ミノドロナート一水和物

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H301：飲み込むと有毒

  H361：生殖能または胎児への悪影響のおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

ミノドロナート一水和物 価格

ミノドロナート一水和物 化学特性,用途語,生産方法

• 外観

  白色～うすい黄色～うすい赤色粉末～結晶

• 効能

  骨吸収抑制薬, 骨粗鬆症治療薬, ファルネシルピロリン酸合成酵素阻害薬

• 商品名

  ボノテオ (アステラス製薬); ボノテオ (アステラス製薬); リカルボン (小野薬品工業); リカルボン (小野薬品工業)

• 作用機序

  Third-generation bisphosphonates, including minodronic acid hydrate, contain an amino group in the imidazole ring and are even more powerful inhibitors of bone resorption. With regard to inhibition of bone resorption, minodronic acid hydrate is 1000 times more effective than etidronate and 10–100 times more effective than alendronic acid. Following administration, minodronic acid hydrate specifically accumulates in the bone. It is then separated from the bone by acid released by osteoclasts during the bone resorption process and selectively taken up by osteoclasts. Conventional bisphosphonates were believed to inhibit bone resorption through the induction of osteoclast apoptosis after being taken up by these cells[1].

• 臨床応用

  The bone resorption inhibitor minodronic acid hydrate was approved and introduced last year in Japan, bringing the total number of bis-phosphonates marketed for this indication to seven. There are an estimated 10 million current and potential osteoporosis sufferers in Japan, a number that is expected to continue growing due to the country’s aging population. Minodronic acid is the first drug to show a significant effect in preventing bone fractures as compared to placebo in a Japanese patient population. Minodronic acid was co-developed by Astellas and Ono, who are marketing the drug as Bonoteo and Recalbon, respectively.

• 合成

  Several syntheses of minodronic acid have been reported,a scalable preparation is described in the scheme. Commercially available acid chloride 71 was first reduced with lithium tritertbutoxy aluminum hydride to the aldehyde 72 at 80??C in 61% yield. Next, reaction of aldehyde 72 with TMSCl and triethylamine generated the corresponding silyl enol ether, which was then treated with bromine to give a-bromoaldehyde 73 in 62% yield. Condensation with 2-amino pyridine furnished imidazopyridine 74, which was hydrolyzed with HCl to acid 75 in 58% yield. Reaction with H3PO3 at 120??C to provide minodronic acid hydrate (XII) in 53% yield.

  

ミノドロナート一水和物 生産企業

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155648-60-5, ミノドロナート一水和物 キーワード