibromomannitol, GR270773, Pentoxifylline, N-Acetylcysteine, Melatonin, Resveratrol, Mesalamine, Single-chain fatty acids, Glutamine, Gemfibrozil, Retinoids, Hydroxyurea, Trihydroxyisoflavones, Deoxykaemperol, Kaempferol, Gingerol, Caffeic acid, Cyanidin, Cryptotancinone, Deguerin, Delphinidin, Equol Fisetin, Myricetin, Procyanidin B2, Metronidazole, Ciprofloxacin, Niclosamide, Thiabendazole, Imipenem-Cilastatin, Fluoroquinolone, Tofacitinib, Glybride, Rolipram, Doxycycline, VX-166, zVAD, L-97-1, ISO-1, Tauroursodeoxycholic acid, HK-156, A-285222, CP-0127, Bis-N-Norgliovictin, Aurintricarboxylic acid, Chloromidine, Ouabain, Terazosin, Prazosin, Tranilast,Apremilast, monobenzone, phenazopyridine, 546C88, NOX-100, gabexate mesylate, urinastatin, somatostatin, octreotide, IKK inhibitor, caspase inhibitor, TAK-242, erythritol, ki16425, camptothecin, phenethyl caffeate, sulforaphane, Tim-3, BN-52021, BB-882, TCV-309, CT-400, ethyl pyruvate, hemin, CORM-2, tancinone IIA sulfonate, nicotine, EGCG, isorhamnetin-3-O-galactoside, persica Phosphorus, catechin, carbenoxolone, glycyrrhizin, emodin-6-O-b-D-glucoside, acteoside, forcitoside B, rosmarinic acid, chlorogenic acid, infliximene, cilostazol, clopidogrel, sarpogrelate, dorotrecodin α, carbamazepine, chloroquine, anakinra, tocilizumab, LMT-28, 1-(3-dimethylaminopropyl)-3-ethylurea, gp130Fc, β-arrestin 2, IL-30, diacelein, secukinumab, ustekinumab, ixekizumab, thalidomide, adalimumab, inflixima Pravastatin, Atorvastatin, Rosuvastatin, Simvastatin, Losartan, Telmisartan, Hydrochlorothiazide, Furosemide, Propranolol, Metoprolol, Captopril, Amlodipine, Clonidine, Methyldopa, Minoxidil, Streptozotocin, Mitomycin, Cisplatin, Daunorubicin, Doxorubicin, Dactinomycin, Bleomycin, Mitramycin, Anthramycin, Calicaemicin, Duocalmycin, Taxol, Docetaxel, Cytochalasin B, Gramicidin D, Ethidium Bromide, Emeth Mitomycin, etoposide, teniposide, vincristine, vinblastine, colchicine, dihydroxyanthracendione, mitoxantrone, mitramycin, actinomycin D, 1-dehydrotestosterone, procaine, tetracaine, lidocaine, propranolol, tamoxifen, bazedoxifen, puromycin, anethole trithione, nivolumab, pembrolizumab, ipilimumab, atezolizumab, α-galactosylceramide, SRT3025, DTA-1, IL-7, IL-2, IL-15, CXCL1, ATRA,A pharmaceutical composition for the prevention or treatment of TNF-overexpression disease according to claim 2, characterized by being selected from the group consisting of gemcitabine, carboplatin, NCX-4016, CDDO-Me, sunitinib, zoledronic acid, astragalus polysaccharide, rituximab, Imuran, abatacept, GW9662, rosiglitazone, Y-27632, and alefacept.

4. A functional food composition for the prevention or improvement of TNF-overexpression disease, wherein the TNF-overexpression disease is rheumatoid arthritis, and the functional food composition is characterized by containing 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone or a pharmaceutically acceptable salt thereof as an active ingredient.

5. A reagent composition for inhibiting TNF activity in vitro in TNF-overexpression diseases, wherein the TNF-overexpression disease is rheumatoid arthritis, and the reagent composition is characterized by containing 2-(2,5-difluorophenyl)-3-carboxy-7-chloro-(4H)-4-benzopyranone or a pharmaceutically acceptable salt thereof as an active ingredient.