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a cytokine release inhibitor and inflammatory technology, applied in the field of pharmaceutical compositions, can solve the problems of inconvenient long-term use, drug is also aspirin is not suitable for long-term use, so as to avoid side effects and inhibit the effect of activity
Inactive Publication Date: 2008-10-09
INST OF MEDICINAL MOLECULAR DESIGN
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[0009]Therefore, an object of the present invention is to provide medicaments useful for preventive and / or therapeutic treatment of inflammatory disorders, autoimmune disease such as chronic arthrorheumatism, and bone disease such as osteoporosis, in which inflammatory cytokine is participated. Another object of the present invention is to provide an inhibitor against release of an inflammatory cytokine which avoids side effects by specifically inhibiting IKK-β, and has inhibitory activity against N F-κ B activation.
Problems solved by technology
However, since huge amount of aspirin needs to be administered to sufficiently suppress NF-κ B activation, and as a result, since possibility of side effects such as gastrointestinal disorders by prostaglandin synthesis inhibition and increase of bleeding tendency by anticoagulation is expected with high probability, aspirin is not suitable for long term application.
However, long term use is not suitable, because they have serious side effects such as aggravation of an infectious disease, generation of peptic ulcer, degradation of bone density, and central action.
Leflunomide as an immunosuppressive agent, as an isoxazole-type agent, also has NF-κ B inhibitory action (Manna S., et al., J. Immunol., 164, 2095-2102 (1999)), however, the drug is also not suitable for long term use due to serious side effects.
Method used
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example 1
Preparation of N-{[3,5-bis(trifluoromethyl)phenyl]methyl}-5-bromo-2-hydroxybenzamide
Compound No. 1
[0491]Under argon atmosphere, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (it is abbreviated as WSC.HCl hereafter.; 192 mg, 1 mmol) was added to a mixture of 5-bromosalicylic acid (217 mg, 1 mmol), 3,5-bis(trifluoromethyl)benzylamine (243 mg, 1 mmol), 4-dimethylaminopyridine(12 mg, 0.1 mmol) and tetrahydrofuran (10 mL), and the mixture was stirred at room temperature for 1 hour. The reaction mixture was poured into diluted hydrochloric acid and extracted with ethyl acetate. After the organic layer was washed with water and brine, dried over anhydrous magnesium sulfate, the residue obtained by evaporation under reduced pressure was purified by chromatography on silica gel(n-hexane:ethyl acetate=4:1) to give the title compound(244.8 mg, 55.4%) as a white solid.
[0503]This compound is a commercially available compound.
Supplier: Specs.
[0504]Catalog code number: AI-233 / 31581024.
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Abstract
A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient:wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application is a Divisional of U.S. application Ser. No. 10 / 433,619, which is a National Stage of PCT / JP2001 / 011084, filed Dec. 18, 2001, which was not published in English under PCT Article 21(2), and which claims priority of Japanese Application No. 2000-383202, filed Dec. 18, 2000. The entire disclosure of application Ser. No. 10 / 433,619 is considered as being part of this application, and the entire disclosure of application Ser. No. 10 / 433,619 is expressly incorporated by reference herein in its entirety.FIELD OF INVENTION[0002]The present invention relates to pharmaceutical compositions having inhibitory activity against the production and release of inflammatory cytokines such as interleukin (IL)-1, IL-6, IL-8 and tumor necrosis factor (TNF-α), and having inhibitory activity against the activation of NF-κ K B.BACKGROUND ART[0003]Inflammation is a basic defense mechanism to various infestations, where inflammatory cytoki...
Claims
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Patent Type & Authority Applications(United States)
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