產品資訊 - Iguratimod intermediate cas 149436-41-9 cas 149457-03-4->active pharmaceutical ingredient

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Iguratimod intermediate cas 149436-41-9 cas 149457-03-4

產品分類 :

化學->活性醫療成份

Iguratimod intermediate cas 149436-41-9 cas 149457-03-4

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產品描述

Chemical Name:


N-(4-(2-aminoacetyl)-5-methoxy-2-phenoxyphenyl)methanesulfonamide hydrochloride


Molecular Formula: C16H19ClN2O5S


Formula Weight: 386.85


CAS No.: 149436-41-9


 <img src="http://i.bosscdn.com/product/df/6b/99/6dd790f9f88871491e6cef0f4a.gif" title="149436-41-9" alt="149436-41-9" />


Chemical Name: MethanesulfonaMide, N-[4-[2-(forMylaMino)acetyl]-5-hydroxy-2-phenoxyphenyl]-


Molecular Formula: C17H18N2O6S


Formula Weight: 378.39962


CAS No.: 149457-03-4


 <img src="http://i.bosscdn.com/product/f8/39/e1/08f5dde1fae519b0c26bf079b4.gif" title="149457-03-4" alt="149457-03-4" width="200" height="99" />


Chemical Name: Iguratimod


Molecular Formula: C17H14N2O6S


Formula Weight: 374.37


CAS No.: 123663-49-0


 <img src="http://i.bosscdn.com/product/66/ee/97/ced27285280b68c59bfdc33241.gif" title="123663-49-0" alt="123663-49-0" />


Iguratimod is an anti-inflammatory small molecule drug used for the treatment of rheumatoid arthritis, together with methotrexate in Japan and China. As of 2015 the biological target was not known, but it prevents NF-κB activation and subsequently selectively inhibits COX-2 and several inflammatory cytokines.


 


Iguratimod is under investigation in Rheumatoid Arthritis.


Iguratimod, a methanesulfonanilide, is a novel disease-modifying antirheumatic drug that has been developed exclusively in Japan and China. It inhibits the production of immunoglobulins and various inflammatory cytokines (interleukin-1, -6 and -8 and TNF), and exerts anabolic effects on bone metabolism by stimulating osteoblastic differentiation and inhibiting osteoclastogenesis. On the molecular level, it inhibits the nuclear transcription factor NF-κB but not its inhibitor, IκBα. In addition to these immunomodulatory and other long-lasting effects, iguratimod inhibits cyclooxygenase-2, which provides a synergistic short-term action against pain and inflammation. Efficacy and tolerability are comparable to salazosulfapyridine, and probably also to methotrexate. Combination with methotrexate is synergistic in patients with insufficient response to methotrexate and does not significantly increase adverse events. Liver enzyme elevations and thrombocytopenia are the most significant side effects to watch for. In summary, iguratimod is a welcome addition to the small-molecule drug therapy of rheumatoid arthritis.


 
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